The research library
Every study cited on a Tasman compound page, collected in one table. Search by title or finding, or filter by compound, model and year. Each row links to its PubMed record so you can read the source yourself.
Each study in the library is a PubMed record, linked by its PMID and, where one exists, its DOI. The model is always stated, so a human trial, an animal study and a cell-culture experiment are never presented as the same kind of evidence. Doses are reported as the study used them; they are a record of the method, not a recommendation.
236 studies
| Study | Compound | Model | Dose used | Duration | Finding |
|---|---|---|---|---|---|
| Babula JJ et al.2024 · Diabetes Obes Metab · DOINicotinamide N-methyltransferase inhibition mitigates obesity-related metabolic dysfunction. | 5-Amino-1MQ | Mouse, diet-induced obese (DIO) mice; plus pharmacokinetics in age- and strain-matched mice | Not stated in the abstract (once daily); PK after intravenous, oral and subcutaneous dosing | 28 days | 5A1MQ dose-dependently limited body weight and fat mass gains, improved oral glucose tolerance and insulin sensitivity, and reduced hepatic steatosis and liver triglycerides. ALT, AST and ketone bodies were normalised, and subcutaneous dosing distributed it to adipose, muscle and liver. |
| Yang M et al.2024 · J Immunother Cancer · DOINAD+ metabolism enzyme NNMT in cancer-associated fibroblasts drives tumor progression and resistance to immunotherapy by modulating macrophages in urothelial bladder cancer. | 5-Amino-1MQ | Mouse, urothelial bladder cancer models; plus human bladder cancer tissue cohorts (association data) | Not stated in the abstract (5-amino-1-methylquinolinium iodide) | Not stated in the abstract | Targeting NNMT with 5-amino-1-methylquinolinium iodide reduced tumour growth and enhanced the apoptotic effects of an anti-PD-L1 antibody in mouse models. The human data were associations between NNMT in tumour fibroblasts and non-response to immunotherapy. |
| Dimet-Wiley A et al.2022 · Sci Rep · DOIReduced calorie diet combined with NNMT inhibition establishes a distinct microbiome in DIO mice. | 5-Amino-1MQ | Mouse, diet-induced obese mice switched to a low-fat diet | Not stated in the abstract (5-amino-1-methylquinolinium with low-fat diet) | Not stated in the abstract | Mice given 5-amino-1MQ plus the low-fat diet had a distinct caecal microbiome, with less Erysipelatoclostridium and more Lactobacillus than vehicle-treated mice on the same diet. The abstract notes the combination normalised adiposity and weight to those of lean mice. |
| Awosemo O et al.2021 · J Pharm Biomed Anal · DOIDevelopment & validation of LC-MS/MS assay for 5-amino-1-methyl quinolinium in rat plasma: Application to pharmacokinetic and oral bioavailability studies. | 5-Amino-1MQ | Rat, pharmacokinetic study with a validated LC-MS/MS assay | Not stated in the abstract (intravenous and oral) | Not stated in the abstract | 5-AMQ reached substantial plasma exposure by both routes, with a mean maximum plasma concentration of 2252 ng/mL after oral dosing. The first terminal half-life reported was 3.80 ± 1.10 h; the stored abstract is cut off before the second value. |
| Akar S et al.2021 · J Obstet Gynaecol · DOISmall molecule inhibitor of nicotinamide N-methyltransferase shows anti-proliferative activity in HeLa cells. | 5-Amino-1MQ | Cell culture (HeLa cervical cancer cells, HEK-293 cells) | 0.1–500 µM 5MQ (5-amino-1-methylquinolinium) | Not stated in the abstract | 5MQ inhibited HeLa cell proliferation in a concentration- and time-dependent manner, with signs of apoptosis and lower phospho-Akt and SIRT1 protein. HEK-293 cell proliferation was not apparently affected. |
| Neelakantan H et al.2019 · Biochem Pharmacol · DOISmall molecule nicotinamide N-methyltransferase inhibitor activates senescent muscle stem cells and improves regenerative capacity of aged skeletal muscle. | 5-Amino-1MQ | Mouse, 24-month-old mice with barium chloride tibialis anterior injury, plus C2C12 myoblasts; NNMT inhibitor from the same group (the abstract does not name the compound) | 5 or 10 mg/kg NNMTi, or saline control | 1 week or 3 weeks after injury | Muscle stem cell proliferation and fusion increased, myofiber cross-sectional area was nearly 2-fold greater and peak torque of the injured muscle was about 70% higher than in controls. |
| Neelakantan H et al.2018 · Biochem Pharmacol · DOISelective and membrane-permeable small molecule inhibitors of nicotinamide N-methyltransferase reverse high fat diet-induced obesity in mice. | 5-Amino-1MQ | Cell culture (adipocytes, Caco-2 permeability) and mouse, diet-induced obese mice; methylquinolinium NNMT inhibitor series (the abstract does not name the compound used in mice) | Not stated in the abstract | Not stated in the abstract | The inhibitors reduced 1-MNA, raised NAD+ and SAM and suppressed lipogenesis in adipocytes. In obese mice, a potent inhibitor reduced body weight, white fat mass, adipocyte size and plasma cholesterol without changing food intake or producing observable adverse effects. |
| Kwon DR et al.2015 · Ann Clin Lab SciEffect of Intra-articular Injection of AOD9604 with or without Hyaluronic Acid in Rabbit Osteoarthritis Model. | AOD-9604 | Rabbit, collagenase-induced knee osteoarthritis model (n=32) | 0.25 mg AOD9604 intra-articular, with or without 6 mg hyaluronic acid, weekly | Weeks 4–7 after the first collagenase injection; assessed at 8 weeks | Cartilage morphology and histopathology scores were better in all treated groups than saline, and best with AOD9604 plus hyaluronic acid, which also gave the shortest lameness period. |
| Cox HD et al.2015 · Drug Test Anal · DOIDetection and in vitro metabolism of AOD9604. | AOD-9604 | In vitro (incubation in human serum and urine); analytical method validation | Not applicable | Not applicable | A urine extraction method detected AOD9604 down to 50 pg/mL. Six metabolites were identified, and one (CRSVEGSCG) was significantly more stable in serum than the parent peptide. |
| Heffernan M et al.2001 · Endocrinology · DOIThe effects of human GH and its lipolytic fragment (AOD9604) on lipid metabolism following chronic treatment in obese mice and beta(3)-AR knock-out mice. | AOD-9604 | Mouse, obese mice and beta3-adrenergic receptor knock-out mice | Not stated in the abstract (intraperitoneal) | 14 days chronic, plus an acute experiment | hGH and AOD9604 reduced body weight and body fat in obese mice and raised beta3-AR RNA to lean-mouse levels. In knock-out mice the chronic weight and lipolysis effects were absent, though AOD9604 still raised energy expenditure and fat oxidation acutely. |
| Ng FM et al.2000 · Horm Res · DOIMetabolic studies of a synthetic lipolytic domain (AOD9604) of human growth hormone. | AOD-9604 | Rat, obese Zucker rats | 500 µg/kg body weight, oral, daily | 19 days | Body weight gain was less than half that of controls (15.8 ± 0.6 vs 35.6 ± 0.8 g) and adipose tissue showed higher lipolytic activity. Unlike chronic intact hGH, AOD9604 had no adverse effect on insulin sensitivity by euglycaemic clamp. |
| Natera SH et al.1994 · Biochem Mol Biol IntReduction of cumulative body weight gain and adipose tissue mass in obese mice: response to chronic treatment with synthetic hGH 177-191 peptide. | AOD-9604 | Mouse, ob/ob (C57BL/6J) mice; unmodified hGH 177-191 peptide | Not stated in the abstract | Not stated in the abstract (described as long-term) | hGH 177-191 reduced cumulative body weight gain and adipose tissue mass, and significantly inhibited lipogenesis in adipose tissue. |
| Wu Z et al.1993 · Biochem Mol Biol IntAntilipogenic action of synthetic C-terminal sequence 177-191 of human growth hormone. | AOD-9604 | Rat, adipose tissue and in vitro; unmodified hGH 177-191 peptide | Not stated in the abstract | Not stated in the abstract | hGH 177-191 had antilipogenic activity identical to intact hGH, with no significant lipolytic effect measured as glycerol release from epididymal fat pads. |
| Jelińska J et al.2026 · Int J Mol Sci · DOIBPC-157 and Its Novel Hybrid Analogs as Inhibitors of Acetylcholinesterase. | BPC-157 | Enzyme assay in vitro (acetylcholinesterase, modified Ellman assay) | Not stated in the abstract | Not applicable (enzyme kinetics) | BPC-157 acted as a reversible competitive acetylcholinesterase inhibitor (Ki = 0.48 mM; IC50 = 2.80 mM), with significantly lower potency than clinically used inhibitors. |
| Lee E et al.2025 · Altern Ther Health MedSafety of Intravenous Infusion of BPC157 in Humans: A Pilot Study. | BPC-157 | Human, safety pilot (n=2 adults), private clinic | 10 mg in 250 cc normal saline over one hour on day 1, then 20 mg on day 2 (intravenous) | 3 days | The infusions produced no measurable effects on the tested heart, liver, kidney and thyroid biomarkers or blood glucose, and no side effects were reported. |
| Lee E et al.2024 · Altern Ther Health MedEffect of BPC-157 on Symptoms in Patients with Interstitial Cystitis: A Pilot Study. | BPC-157 | Human, uncontrolled pilot study (n=12 women with interstitial cystitis), private clinic | 10 mg total, given by injection around the inflamed area of the bladder during cystoscopy | Single procedure; follow-up period not stated in the abstract | Ten of 12 patients reported complete resolution of symptoms and 2 of 12 rated their success at 80% on the Global Response Assessment. No adverse events were reported. The study had no control group. |
| Lee E et al.2021 · Altern Ther Health MedIntra-Articular Injection of BPC 157 for Multiple Types of Knee Pain. | BPC-157 | Human, retrospective chart review with phone survey (n=16, knee pain) | Intra-articular BPC-157 alone (n=12) or with thymosin beta-4 (n=4); amount not stated in the abstract | Most patients surveyed 6 months to 1 year after the injection | Eleven of 12 patients given BPC-157 alone reported significant improvement in knee pain, and 14 of 16 overall reported relief. No specific tools were used to measure function or quality of life. |
| Perovic D et al.2019 · J Orthop Surg Res · DOIStable gastric pentadecapeptide BPC 157 can improve the healing course of spinal cord injury and lead to functional recovery in rats. | BPC-157 | Rat, spinal cord compression injury model | 200 or 2 μg/kg, one intraperitoneal injection 10 min after injury | Assessed at 1, 4, 7, 15, 30, 90, 180 and 360 days | All injured rats given BPC-157 showed better tail motor function, no autotomy and resolved spasticity by day 15, with less axon loss, oedema and motoneuron loss on microscopy. |
| Duzel A et al.2017 · World J Gastroenterol · DOIStable gastric pentadecapeptide BPC 157 in the treatment of colitis and ischemia and reperfusion in rats: New insights. | BPC-157 | Rat, ischaemic colitis and reperfusion model | 10 μg/kg as a bath (1 mL/rat) on the blood-deprived colon segment | 15 min vessel recording; day 10 in the colon obstruction group | BPC-157 increased vessel presentation and collateral connections, and MDA and NO levels were normal in treated rats. On day 10 the obstructed segments showed almost completely spared mucosa. |
| Zivanovic-Posilovic G et al.2016 · Eur J Pharmacol · DOIStable gastric pentadecapeptide BPC 157 and bupivacaine. | BPC-157 | Rat, bupivacaine cardiotoxicity model; HEK293 cells | 50 µg/kg, 10 µg/kg, 10 ng/kg or 10 pg/kg intraperitoneal, 30 min before or 1 min after bupivacaine; 1 µM in cells | Not stated in the abstract | BPC-157 largely counteracted bupivacaine-induced arrhythmias, AV block and asystole, and given after QRS prolongation it markedly postponed the fatal outcome. In HEK293 cells it inhibited bupivacaine-induced depolarisation. |
| Yamauchi T et al.2026 · Lancet Diabetes Endocrinol · DOIEfficacy and safety of co-administered cagrilintide and semaglutide versus semaglutide alone in adults with overweight or obesity with or without type 2 diabetes in Japan and Taiwan (REDEFINE 5): a multicentre, randomised, active-controlled, phase 3a trial. | Cagrilintide | Human, phase 3a randomised active-controlled trial (REDEFINE 5), CagriSema vs semaglutide, adults in Japan and Taiwan with or without type 2 diabetes (n=331) | Cagrilintide + semaglutide or semaglutide alone, both escalated to 2.4 mg once weekly subcutaneous | 68 weeks | Mean body weight change was −18.4% with CagriSema versus −11.9% with semaglutide alone (difference −6.5 percentage points). |
| Rosenstock J et al.2026 · Lancet · DOICagrilintide-semaglutide (CagriSema) as an add-on to basal insulin in adults with type 2 diabetes (REIMAGINE 3): a randomised, double-blind, placebo-controlled, multicentre, phase 3 study. | Cagrilintide | Human, phase 3a randomised placebo-controlled trial (REIMAGINE 3), CagriSema added to basal insulin, type 2 diabetes (n=274) | Cagrilintide 2.4 mg + semaglutide 2.4 mg, or 1.0 mg + 1.0 mg, or dose-matched placebo, once weekly subcutaneous | 40 weeks | HbA1c fell by 2.33 points (2.4 mg each) and 2.10 points (1.0 mg each) versus 0.66 points with placebo. |
| Garvey WT et al.2025 · N Engl J Med · DOICoadministered Cagrilintide and Semaglutide in Adults with Overweight or Obesity. | Cagrilintide | Human, phase 3a randomised controlled trial (REDEFINE 1), CagriSema vs each component vs placebo, adults with overweight or obesity without diabetes (n=3417) | Cagrilintide 2.4 mg + semaglutide 2.4 mg, semaglutide 2.4 mg, cagrilintide 2.4 mg, or placebo, once weekly | 68 weeks | Mean body weight change was −20.4% with CagriSema versus −3.0% with placebo (difference −17.3 percentage points). The abstract does not report the result for the cagrilintide-alone arm. |
| Davies MJ et al.2025 · N Engl J Med · DOICagrilintide-Semaglutide in Adults with Overweight or Obesity and Type 2 Diabetes. | Cagrilintide | Human, phase 3a randomised placebo-controlled trial (REDEFINE 2), CagriSema, adults with overweight or obesity and type 2 diabetes (n=1206) | Cagrilintide 2.4 mg + semaglutide 2.4 mg or placebo, once weekly | 68 weeks | Mean body weight change was −13.7% with CagriSema versus −3.4% with placebo. HbA1c of 6.5% or less was reached by 73.5% versus 15.9%. |
| Gabe MBN et al.2024 · Diabetes Obes Metab · DOICagrilintide is not associated with clinically relevant QTc prolongation: A thorough QT study in healthy participants. | Cagrilintide | Human, randomised double-blind thorough QT study, cagrilintide alone, healthy participants (n=105) | Cagrilintide once weekly subcutaneous, escalated to 4.5 mg; placebo arms received moxifloxacin 400 mg as a positive control | Not stated in the abstract | No clinically relevant QTcF prolongation occurred after the last 4.5 mg dose; the upper limits of the 90% confidence intervals of the placebo-adjusted changes were below 10 ms at all time points. |
| Frias JP et al.2023 · Lancet · DOIEfficacy and safety of co-administered once-weekly cagrilintide 2·4 mg with once-weekly semaglutide 2·4 mg in type 2 diabetes: a multicentre, randomised, double-blind, active-controlled, phase 2 trial. | Cagrilintide | Human, phase 2 randomised double-blind trial, CagriSema vs semaglutide vs cagrilintide, type 2 diabetes on metformin (n=92) | CagriSema, semaglutide or cagrilintide, each escalated to 2.4 mg once weekly subcutaneous | 32 weeks | HbA1c fell by 2.2 points with CagriSema, 1.8 with semaglutide and 0.9 with cagrilintide alone. Body weight fell by 15.6%, 5.1% and 8.1% respectively; CagriSema beat both single agents on weight. |
| Lau DCW et al.2021 · Lancet · DOIOnce-weekly cagrilintide for weight management in people with overweight and obesity: a multicentre, randomised, double-blind, placebo-controlled and active-controlled, dose-finding phase 2 trial. | Cagrilintide | Human, phase 2 randomised controlled trial, cagrilintide alone, adults with overweight or obesity without diabetes (n=906 randomised: 706 cagrilintide, 99 liraglutide, 101 placebo) | Cagrilintide 0.3, 0.6, 1.2, 2.4 or 4.5 mg once weekly, subcutaneous; comparator liraglutide 3.0 mg once daily | 26 weeks treatment (including up to 6 weeks escalation), plus 6 weeks follow-up | Mean weight reduction was 6.0%–10.8% across the cagrilintide doses versus 3.0% with placebo (trial product estimand). Cagrilintide 4.5 mg reduced weight by 10.8% compared with 9.0% for liraglutide 3.0 mg. |
| Enebo LB et al.2021 · Lancet · DOISafety, tolerability, pharmacokinetics, and pharmacodynamics of concomitant administration of multiple doses of cagrilintide with semaglutide 2·4 mg for weight management: a randomised, controlled, phase 1b trial. | Cagrilintide | Human, phase 1b randomised placebo-controlled trial, cagrilintide + semaglutide 2.4 mg, otherwise healthy adults with BMI 27.0–39.9 (n=96 randomised, 95 exposed) | Cagrilintide 0.16, 0.30, 0.60, 1.2, 2.4 or 4.5 mg or placebo, each with semaglutide 2.4 mg, once weekly subcutaneous | Co-escalation over 16 weeks, 4 weeks at target dose, then 5 weeks follow-up | The primary endpoint was the number of treatment-emergent adverse events; 566 adverse events were reported in 92 participants. Pharmacokinetics, body weight, glycaemic measures and hormones were secondary or exploratory endpoints. |
| Teichman SL et al.2006 · J Clin Endocrinol Metab · DOIProlonged stimulation of growth hormone (GH) and insulin-like growth factor I secretion by CJC-1295, a long-acting analog of GH-releasing hormone, in healthy adults. | CJC-1295 (no DAC) | Human, two randomised, placebo-controlled, double-blind ascending-dose trials in healthy adults aged 21-61 (n not stated in the abstract). Tested CJC-1295 WITH DAC, not the no-DAC compound | Four ascending single s.c. doses, then two or three weekly or fortnightly doses; the abstract names 30 and 60 micrograms/kg as the better-tolerated doses | 28 and 49 days | A single injection raised mean GH 2- to 10-fold for 6 days or more and IGF-I 1.5- to 3-fold for 9-11 days. The half-life was 5.8-8.1 days, a result of the DAC and not expected for the no-DAC compound. |
| Ionescu M et al.2006 · J Clin Endocrinol Metab · DOIPulsatile secretion of growth hormone (GH) persists during continuous stimulation by CJC-1295, a long-acting GH-releasing hormone analog. | CJC-1295 (no DAC) | Human, healthy men aged 20-40 (n not stated in the abstract). Tested CJC-1295 WITH DAC | 60 or 90 micrograms/kg, single injection | Sampling before and 1 week after injection | GH secretion rose while pulse frequency and size were unchanged. Trough GH rose 7.5-fold, mean GH 46% and IGF-I 45%, with no difference between the two doses. |
| Jetté L et al.2005 · Endocrinology · DOIHuman growth hormone-releasing factor (hGRF)1-29-albumin bioconjugates activate the GRF receptor on the anterior pituitary in rats: identification of CJC-1295 as a long-lasting GRF analog. | CJC-1295 (no DAC) | Rat (Sprague Dawley) and cultured rat anterior pituitary cells. Tested CJC-1295 WITH DAC, compared against native hGRF(1-29) | Not stated in the abstract (s.c.) | Plasma followed beyond 72 h | CJC-1295 is described as a tetrasubstituted hGRF(1-29) with an added maleimido lysine at the C-terminus. It gave a 4-fold larger growth hormone area under the curve over 2 h than hGRF(1-29) and bound to serum albumin within 15 min. This is the paper that defines the difference between the two molecules. |
| Cervini LA et al.1998 · J Med Chem · DOIHuman growth hormone-releasing hormone hGHRH(1-29)-NH2: systematic structure-activity relationship studies. | CJC-1295 (no DAC) | In vitro structure-activity study of hGRF(1-29)-NH2 analogues (growth hormone release) | Not stated in the abstract | Not applicable (in vitro) | Single alanine swaps at positions 8, 9, 15, 22 and 28 gave analogues 2-6 times more potent than hGRF(1-40)-OH. Multiple-substituted analogues released growth hormone 11 to 26 times more effectively than the standard. This is the design family Mod GRF 1-29 belongs to; the no-DAC compound itself was not tested. |
| Gaudreau P et al.1992 · J Med Chem · DOIAffinity of human growth hormone-releasing factor (1-29)NH2 analogues for GRF binding sites in rat adenopituitary. | CJC-1295 (no DAC) | Rat anterior pituitary membranes, receptor binding assay of hGRF(1-29)NH2 analogues | Not stated in the abstract | Not applicable (binding assay) | Residues in segment 13-21 mattered more for receptor affinity than those in 24-29. Acylating the N-terminus reduced affinity (26-85% of hGRF(1-29)NH2), and replacing the C-terminal amide with a free acid reduced it to 57%. |
| Rafferty B et al.1985 · J Endocrinol · DOIGrowth hormone-releasing factor analogue (hGRF1-29NH2): immunoreactive-GRF plasma levels after intravenous and subcutaneous administration. | CJC-1295 (no DAC) | Rat (anaesthetised), pharmacokinetic study of native hGRF(1-29)NH2, the unmodified parent peptide | 10 micrograms i.v.; s.c. dose not stated in the abstract | Single dose | After i.v. injection the peptide cleared with half-lives of 1.9 min (distribution) and 10.4 min (elimination). After s.c. injection the amount reaching the circulation was only 4% of the i.v. amount, which the authors put down to rapid breakdown. |
| Beck DE et al.2014 · Int J Colorectal Dis · DOIProspective, randomized, controlled, proof-of-concept study of the Ghrelin mimetic ipamorelin for the management of postoperative ileus in bowel resection patients. | CJC-1295 + Ipamorelin | Human, phase 2 randomised, double-blind, placebo-controlled trial (n=114 analysed, bowel resection patients) | 0.03 mg/kg intravenous infusion, twice daily | Postoperative day 1 to 7 or hospital discharge | Treatment-emergent adverse events occurred in 87.5% on ipamorelin and 94.8% on placebo. Median time to first tolerated meal was 25.3 vs 32.6 hours (p = 0.15), and no efficacy analysis differed significantly from placebo. |
| Teichman SL et al.2006 · J Clin Endocrinol Metab · DOIProlonged stimulation of growth hormone (GH) and insulin-like growth factor I secretion by CJC-1295, a long-acting analog of GH-releasing hormone, in healthy adults. | CJC-1295 + Ipamorelin | DAC STUDY. Human, two randomised, placebo-controlled, double-blind ascending-dose trials in healthy adults aged 21-61 (n not stated in the abstract). Tested CJC-1295 WITH DAC | Four ascending single s.c. doses, then two or three weekly or fortnightly doses; 30 and 60 micrograms/kg named as better tolerated | 28 and 49 days | A single injection raised mean GH 2- to 10-fold for 6 days or more and IGF-I 1.5- to 3-fold for 9-11 days, with a half-life of 5.8-8.1 days. That duration comes from the DAC and is not expected for the no-DAC compound in this blend. |
| Ionescu M et al.2006 · J Clin Endocrinol Metab · DOIPulsatile secretion of growth hormone (GH) persists during continuous stimulation by CJC-1295, a long-acting GH-releasing hormone analog. | CJC-1295 + Ipamorelin | DAC STUDY. Human, healthy men aged 20-40 (n not stated in the abstract). Tested CJC-1295 WITH DAC | 60 or 90 micrograms/kg, single injection | Sampling before and 1 week after injection | Growth hormone secretion rose while pulse frequency and size were unchanged. Trough GH rose 7.5-fold, mean GH 46% and IGF-I 45%, with no difference between the two doses. |
| Gobburu JV et al.1999 · Pharm Res · DOIPharmacokinetic-pharmacodynamic modeling of ipamorelin, a growth hormone releasing peptide, in human volunteers. | CJC-1295 + Ipamorelin | Human, randomised dose-escalation PK/PD trial (healthy men, 8 per dose level, 5 dose levels) | 4.21, 14.02, 42.13, 84.27 or 140.45 nmol/kg infused over 15 minutes | Single infusion | Ipamorelin had a terminal half-life of 2 hours and dose-proportional pharmacokinetics. Each dose produced a single episode of growth hormone release peaking at 0.67 hours, then an exponential decline to negligible levels. |
| Johansen PB et al.1999 · Growth Horm IGF Res · DOIIpamorelin, a new growth-hormone-releasing peptide, induces longitudinal bone growth in rats. | CJC-1295 + Ipamorelin | Rat, adult females | 0, 18, 90 or 450 micrograms/day s.c., given three times daily | 15 days | Longitudinal bone growth rose dose-dependently from 42 to 44, 50 and 52 micrometres/day, with a dose-dependent gain in body weight. Total IGF-I, IGFBPs and bone turnover markers did not change. |
| Raun K et al.1998 · Eur J Endocrinol · DOIIpamorelin, the first selective growth hormone secretagogue. | CJC-1295 + Ipamorelin | Rat pituitary cells in vitro; anaesthetised rats; conscious swine | ED50 for GH release 80 nmol/kg in rats and 2.3 nmol/kg in swine; specificity tested at more than 200-fold the ED50 | Single doses | Ipamorelin released growth hormone with potency and efficacy similar to GHRP-6. Unlike GHRP-6 and GHRP-2, it did not raise ACTH or cortisol, and it did not affect FSH, LH, prolactin or TSH in swine. |
| Cervini LA et al.1998 · J Med Chem · DOIHuman growth hormone-releasing hormone hGHRH(1-29)-NH2: systematic structure-activity relationship studies. | CJC-1295 + Ipamorelin | In vitro structure-activity study of hGRF(1-29)-NH2 analogues (growth hormone release) | Not stated in the abstract | Not applicable (in vitro) | Single alanine swaps at positions 8, 9, 15, 22 and 28 gave analogues 2-6 times more potent than hGRF(1-40)-OH, and multiple-substituted analogues were 11 to 26 times more effective. This is the design family Mod GRF 1-29 belongs to; the no-DAC compound itself was not tested. |
| Rafferty B et al.1985 · J Endocrinol · DOIGrowth hormone-releasing factor analogue (hGRF1-29NH2): immunoreactive-GRF plasma levels after intravenous and subcutaneous administration. | CJC-1295 + Ipamorelin | Rat (anaesthetised), pharmacokinetic study of native hGRF(1-29)NH2, the unmodified parent of CJC-1295 without DAC | 10 micrograms i.v.; s.c. dose not stated in the abstract | Single dose | After i.v. injection the peptide cleared with half-lives of 1.9 min (distribution) and 10.4 min (elimination). After s.c. injection the amount reaching the circulation was only 4% of the i.v. amount. |
| Timms M et al.2019 · Drug Test Anal · DOIAn immuno polymerase chain reaction screen for the detection of CJC-1295 and other growth-hormone-releasing hormone analogs in equine plasma. | CJC-1295 with DAC | Horse (thoroughbred), assay development and validation | Not stated in the abstract | Not stated in the abstract | An immuno-PCR assay detected the CJC-1295-protein conjugate down to 0.8 pg/mL, with a 50 pg/mL screening threshold in equine plasma. Albumin binding hides the peptide from standard mass-spectrometry peptide screens. |
| Sackmann-Sala L et al.2009 · Growth Horm IGF Res · DOIActivation of the GH/IGF-1 axis by CJC-1295, a long-acting GHRH analog, results in serum protein profile changes in normal adult subjects. | CJC-1295 with DAC | Human, healthy young men (n=11), serum proteomics | Not stated in the abstract | Sera before and 1 week after injection | Two protein spots fell (an apolipoprotein A1 isoform and a transthyretin isoform) and three rose, including beta-haemoglobin and albumin fragments. One spot varied linearly with IGF-1, and the authors propose these as possible biomarkers of GH or IGF-1 action. |
| Teichman SL et al.2006 · J Clin Endocrinol Metab · DOIProlonged stimulation of growth hormone (GH) and insulin-like growth factor I secretion by CJC-1295, a long-acting analog of GH-releasing hormone, in healthy adults. | CJC-1295 with DAC | Human, two randomised, placebo-controlled, double-blind ascending-dose trials in healthy adults aged 21-61 (n not stated in the abstract) | Four ascending single s.c. doses, then two or three weekly or fortnightly doses; 30 and 60 micrograms/kg named as better tolerated | 28 and 49 days | One injection raised mean GH 2- to 10-fold for 6 days or more and IGF-I 1.5- to 3-fold for 9-11 days, with a half-life of 5.8-8.1 days. After multiple doses IGF-I stayed above baseline for up to 28 days, and no serious adverse reactions were reported. |
| Ionescu M et al.2006 · J Clin Endocrinol Metab · DOIPulsatile secretion of growth hormone (GH) persists during continuous stimulation by CJC-1295, a long-acting GH-releasing hormone analog. | CJC-1295 with DAC | Human, healthy men aged 20-40 (n not stated in the abstract) | 60 or 90 micrograms/kg, single injection | Overnight sampling before and 1 week after injection | GH secretion rose while pulse frequency and size were unchanged. Trough GH rose 7.5-fold, mean GH 46% and IGF-I 45%, with no difference between the two doses. |
| Alba M et al.2006 · Am J Physiol Endocrinol Metab · DOIOnce-daily administration of CJC-1295, a long-acting growth hormone-releasing hormone (GHRH) analog, normalizes growth in the GHRH knockout mouse. | CJC-1295 with DAC | Mouse, GHRH knockout (from 1 week of age) | 2 micrograms | 5 weeks, every 24, 48 or 72 h | Daily dosing gave normal body weight and length. Dosing every 48 or 72 h improved growth over placebo without normalising it, and treatment raised pituitary RNA and GH mRNA, with signs of somatotroph proliferation. |
| Jetté L et al.2005 · Endocrinology · DOIHuman growth hormone-releasing factor (hGRF)1-29-albumin bioconjugates activate the GRF receptor on the anterior pituitary in rats: identification of CJC-1295 as a long-lasting GRF analog. | CJC-1295 with DAC | Rat (Sprague Dawley) and cultured rat anterior pituitary cells | Not stated in the abstract (s.c.) | Plasma followed beyond 72 h | Albumin conjugates resisted DPP-IV breakdown and stayed active on pituitary cells. CJC-1295 gave a 4-fold larger GH area under the curve over 2 h than hGRF(1-29), bound to albumin within 15 min and was still in plasma beyond 72 h. |
| Pomfrett CJ et al.2009 · Eur J Anaesthesiol · DOIDelta sleep-inducing peptide alters bispectral index, the electroencephalogram and heart rate variability when used as an adjunct to isoflurane anaesthesia. | DSIP | Human, randomised controlled trial in women under isoflurane anaesthesia (n=24; 12 DSIP, 12 saline) | Intravenous bolus of 25, 50 or 100 nmol/kg | Two doses: awake and after induction of anaesthesia | DSIP raised heart rate, lowered heart rate variability and, against the authors' hypothesis, reduced EEG delta rhythm and raised bispectral index at 25 nmol/kg, suggesting lighter anaesthesia. |
| Späth-Schwalbe E et al.1995 · Psychoneuroendocrinology · DOIDelta-sleep-inducing peptide does not affect CRH and meal-induced ACTH and cortisol secretion. | DSIP | Human, placebo-controlled studies in healthy young men (n=5 per CRH condition; n=10 meal study) | Total 3 or 4 mg intravenous infusion | From 30 minutes before to 90 minutes after CRH injection; single session | ACTH and cortisol responses to CRH and to a midday meal were almost identical with DSIP and placebo. The authors say the data do not support an inhibitory role of DSIP on ACTH and cortisol in man. |
| Chiodera P et al.1994 · Horm Res · DOIDifferent effects of delta-sleep-inducing peptide on arginine-vasopressin and ACTH secretion in normal men. | DSIP | Human, placebo-controlled trial in healthy men (n=8, plus 7 in a second arm) | 25 nmol/kg intravenous over 10 minutes | Single infusion before 2-hour saline or hypertonic saline, or an orthostatic test | DSIP significantly lowered ACTH but did not change basal vasopressin or the vasopressin rise after hypertonic saline or standing. |
| Giusti M et al.1993 · Psychoneuroendocrinology · DOIDelta sleep-inducing peptide administration does not influence growth hormone and prolactin secretion in normal women. | DSIP | Human, controlled study in healthy women (n=8) | 25 micrograms/kg intravenous over 30 minutes (or 1 hour in the circadian arm) | Single infusions | DSIP did not change basal growth hormone or prolactin, their circadian rhythm, or their response to arginine. |
| Bes F et al.1992 · Neuropsychobiology · DOIEffects of delta sleep-inducing peptide on sleep of chronic insomniac patients. A double-blind study. | DSIP | Human, double-blind randomised matched-pairs trial in chronic insomnia (n=16) | 25 nmol/kg intravenous DSIP or glucose placebo | Given the afternoon before nights 3, 4 and 5 of a 5-night laboratory stay | Sleep efficiency was higher and sleep latency shorter with DSIP, but the effects were weak and partly explained by a change in the placebo group. Subjective sleep quality did not change, and the authors concluded short-term DSIP is unlikely to be of major therapeutic benefit. |
| Monti JM et al.1987 · Int J Clin Pharmacol ResStudy of delta sleep-inducing peptide efficacy in improving sleep on short-term administration to chronic insomniacs. | DSIP | Human, double-blind crossover trial in chronic insomnia (n not stated in the abstract) | 25 nmol/kg intravenous or placebo | 4 nights | Total sleep time and NREM time rose, driven by stage 2 sleep, while slow-wave and REM sleep did not change. Differences from placebo already existed at baseline, and the authors judged the improvement of little clinical significance. |
| Schneider-Helmert D1987 · Eur Neurol · DOIEffects of delta-sleep-inducing peptide on 24-hour sleep-wake behaviour in severe chronic insomnia. | DSIP | Human, placebo-controlled double-blind trial in severe chronic insomnia (n=14) | Not stated in the abstract | 7 successive nights, plus a placebo night afterwards | Night sleep improved with the first dose and further with repeated doses, and the effect held on the first placebo night. Daytime alertness and performance increased significantly. |
| Schneider-Helmert D et al.1981 · Int J Clin Pharmacol Ther ToxicolAcute and delayed effects of DSIP (delta sleep-inducing peptide) on human sleep behavior. | DSIP | Human, double-blind crossover in healthy volunteers (n=6) | 25 nmol/kg slow intravenous infusion, in the morning | Single infusion, sleep followed into the next night | Median total sleep time rose 59% within 130 minutes compared with placebo, without classic sedation on EEG and behavioural tests. The next night showed shorter sleep onset and better sleep efficiency, and no side effects were observed. |
| Al-Dulaimi S et al.2025 · Biogerontology · DOIEpitalon increases telomere length in human cell lines through telomerase upregulation or ALT activity. | Epitalon | Cell culture (human breast cancer lines 21NT and BT474, normal epithelial cells and fibroblasts) | Not stated in the abstract (dose-dependent effect reported) | Not stated in the abstract | Telomere length increased with dose in normal cells through hTERT and telomerase upregulation. In the cancer cell lines, telomeres also lengthened, through ALT activation rather than telomerase. |
| Gatta M et al.2025 · Stem Cell Rev Rep · DOIThe Antioxidant Tetrapeptide Epitalon Enhances Delayed Wound Healing in an in Vitro Model of Diabetic Retinopathy. | Epitalon | Cell culture (human retinal pigment epithelial cells, ARPE-19, injured by high glucose) | Not stated in the abstract | Not stated in the abstract | Epitalon restored delayed wound closure in high-glucose-injured cells by inhibiting epithelial-mesenchymal transition and fibrosis-related changes. The authors say more work is needed to confirm benefits and safety. |
| Yue X et al.2022 · Aging (Albany NY) · DOIEpitalon protects against post-ovulatory aging-related damage of mouse oocytes in vitro. | Epitalon | Mouse oocytes, in vitro post-ovulatory ageing model | 0.1 mM in culture medium | 6, 12 and 24 hours of culture | Epitalon reduced reactive oxygen species, lowered spindle defects and abnormal cortical granule distribution at 12 and 24 hours, raised mitochondrial membrane potential and reduced oocyte apoptosis by 24 hours. |
| Ivko OM et al.2020 · Adv Gerontol[AEDG peptide regulates human circadian rhythms genes expression during pineal gland accelerated aging.]. | Epitalon | Human, middle-aged people with reduced pineal melatonin function; design and n not stated in the abstract | Not stated in the abstract | Not stated in the abstract | AEDG increased urinary 6-sulfatoxymelatonin excretion 1.7-fold, normalised raised Clock and Csnk1e gene expression in leukocytes (1.9–2.1-fold) and doubled low Cry2 expression in lymphocytes. |
| Vinogradova IA2009 · Adv Gerontol[Effect of preparations melatonin and epitalon on the age-related dynamics of thyrotrophic activity of the hypophysis and thyroid gland function in different light regimes]. | Epitalon | Rat, ageing study under different light regimes | Not stated in the abstract | Not stated in the abstract | Age-related changes in thyroid-related hormones appeared later in rats given melatonin or epitalon than in controls, and both smoothed seasonal variation in thyroid hormone levels under the natural light regime of north-west Russia. |
| Khavinson VKh et al.2003 · Bull Exp Biol Med · DOIRetinoprotective effect of Epithalon in campbell rats of various ages. | Epitalon | Rat, Campbell rats with inherited retinal degeneration | Not stated in the abstract | Given to offspring after birth, and to mothers before mating and during pregnancy | Retinal structure and function were preserved about twice as long as in control rats, and 30% longer than in rats given the peptide only after birth. |
| Khavinson VKh et al.2003 · Bull Exp Biol Med · DOIEpithalon peptide induces telomerase activity and telomere elongation in human somatic cells. | Epitalon | Cell culture (telomerase-negative human fetal fibroblasts) | Not stated in the abstract | Not stated in the abstract | Adding epitalon induced expression of the catalytic subunit of telomerase, telomerase activity and telomere elongation. |
| Khavinson V et al.2002 · Neuro Endocrinol LettPineal-regulating tetrapeptide epitalon improves eye retina condition in retinitis pigmentosa. | Epitalon | Human, controlled clinical trial in patients with degenerative retinal lesions, with a Campbell rat model of inherited retinal degeneration; n not stated in the abstract | Not stated in the abstract | Not stated in the abstract | In rats, epitalon was associated with greater bioelectric and functional activity of the retina and preserved retinal structure. In patients, the authors report a positive clinical effect in 90% of cases. |
| Bian Y et al.2024 · Redox Biol · DOIThe glycyl-l-histidyl-l-lysine-Cu2+ tripeptide complex attenuates lung inflammation and fibrosis in silicosis by targeting peroxiredoxin 6. | GHK-Cu | Mouse, crystalline silica (silicosis) model; RAW264.7 macrophage cells | Not stated in the abstract | Not stated in the abstract | GHK-Cu bound peroxiredoxin 6 and reduced lung inflammation and fibrosis in silicosis mice without significant systemic toxicity, partly by limiting oxidative stress in alveolar macrophages. |
| Deng M et al.2023 · J Cachexia Sarcopenia Muscle · DOIGlycyl-l-histidyl-l-lysine-Cu2+ rescues cigarette smoking-induced skeletal muscle dysfunction via a sirtuin 1-dependent pathway. | GHK-Cu | Mouse (C57BL/6), cigarette-smoke muscle dysfunction model; C2C12 muscle cells; plasma GHK measured in people with COPD (n=9) and healthy controls (n=11) | 0.2 and 2 mg/kg (route not stated in the abstract) | Not stated in the abstract | GHK-Cu reduced smoke-induced loss of muscle mass and improved grip strength (175.5 g untreated vs 257.6 g and 339.1 g). Plasma GHK was lower in the COPD group than in controls (70.27 vs 133.0 ng/mL). |
| Zhang Q et al.2023 · Biomed Pharmacother · DOIRelief of ovalbumin-induced airway remodeling by the glycyl-l-histidyl-l-lysine-Cu2+ tripeptide complex via activation of SIRT1 in airway epithelial cells. | GHK-Cu | Mouse, ovalbumin-induced asthma model; airway epithelial cells; plasma GHK measured in asthma patients | Not stated in the abstract | Not stated in the abstract | GHK-Cu reduced peribronchial collagen deposition, airway mucus secretion and epithelial-mesenchymal transition, linked to lower TGF-β1 through SIRT1. Plasma GHK was lower in asthma patients than in age-matched controls. |
| Synytsya A et al.2020 · Int J Biol Macromol · DOIHydrogels based on low-methoxyl amidated citrus pectin and flaxseed gum formulated with tripeptide glycyl-l-histidyl-l-lysine improve the healing of experimental cutting wounds in rats. | GHK-Cu | Rat, experimental cutting wound model (tripeptide GHK in hydrogels; copper not stated in the abstract) | Not stated in the abstract | Not stated in the abstract | GHK in pectin or flaxseed gum hydrogels gave a significantly higher healing degree and shorter healing time than untreated controls or GHK in aqueous solution. Complete histological healing was seen only with the flaxseed gum hydrogel. |
| Wang X et al.2017 · Wound Repair Regen · DOIGHK-Cu-liposomes accelerate scald wound healing in mice by promoting cell proliferation and angiogenesis. | GHK-Cu | Mouse, scald burn model; human umbilical vein endothelial cells (HUVECs) | GHK-Cu in liposomes; amount not stated in the abstract | Wound healing time 14 days post injury in the liposome group | GHK-Cu liposomes raised HUVEC proliferation by 33.1% and gave better angiogenesis in burned skin than free GHK-Cu, with wound healing time shortened to 14 days. |
| Li H et al.2015 · Pharm Res · DOIMicroneedle-Mediated Delivery of Copper Peptide Through Skin. | GHK-Cu | Human skin in vitro, cell culture and pig (porcine) model; microneedle delivery | Not stated in the abstract | 9 hours (skin permeation test) | After microneedle pre-treatment, 134 ± 12 nanomoles of peptide and 705 ± 84 nanomoles of copper passed through human skin in 9 h, against almost none through intact skin. No obvious signs of skin irritation were observed. |
| Miller TR et al.2006 · Arch Facial Plast Surg · DOIEffects of topical copper tripeptide complex on CO2 laser-resurfaced skin. | GHK-Cu | Human, randomised controlled trial (n=13 completed), skin after CO2 laser resurfacing | Topical skin care products with or without GHK-Cu; concentration not stated in the abstract | 12 weeks | Computer analysis and blinded evaluators found no significant difference between groups in erythema, wrinkles or overall skin quality. On the patient questionnaire, rated improvement in overall skin quality was higher in the GHK-Cu group (P = .04). |
| Pollard JD et al.2005 · Arch Facial Plast Surg · DOIEffects of copper tripeptide on the growth and expression of growth factors by normal and irradiated fibroblasts. | GHK-Cu | Cell culture (normal and irradiated human dermal fibroblasts) | 1 × 10⁻⁹ mol/L | Not stated in the abstract | GHK-Cu shortened the population-doubling time of normal and irradiated fibroblasts. Treated irradiated fibroblasts produced significantly more basic FGF and VEGF than untreated controls early after exposure. |
| Maar K et al.2025 · Int J Mol Sci · DOIThymosin Beta-4 Modulates Cardiac Remodeling by Regulating ROCK1 Expression in Adult Mammals. | GLOW blend | Mouse, permanent coronary ligation (heart attack) model; human cardiac cells | Systemic TB4 injection; amount not stated in the abstract | Not stated in the abstract | TB4 raised miR139-5p expression and modulated ROCK1 protein levels in mouse hearts and human cardiac cells, and may reverse or inhibit fibroblast-to-myofibroblast transformation. |
| Lee E et al.2024 · Altern Ther Health MedEffect of BPC-157 on Symptoms in Patients with Interstitial Cystitis: A Pilot Study. | GLOW blend | Human, uncontrolled pilot study (n=12 women with interstitial cystitis), private clinic | 10 mg total, given by injection around the inflamed area of the bladder during cystoscopy | Single procedure; follow-up period not stated in the abstract | Ten of 12 patients reported complete resolution of symptoms and 2 of 12 rated their success at 80%. No adverse events were reported. The study had no control group. |
| Deng M et al.2023 · J Cachexia Sarcopenia Muscle · DOIGlycyl-l-histidyl-l-lysine-Cu2+ rescues cigarette smoking-induced skeletal muscle dysfunction via a sirtuin 1-dependent pathway. | GLOW blend | Mouse (C57BL/6), cigarette-smoke muscle dysfunction model; C2C12 muscle cells; plasma GHK measured in people with COPD (n=9) and healthy controls (n=11) | 0.2 and 2 mg/kg (route not stated in the abstract) | Not stated in the abstract | GHK-Cu reduced smoke-induced loss of muscle mass and improved grip strength (175.5 g untreated vs 257.6 g and 339.1 g). Plasma GHK was lower in the COPD group than in controls. |
| Bako P et al.2023 · Int Immunopharmacol · DOIThymosin beta-4 - A potential tool in healing middle ear lesions in adult mammals. | GLOW blend | Mouse tympanic membrane (eardrum) explants, ex vivo and on collagen gels | Not stated in the abstract | Not stated in the abstract | TB4 affected the migration and proliferation of epidermal and epithelial cells of the tympanic membrane in vitro, most likely acting on local epidermal progenitor cells. |
| Wang X et al.2017 · Wound Repair Regen · DOIGHK-Cu-liposomes accelerate scald wound healing in mice by promoting cell proliferation and angiogenesis. | GLOW blend | Mouse, scald burn model; human umbilical vein endothelial cells (HUVECs) | GHK-Cu in liposomes; amount not stated in the abstract | Wound healing time 14 days post injury in the liposome group | GHK-Cu liposomes raised HUVEC proliferation by 33.1% and gave better angiogenesis in burned skin than free GHK-Cu, with wound healing time shortened to 14 days. |
| Duzel A et al.2017 · World J Gastroenterol · DOIStable gastric pentadecapeptide BPC 157 in the treatment of colitis and ischemia and reperfusion in rats: New insights. | GLOW blend | Rat, ischaemic colitis and reperfusion model | 10 μg/kg as a bath (1 mL/rat) on the blood-deprived colon segment | 15 min vessel recording; day 10 in the colon obstruction group | BPC-157 increased vessel presentation and collateral connections, and MDA and NO levels were normal in treated rats. On day 10 the obstructed segments showed almost completely spared mucosa. |
| Miller TR et al.2006 · Arch Facial Plast Surg · DOIEffects of topical copper tripeptide complex on CO2 laser-resurfaced skin. | GLOW blend | Human, randomised controlled trial (n=13 completed), skin after CO2 laser resurfacing | Topical skin care products with or without GHK-Cu; concentration not stated in the abstract | 12 weeks | Computer analysis and blinded evaluators found no significant difference between groups in erythema, wrinkles or overall skin quality. On the patient questionnaire, rated improvement in overall skin quality was higher in the GHK-Cu group (P = .04). |
| Pollard JD et al.2005 · Arch Facial Plast Surg · DOIEffects of copper tripeptide on the growth and expression of growth factors by normal and irradiated fibroblasts. | GLOW blend | Cell culture (normal and irradiated human dermal fibroblasts) | 1 × 10⁻⁹ mol/L | Not stated in the abstract | GHK-Cu shortened the population-doubling time of normal and irradiated fibroblasts. Treated irradiated fibroblasts produced significantly more basic FGF and VEGF than untreated controls early after exposure. |
| Mawu FO et al.2025 · Acta Dermatovenerol Alp Pannonica AdriatEffectiveness of oral glutathione in reducing nitric oxide and IL-1α concentrations for clinical improvement in mild to moderate acne vulgaris: a randomized controlled trial. | Glutathione | Human, randomised controlled trial (n=40), mild to moderate acne vulgaris | 500 mg once daily, oral | 4 weeks | Serum nitric oxide and IL-1α fell in the glutathione group but not significantly (p > 0.05). Seven of 22 subjects (31.8%) improved from moderate to mild severity, and no adverse reactions were reported. |
| Duperray J et al.2022 · J Cosmet Dermatol · DOIThe effects of the oral supplementation of L-Cystine associated with reduced L-Glutathione-GSH on human skin pigmentation: a randomized, double-blinded, benchmark- and placebo-controlled clinical trial. | Glutathione | Human, randomised double-blind placebo- and benchmark-controlled trial (n=124 Asian women) | Oral, daily: 500 mg L-cystine + 250 mg L-glutathione, 250 mg L-glutathione alone, 500 mg L-cystine alone, or placebo | 12 weeks | The cystine plus glutathione combination significantly lightened skin by spectrophotometry and reduced facial dark-spot size at 6 and 12 weeks. Its effect was significantly better than placebo and than either ingredient alone. |
| Søndergård SD et al.2021 · Appl Physiol Nutr Metab · DOIThe effects of 3 weeks of oral glutathione supplementation on whole body insulin sensitivity in obese males with and without type 2 diabetes: a randomized trial. | Glutathione | Human, randomised double-blind placebo-controlled trial (n=20 obese males, 10 with type 2 diabetes) | 1,000 mg/day, oral | 3 weeks | Whole-body insulin sensitivity by hyperinsulinaemic-euglycaemic clamp increased significantly with GSH. Muscle GSH rose about 19% (numerically only), and mitochondrial H2O2 emission and urinary oxidation markers did not change. |
| Bozic M et al.2020 · J Pediatr Gastroenterol Nutr · DOIOral Glutathione and Growth in Cystic Fibrosis: A Multicenter, Randomized, Placebo-controlled, Double-blind Trial. | Glutathione | Human, multicentre randomised double-blind placebo-controlled phase II trial (n=58 completed), children aged 2–10 with cystic fibrosis | Not stated in the abstract (reduced glutathione, oral, daily) | 24 weeks | No significant difference from placebo in weight-for-age z-score, weight, BMI or serum and faecal inflammatory markers. Glutathione was reported as safe and well tolerated. |
| Tanzilli G et al.2019 · BMJ Open · DOIGlutathione infusion before primary percutaneous coronary intervention: a randomised controlled pilot study. | Glutathione | Human, randomised controlled pilot trial (n=50), STEMI patients undergoing primary angioplasty | 2,500 mg in 25 mL by intravenous infusion over 10 minutes before the procedure, repeated at 24, 48 and 72 hours | 4 infusions over 72 hours; blood sampled up to 5 days | After reperfusion the GSH group had lower H2O2 production and 8-iso-PGF2α and higher H2O2 breakdown activity and nitric oxide bioavailability than placebo. Lower H2O2 production persisted to day 5 and tracked troponin T levels. |
| Richie JP et al.2015 · Eur J Nutr · DOIRandomized controlled trial of oral glutathione supplementation on body stores of glutathione. | Glutathione | Human, randomised double-blind placebo-controlled trial (n=54 healthy non-smoking adults) | 250 or 1,000 mg/day, oral | 6 months, then a 1-month washout | At 6 months the high dose raised GSH by 30–35% in erythrocytes, plasma and lymphocytes and by 260% in buccal cells; the low dose raised blood and erythrocyte GSH by 17% and 29%. Levels returned to baseline after washout, and natural killer cytotoxicity more than doubled at 3 months on the high dose. |
| Cascinu S et al.2002 · J Clin Oncol · DOINeuroprotective effect of reduced glutathione on oxaliplatin-based chemotherapy in advanced colorectal cancer: a randomized, double-blind, placebo-controlled trial. | Glutathione | Human, randomised double-blind placebo-controlled trial (n=52), advanced colorectal cancer on oxaliplatin | 1,500 mg/m² by intravenous infusion over 15 minutes before each oxaliplatin dose | Bimonthly oxaliplatin regimen, assessed after 4, 8 and 12 cycles | Grade 2–4 neuropathy occurred in 2 patients on GSH vs 11 on placebo (P = .003), and after 12 cycles in 3 vs 8 (P = .004). Tumour response was 26.9% vs 23.1%, so GSH did not reduce oxaliplatin activity. |
| Beck DE et al.2014 · Int J Colorectal Dis · DOIProspective, randomized, controlled, proof-of-concept study of the Ghrelin mimetic ipamorelin for the management of postoperative ileus in bowel resection patients. | Ipamorelin | Human, randomised, double-blind, placebo-controlled phase 2 trial in adults after bowel resection (n=114 in the safety population) | 0.03 mg/kg by intravenous infusion, twice daily | Postoperative day 1 to 7 or hospital discharge | Treatment-emergent adverse events occurred in 87.5% of the ipamorelin group and 94.8% of the placebo group. Median time to the first tolerated solid meal was 25.3 h vs 32.6 h (p = 0.15), and there were no significant differences in the key or secondary efficacy analyses. |
| Greenwood-Van Meerveld B et al.2012 · J Exp Pharmacol · DOIEfficacy of ipamorelin, a ghrelin mimetic, on gastric dysmotility in a rodent model of postoperative ileus. | Ipamorelin | Rat, postoperative ileus model, plus isolated gastric fundus tissue | 0.014–0.14 µmol/kg intravenous; 1 µM in the organ bath | Single dose | After surgery, 78% of a test meal remained in the stomach of vehicle-treated rats compared with 52% after ipamorelin 0.014 µmol/kg (P < 0.05). Ipamorelin also reversed the loss of gastric muscle contractility caused by the surgery. |
| Venkova K et al.2009 · J Pharmacol Exp Ther · DOIEfficacy of ipamorelin, a novel ghrelin mimetic, in a rodent model of postoperative ileus. | Ipamorelin | Rat, postoperative ileus model (laparotomy and intestinal manipulation) | 0.01–1 mg/kg intravenous bolus | Single dose, or 2 days of repeated dosing (four doses a day at 3-h intervals) | A single 1 mg/kg dose shortened the time to first bowel movement. Repeated dosing at 0.1 or 1 mg/kg significantly increased cumulative faecal pellet output, food intake and body weight gain over 48 h. |
| Andersen NB et al.2001 · Growth Horm IGF Res · DOIThe growth hormone secretagogue ipamorelin counteracts glucocorticoid-induced decrease in bone formation of adult rats. | Ipamorelin | Rat, 8-month-old females given the glucocorticoid methylprednisolone | 100 micrograms/kg s.c., three times daily | 3 months | Given with the glucocorticoid, ipamorelin significantly increased maximum tetanic tension of the calf muscles, and periosteal bone formation rate was four-fold higher than with the glucocorticoid alone. |
| Svensson J et al.2000 · J Endocrinol · DOIThe GH secretagogues ipamorelin and GH-releasing peptide-6 increase bone mineral content in adult female rats. | Ipamorelin | Rat, young adult females (n=7 for ipamorelin) | 0.5 mg/kg per day, continuous s.c. infusion by osmotic minipump | 12 weeks | Ipamorelin, GHRP-6 and GH all increased body weight and tibial and vertebral bone mineral content. Bone mineral content corrected for body weight was unchanged, and the authors attributed the increase to larger bone dimensions rather than denser bone. |
| Gobburu JV et al.1999 · Pharm Res · DOIPharmacokinetic-pharmacodynamic modeling of ipamorelin, a growth hormone releasing peptide, in human volunteers. | Ipamorelin | Human, healthy male volunteers, dose-escalation pharmacokinetic study (8 subjects at each of 5 dose levels) | 4.21, 14.02, 42.13, 84.27 and 140.45 nmol/kg infused over 15 minutes | Single infusion | Pharmacokinetics were dose-proportional, with a terminal half-life of 2 hours. Each dose produced a single episode of growth hormone release peaking at 0.67 hours, then declining to negligible levels. |
| Johansen PB et al.1999 · Growth Horm IGF Res · DOIIpamorelin, a new growth-hormone-releasing peptide, induces longitudinal bone growth in rats. | Ipamorelin | Rat, adult females | 18, 90 and 450 micrograms/day, s.c., split over three injections a day | 15 days | Longitudinal bone growth rose dose-dependently from 42 micrometres/day with vehicle to 44, 50 and 52 micrometres/day (P < 0.0001), with a dose-dependent gain in body weight. Total IGF-I, IGFBPs and serum bone-turnover markers did not change. |
| Raun K et al.1998 · Eur J Endocrinol · DOIIpamorelin, the first selective growth hormone secretagogue. | Ipamorelin | Primary rat pituitary cells, anaesthetised rats and conscious swine | Not stated in the abstract (dose-response; ED50 of 80 nmol/kg in rats and 2.3 nmol/kg in swine) | Acute dosing | Ipamorelin released growth hormone with potency and efficacy similar to GHRP-6. In swine it did not affect FSH, LH, prolactin or TSH, and unlike GHRP-6 and GHRP-2 it did not raise ACTH or cortisol, even at doses more than 200-fold above the ED50. |
| Li Y et al.2025 · J Allergy Clin Immunol · DOIPlasmacytoid dendritic cells alleviate allergic asthma via airway epithelial cell-dependent thymosin β4 expression. | KLOW | Mouse, house dust mite allergic asthma model (BDCA2-DTR mice); cell experiments | Tβ4 supplementation; amount not stated in the abstract | Not stated in the abstract | Tβ4 supplementation reversed the worsened asthma phenotype in mice depleted of plasmacytoid dendritic cells. Tβ4 inhibited IL-4/IL-13-induced JAK1/STAT6 signalling and CCL2 expression in macrophages. |
| Maar K et al.2025 · Int J Mol Sci · DOIThymosin Beta-4 Modulates Cardiac Remodeling by Regulating ROCK1 Expression in Adult Mammals. | KLOW | Mouse, permanent coronary ligation (heart attack) model; human cardiac cells | Systemic TB4 injection; amount not stated in the abstract | Not stated in the abstract | TB4 raised miR139-5p expression and modulated ROCK1 protein levels in mouse hearts and human cardiac cells, and may reverse or inhibit fibroblast-to-myofibroblast transformation. |
| Deng M et al.2023 · J Cachexia Sarcopenia Muscle · DOIGlycyl-l-histidyl-l-lysine-Cu2+ rescues cigarette smoking-induced skeletal muscle dysfunction via a sirtuin 1-dependent pathway. | KLOW | Mouse (C57BL/6), cigarette-smoke muscle dysfunction model; C2C12 muscle cells; plasma GHK measured in people with COPD (n=9) and healthy controls (n=11) | 0.2 and 2 mg/kg (route not stated in the abstract) | Not stated in the abstract | GHK-Cu reduced smoke-induced loss of muscle mass and improved grip strength (175.5 g untreated vs 257.6 g and 339.1 g). Plasma GHK was lower in the COPD group than in controls (70.27 vs 133.0 ng/mL). |
| Lee E et al.2021 · Altern Ther Health MedIntra-Articular Injection of BPC 157 for Multiple Types of Knee Pain. | KLOW | Human, retrospective chart review with phone survey (n=16, knee pain) | Intra-articular BPC-157 alone (n=12) or with thymosin beta-4 (n=4); amount not stated in the abstract | Most patients surveyed 6 months to 1 year after the injection | Eleven of 12 patients given BPC-157 alone reported significant improvement in knee pain, and 14 of 16 overall reported relief. No specific tools were used to measure function or quality of life. |
| Perovic D et al.2019 · J Orthop Surg Res · DOIStable gastric pentadecapeptide BPC 157 can improve the healing course of spinal cord injury and lead to functional recovery in rats. | KLOW | Rat, spinal cord compression injury model | 200 or 2 μg/kg, one intraperitoneal injection 10 min after injury | Assessed at 1, 4, 7, 15, 30, 90, 180 and 360 days | All injured rats given BPC-157 showed better tail motor function, no autotomy and resolved spasticity by day 15, with less axon loss, oedema and motoneuron loss on microscopy. |
| Dalmasso G et al.2008 · Gastroenterology · DOIPepT1-mediated tripeptide KPV uptake reduces intestinal inflammation. | KLOW | Mouse, DSS- and TNBS-induced colitis models; human intestinal epithelial cells (Caco2-BBE, HT29-Cl.19A) and T cells (Jurkat) | Nanomolar concentrations in cells; in mice, KPV added to drinking water (amount not stated in the abstract) | Not stated in the abstract | Nanomolar KPV inhibited NF-κB and MAP kinase signalling and reduced pro-inflammatory cytokine secretion, acting through the PepT1 transporter. Oral KPV reduced the incidence of DSS- and TNBS-induced colitis in mice. |
| Kannengiesser K et al.2008 · Inflamm Bowel Dis · DOIMelanocortin-derived tripeptide KPV has anti-inflammatory potential in murine models of inflammatory bowel disease. | KLOW | Mouse, DSS colitis and CD45RBhi transfer colitis models, including mice with a nonfunctional MC1 receptor | Not stated in the abstract | Not stated in the abstract | KPV gave earlier recovery and stronger regain of body weight, with fewer inflammatory infiltrates and lower colonic MPO activity. In MC1R-deficient mice, KPV rescued all treated animals from death during DSS colitis. |
| Miller TR et al.2006 · Arch Facial Plast Surg · DOIEffects of topical copper tripeptide complex on CO2 laser-resurfaced skin. | KLOW | Human, randomised controlled trial (n=13 completed), skin after CO2 laser resurfacing | Topical skin care products with or without GHK-Cu; concentration not stated in the abstract | 12 weeks | Computer analysis and blinded evaluators found no significant difference between groups in erythema, wrinkles or overall skin quality. On the patient questionnaire, rated improvement in overall skin quality was higher in the GHK-Cu group (P = .04). |
| Zhang L et al.2024 · Adv Healthc Mater · DOIKPV and RAPA Self-Assembled into Carrier-Free Nanodrugs for Vascular Calcification Therapy. | KPV | Mouse, vascular calcification model; cells in vitro (KPV combined with rapamycin) | KPV-rapamycin nanoparticles; amount not stated in the abstract | Not stated in the abstract | KPV-rapamycin nanoparticles significantly inhibited vascular calcification in mice compared with the other treatment groups, with reduced inflammatory responses and activated autophagy. The effect of KPV alone cannot be separated from rapamycin in this design. |
| Zhao Y et al.2022 · Acta Biomater · DOIA KPV-binding double-network hydrogel restores gut mucosal barrier in an inflamed colon. | KPV | Rat, TNBS-induced colitis model (intracolonic hydrogel) | KPV captured in a PMSP hydrogel, given intracolonically; amount not stated in the abstract | Not stated in the abstract | The hydrogel significantly improved the effect of KPV on colitis, the colon's epithelial barrier recovered, and gut flora shifted toward microorganisms associated with gut homeostasis. |
| Sun J et al.2021 · ACS Biomater Sci Eng · DOISelf-Cross-Linked Hydrogel of Cysteamine-Grafted γ-Polyglutamic Acid Stabilized Tripeptide KPV for Alleviating TNBS-Induced Ulcerative Colitis in Rats. | KPV | Rat, TNBS-induced ulcerative colitis model (rectal hydrogel) | KPV in a 4% SH-PGA hydrogel, given rectally; KPV amount not stated in the abstract | Not stated in the abstract | The KPV hydrogel reduced body weight loss and disease activity score, prevented colon shortening, lowered colonic myeloperoxidase and reduced TNF-α and IL-6. The abstract notes that plain KPV solution is very unstable when given rectally. |
| Xiao B et al.2017 · Mol Ther · DOIOrally Targeted Delivery of Tripeptide KPV via Hyaluronic Acid-Functionalized Nanoparticles Efficiently Alleviates Ulcerative Colitis. | KPV | Mouse, ulcerative colitis model; colonic epithelial cells and macrophages | Oral KPV in hyaluronic acid-functionalised nanoparticles within a chitosan/alginate hydrogel; amount not stated in the abstract | Not stated in the abstract | The HA-KPV nanoparticle hydrogel prevented mucosal damage and lowered TNF-α more than a KPV nanoparticle hydrogel without hyaluronic acid. The nanoparticles appeared nontoxic and biocompatible with intestinal cells. |
| Pawar K et al.2017 · J Pharm Sci · DOITransdermal Iontophoretic Delivery of Lysine-Proline-Valine (KPV) Peptide Across Microporated Human Skin. | KPV | Human skin ex vivo (dermatomed), transdermal delivery study | Not stated in the abstract | Not stated in the abstract | Passive KPV permeation was below detection (0.01 μg/mL). Microneedles raised it to 4.4 μg/cm²/h, and iontophoresis alone and with microneedles increased it 8- and 35-fold over microneedles alone. |
| Dalmasso G et al.2008 · Gastroenterology · DOIPepT1-mediated tripeptide KPV uptake reduces intestinal inflammation. | KPV | Mouse, DSS- and TNBS-induced colitis models; human intestinal epithelial cells (Caco2-BBE, HT29-Cl.19A) and T cells (Jurkat) | Nanomolar concentrations in cells; in mice, KPV added to drinking water (amount not stated in the abstract) | Not stated in the abstract | Nanomolar KPV inhibited NF-κB and MAP kinase signalling and reduced pro-inflammatory cytokine secretion, acting through the PepT1 transporter. Oral KPV reduced the incidence of DSS- and TNBS-induced colitis in mice. |
| Kannengiesser K et al.2008 · Inflamm Bowel Dis · DOIMelanocortin-derived tripeptide KPV has anti-inflammatory potential in murine models of inflammatory bowel disease. | KPV | Mouse, DSS colitis and CD45RBhi transfer colitis models, including mice with a nonfunctional MC1 receptor | Not stated in the abstract | Not stated in the abstract | KPV gave earlier recovery and stronger regain of body weight, with fewer inflammatory infiltrates and lower colonic MPO activity. In MC1R-deficient mice, KPV rescued all treated animals from death during DSS colitis, suggesting effects partly independent of MC1R. |
| Elliott RJ et al.2004 · J Invest Dermatol · DOIalpha-Melanocyte-stimulating hormone, MSH 11-13 KPV and adrenocorticotropic hormone signalling in human keratinocyte cells. | KPV | Cell culture (HaCaT and normal human keratinocytes; Chinese hamster ovary cells expressing MC1R) | 10⁻¹⁵ to 10⁻⁷ M | Not stated in the abstract | KPV did not raise cyclic AMP in keratinocytes. It raised intracellular calcium in HaCaT keratinocytes when an adenosine agonist was present, and in cells transfected with the MC1 receptor. |
| Lonati C et al.2021 · Peptides · DOINDP-MSH treatment recovers marginal lungs during ex vivo lung perfusion (EVLP). | Melanotan I | Rat, ex vivo lung perfusion after ischaemia/reperfusion or cardiac death (N=10 per protocol, 5 treated) | Not stated in the abstract (NDP-MSH given before lung procurement and during perfusion) | Not stated in the abstract | NDP-MSH lowered inflammatory mediators, leukocytes and lactate in perfusate, raised ATP in ischaemia/reperfusion lungs and improved vascular and airway measures in cardiac-death lungs. MC1R and MC5R were found in lung tissue. |
| Langendonk JG et al.2015 · N Engl J Med · DOIAfamelanotide for Erythropoietic Protoporphyria. | Melanotan I | Human, two randomised double-blind placebo-controlled trials in erythropoietic protoporphyria (EU n=74, US n=94) | Afamelanotide 16 mg subcutaneous implant (Scenesse formulation) or placebo, every 60 days | 180 days (US, 3 implants) and 270 days (EU, 5 implants) | Median pain-free time in direct sunlight was longer with afamelanotide (US 69.4 vs 40.8 hours, P=0.04; EU 6.0 vs 0.8 hours, P=0.005), and the EU trial recorded fewer phototoxic reactions (77 vs 146). Adverse events were mostly mild. |
| Lengweiler S et al.2015 · Skin Pharmacol Physiol · DOIEvaluation of the immunogenicity of the synthetic α-melanocyte-stimulating hormone (α-MSH) analogue afamelanotide ([Nle4-D-Phe7]-α-MSH, Scenesse®) in erythropoietic protoporphyria patients by ELISA detecting both anti-afamelanotide and anti-α-MSH antibodies. | Melanotan I | Human, erythropoietic protoporphyria patients in phase II/III trials (n=26), antibody assay | Not stated in the abstract (afamelanotide, Scenesse) | Up to 6 years of exposure | A new ELISA found no anti-drug antibodies in 23 of 26 patients. Three had pre-existing immunoreactivity to afamelanotide and alpha-MSH, and their titres did not change during treatment. |
| Böhm M et al.2014 · J Eur Acad Dermatol Venereol · DOIBeneficial effects of the melanocortin analogue Nle4-D-Phe7-α-MSH in acne vulgaris. | Melanotan I | Human, phase II open-label pilot in acne vulgaris (n=3) | Afamelanotide 16 mg subcutaneous sustained-release resorbable implant | Assessed 56 days after the first implant | Total and inflammatory acne lesion counts fell in all 3 patients and quality-of-life scores improved. All 3 showed increased pigmentation, mainly on the face. |
| Biolcati G et al.2014 · Clin Exp Dermatol · DOIEfficacy of the melanocortin analogue Nle4-D-Phe7-α-melanocyte-stimulating hormone in the treatment of patients with Hailey-Hailey disease. | Melanotan I | Cell culture (Hailey-Hailey lesion keratinocytes) plus human open-label pilot (n=2) | Patients: afamelanotide 16 mg subcutaneous sustained-release resorbable implant; cell dose not stated in the abstract | Assessed 30 and 60 days after the first implant | In lesion-derived keratinocytes, afamelanotide upregulated Nrf2 and restored defective proliferation. Both patients had 100% clearance of lesions at 60 days. |
| Rennalls LP et al.2010 · Immunology · DOIThe melanocortin receptor agonist NDP-MSH impairs the allostimulatory function of dendritic cells. | Melanotan I | Cell culture (human dendritic cells) | Not stated in the abstract | Not stated in the abstract | Dendritic cells expressed mRNA for all known melanocortin receptors. NDP-MSH reduced their ability to stimulate allogeneic T cells and lowered surface CD86, ICAM-1 and CD1a. |
| Jiang J et al.1995 · Pigment Cell Res · DOIThe melanotropic peptide, [Nle4,D-Phe7] alpha-MSH, stimulates human melanoma tyrosinase activity and inhibits cell proliferation. | Melanotan I | Cell culture (17 human melanoma cell lines) | Not stated in the abstract | 72 hours, and 6 to 43 days in some lines | Only one melanotic line consistently raised tyrosinase activity. Cell numbers fell sharply in both melanotic and amelanotic lines, and growth inhibition persisted days after the peptide was removed. |
| Frändberg PA et al.1994 · Biochem Biophys Res Commun · DOIEvidence for alternate points of attachment for alpha-MSH and its stereoisomer [Nle4, D-Phe7]-alpha-MSH at the melanocortin-1 receptor. | Melanotan I | Cell culture (COS-7 cells expressing wild-type and mutant human MC1R) | Not applicable (receptor binding assay) | Not applicable | Single alanine mutations at Asp117 or His260 cut alpha-MSH binding affinity by 267-fold and 132-fold, while NDP-MSH affinity was unchanged, pointing to different attachment points for the two agonists. |
| Wekwejt P et al.2023 · Biomed Pharmacother · DOIMelanotan-II reverses memory impairment induced by a short-term HF diet. | Melanotan II | Zebrafish, short-term high-fat diet | Not stated in the abstract | About three weeks of high-fat diet | A high-fat diet impaired recognition memory, raised anxiety-like behaviour and reduced exploration. Fish on the high-fat diet given MT-II behaved like the control-diet group. |
| Gilhooley E et al.2021 · Dermatology · DOIMelanotan II User Experience: A Qualitative Study of Online Discussion Forums. | Melanotan II | Human, qualitative study of online forums (623 entries, 205 participants, UK and Ireland) | Not stated in the abstract | Forum data from January 2016 to October 2017 | Users sought a tan before holidays and fitness or bodybuilding competitions. The authors flagged risks to pigmented skin lesions, infection, contaminated products, polypharmacy and sunbed use. |
| Peters B et al.2020 · CEN Case Rep · DOIMelanotan II: a possible cause of renal infarction: review of the literature and case report. | Melanotan II | Human, case report with literature review | Not stated in the abstract | Not stated in the abstract | The authors report a renal infarction most likely attributed to Melanotan II and note earlier reports of rhabdomyolysis and renal failure. They suggest a thrombotic effect and possible direct kidney toxicity as mechanisms. |
| Dreyer BA et al.2019 · BMJ Case Rep · DOIMelanotan-induced priapism: a hard-earned tan. | Melanotan II | Human, single case report | Not stated in the abstract (abdominal subcutaneous injection) | Single presentation; 4-week follow-up | A man presented with low-flow priapism after injecting melanotan. It was managed without surgical shunting, but erectile function had not recovered at 4 weeks. |
| Strader AD et al.2007 · J Pharmacol Exp Ther · DOIThe effects of the melanocortin agonist (MT-II) on subcutaneous and visceral adipose tissue in rodents. | Melanotan II | Mouse (diet-induced obese and low-fat fed), replicated in diet-induced obese rats | Not stated in the abstract (peripheral administration) | Not stated in the abstract | Obese mice given MT-II lost weight and body fat, with reductions in both visceral and subcutaneous fat; low-fat fed mice kept their body weight. Pair-fed controls lost similar weight but kept more fat. |
| Seeley RJ et al.2005 · Endocrinology · DOIThe effect of the melanocortin agonist, MT-II, on the defended level of body adiposity. | Melanotan II | Rat, diet-induced obesity (some pre-restricted to different body weights) | Various doses by osmotic minipump (values not stated in the abstract) | 28 days | Whatever the starting body fat, final body fat was set by the MT-II dose, and MT-II rats had less body fat than vehicle rats. Food-restricted rats given MT-II ate more than ad libitum rats given MT-II. |
| Wessells H et al.2003 · Ann N Y Acad Sci · DOIMT-II induces penile erection via brain and spinal mechanisms. | Melanotan II | Rat (awake males; anaesthetised rats for intracorporal pressure) | Graded doses i.c.v., intrathecal and i.v.; optimal erectile response at 1 microgram i.c.v. and intrathecal | Single dose, erections scored for 90 min | MT-II produced dose-dependent penile erections through brain and lumbosacral spinal melanocortin receptors, blocked by SHU-9119. Injected directly into the penis it did not raise intracorporal pressure, so the action is central, not in the penis. |
| Bednarek MA et al.1999 · Peptides · DOIStructure-function studies on the cyclic peptide MT-II, lactam derivative of alpha-melanotropin. | Melanotan II | Cell/receptor assays (human MC3, MC4 and MC5 receptors) and NMR | Not applicable (in-vitro binding and activation) | Not applicable | Swapping His for Ala left potency similar to MT-II, Arg to Ala cut potency about 100-fold, and Phe or Trp to Ala gave inactive compounds. Retro, enantio and retro-enantio analogues lost much of their potency. |
| Li X et al.2025 · Redox Biol · DOIMOTS-c attenuates lung ischemia-reperfusion injury via MYH9-Dependent nuclear translocation and transcriptional activation of antioxidant genes. | MOTS-C | Rat, lung ischaemia-reperfusion injury model; human cardiopulmonary bypass patients (serum levels) | Not stated in the abstract | Serum measured within 24 h after bypass | Exogenous MOTS-c in rats reduced oxidative damage, inflammation, lung injury and mortality. In patients, the rise in serum MOTS-c within 24 h of bypass predicted ARDS (multivariate model AUC 0.885). |
| Li K et al.2025 · Free Radic Biol Med · DOIMOTS-c attenuates mitochondrial dysfunction induces pyroptosis and cartilage degradation in osteoarthritis via an Nrf2-Dependent Mechanism. | MOTS-C | Chondrocytes (LPS-induced) and mouse osteoarthritis model | Not stated in the abstract | Not stated in the abstract | MOTS-c improved mitochondrial dysfunction and reduced chondrocyte pyroptosis via the Nrf2/TXNIP/NLRP3 axis, and on imaging and histology delayed cartilage degeneration in the mouse model. |
| Lin C et al.2024 · Gut · DOINovel function of MOTS-c in mitochondrial remodelling contributes to its antiviral role during HBV infection. | MOTS-C | Human observational cohort (85 healthy subjects, 404 HBV patients) plus HBV-infected mice and cells | Not stated in the abstract | Not stated in the abstract | MOTS-c levels correlated negatively with HBV DNA (R = −0.71). In mice and cells MOTS-c inhibited HBV replication by 50–70% with improved liver function and no notable toxicity, and promoted mitochondrial biogenesis and MAVS signalling. |
| Yin Y et al.2024 · Adv Sci (Weinh) · DOIMitochondrial-Derived Peptide MOTS-c Suppresses Ovarian Cancer Progression by Attenuating USP7-Mediated LARS1 Deubiquitination. | MOTS-C | Ovarian cancer cell lines and mouse xenograft; patient serum and tumour tissue | Not stated in the abstract | Not stated in the abstract | MOTS-c levels were lower in serum and tumour tissue from ovarian cancer patients. Exogenous MOTS-c inhibited ovarian cancer cell proliferation, migration and invasion and showed an anti-tumour effect in vivo without systemic toxicity, by promoting LARS1 degradation. |
| Wu J et al.2023 · Acta Biochim Biophys Sin (Shanghai) · DOIThe protective effect of the mitochondrial-derived peptide MOTS-c on LPS-induced septic cardiomyopathy. | MOTS-C | LPS-induced septic cardiomyopathy model (species not stated in the abstract) | Not stated in the abstract | Not stated in the abstract | MOTS-c reduced inflammatory cytokine mRNA in cardiomyocytes, lowered circulating CK-MB and TnT, and reduced cardiomyocyte apoptosis; the AMPK inhibitor compound C abolished these effects. |
| Kim KH et al.2018 · Cell Metab · DOIThe Mitochondrial-Encoded Peptide MOTS-c Translocates to the Nucleus to Regulate Nuclear Gene Expression in Response to Metabolic Stress. | MOTS-C | Cell culture (metabolic stress models) | Not stated in the abstract | Not stated in the abstract | Under metabolic stress MOTS-c translocated to the nucleus in an AMPK-dependent manner and regulated a broad range of genes in response to glucose restriction, including antioxidant response element genes, and interacted with NRF2. |
| Lee C et al.2015 · Cell Metab · DOIThe mitochondrial-derived peptide MOTS-c promotes metabolic homeostasis and reduces obesity and insulin resistance. | MOTS-C | Mouse, high-fat diet and ageing models; cell work | Not stated in the abstract | Not stated in the abstract | The paper that named MOTS-c. Its primary target appeared to be skeletal muscle, where it inhibited the folate cycle and de novo purine biosynthesis and activated AMPK; MOTS-c treatment in mice prevented age-dependent and high-fat-diet-induced insulin resistance and diet-induced obesity. |
| Christen S et al.2026 · Nat Metab · DOIThe differential impact of three different NAD+ boosters on circulatory NAD and microbial metabolism in humans. | NAD+ | Human, randomised open-label placebo-controlled study (n=65, healthy adults); molecules: oral NR, NMN and nicotinamide | Not stated in the abstract | 14 days | NR and NMN, but not nicotinamide, comparably raised circulating NAD+. Ex vivo work suggested NR and NMN are converted by gut microbes to nicotinic acid, which then raises NAD+. |
| Pencina KM et al.2023 · J Clin Endocrinol Metab · DOINicotinamide Adenine Dinucleotide Augmentation in Overweight or Obese Middle-Aged and Older Adults: A Physiologic Study. | NAD+ | Human, randomised controlled trial (n=30, overweight or obese adults aged 45+); molecule: oral NMN (MIB-626 tablets) | Two 500 mg NMN tablets twice daily | 28 days | NMN substantially raised circulating NAD+ and its metabolites. Body weight (−1.9 kg), diastolic blood pressure, total and LDL cholesterol fell more than with placebo; muscle strength, aerobic capacity, insulin sensitivity and liver fat did not differ. |
| Vreones M et al.2023 · Aging Cell · DOIOral nicotinamide riboside raises NAD+ and lowers biomarkers of neurodegenerative pathology in plasma extracellular vesicles enriched for neuronal origin. | NAD+ | Human, randomised placebo-controlled crossover trial (n=22, healthy older adults); molecule: oral NR | 500 mg NR twice a day | 6 weeks | NR increased NAD+ in plasma extracellular vesicles enriched for neuronal origin and lowered their levels of Aβ42, pJNK and pERK1/2. |
| Katayoshi T et al.2023 · Sci Rep · DOINicotinamide adenine dinucleotide metabolism and arterial stiffness after long-term nicotinamide mononucleotide supplementation: a randomized, double-blind, placebo-controlled trial. | NAD+ | Human, randomised double-blind placebo-controlled trial (n=36, healthy middle-aged adults); molecule: oral NMN | 125 mg NMN capsule twice a day (250 mg/day) | 12 weeks | Serum nicotinamide rose in the NMN group. Pulse wave velocity tended to fall but did not differ significantly from placebo; no adverse events were reported. |
| Brakedal B et al.2022 · Cell Metab · DOIThe NADPARK study: A randomized phase I trial of nicotinamide riboside supplementation in Parkinson's disease. | NAD+ | Human, randomised double-blind phase I trial (n=30, newly diagnosed Parkinson's disease); molecule: oral NR | 1,000 mg NR | 30 days | NR was well tolerated and gave a significant but variable rise in brain NAD measured by 31P-MRS, altered cerebral metabolism on FDG-PET in those whose brain NAD rose, and lowered inflammatory cytokines in serum and cerebrospinal fluid. |
| Castro-Marrero J et al.2021 · Nutrients · DOIEffect of Dietary Coenzyme Q10 Plus NADH Supplementation on Fatigue Perception and Health-Related Quality of Life in Individuals with Myalgic Encephalomyelitis/Chronic Fatigue Syndrome: A Prospective, Randomized, Double-Blind, Placebo-Controlled Trial. | NAD+ | Human, randomised double-blind placebo-controlled trial (n=207, ME/CFS); molecule: oral NADH combined with CoQ10 | 20 mg NADH plus 200 mg CoQ10 once daily | 12 weeks | Within the treatment group, cognitive fatigue and overall FIS-40 score fell and quality of life improved from baseline; the effect of NADH cannot be separated from that of CoQ10. |
| Elhassan YS et al.2019 · Cell Rep · DOINicotinamide Riboside Augments the Aged Human Skeletal Muscle NAD+ Metabolome and Induces Transcriptomic and Anti-inflammatory Signatures. | NAD+ | Human, randomised double-blind crossover trial (n=12, aged men); molecule: oral NR | 1 g NR per day | 21 days | NR raised the skeletal muscle NAD+ metabolome and lowered circulating inflammatory cytokines, without altering mitochondrial bioenergetics. |
| Martens CR et al.2018 · Nat Commun · DOIChronic nicotinamide riboside supplementation is well-tolerated and elevates NAD+ in healthy middle-aged and older adults. | NAD+ | Human, randomised double-blind placebo-controlled crossover trial (healthy middle-aged and older adults; n not stated in the abstract); molecule: oral NR | Not stated in the abstract | 2 × 6 weeks | Chronic NR was well tolerated and stimulated NAD+ metabolism; the authors suggest blood pressure and arterial stiffness as outcomes for future trials. |
| Clayton AH et al.2022 · J Womens Health (Larchmt) · DOISafety Profile of Bremelanotide Across the Clinical Development Program. | PT-141 | Human, integrated safety review of phase 1–3 programme (3,500 subjects, 43 studies; phase 3 double-blind n=1,247) | Not stated in the abstract (dosed per label in phase 3) | Up to 18 months in phase 3 | The most common adverse events versus placebo were nausea (40.0% vs 1.3%), flushing (20.3% vs 1.3%), headache (11.3% vs 1.9%) and injection site reactions (5.4% vs 0.5%). Small, transient blood pressure rises were seen. |
| Kingsberg SA et al.2019 · Obstet Gynecol · DOIBremelanotide for the Treatment of Hypoactive Sexual Desire Disorder: Two Randomized Phase 3 Trials. | PT-141 | Human, two randomised controlled phase 3 trials (RECONNECT; n=1,267 randomised; premenopausal women with HSDD) | 1.75 mg subcutaneous, as needed | 24 weeks | Compared with placebo, bremelanotide increased sexual desire (integrated 0.35, P<.001) and reduced distress related to low desire (integrated −0.33, P<.001). Nausea, flushing and headache were more common with bremelanotide. |
| White WB et al.2017 · J Hypertens · DOIUsefulness of ambulatory blood pressure monitoring to assess the melanocortin receptor agonist bremelanotide. | PT-141 | Human, randomised double-blind placebo-controlled trial (n=397 premenopausal women) | 0.75, 1.25 or 1.75 mg subcutaneous | Two doses 24 h apart, ambulatory monitoring | Systolic pressure rose by up to about 3 mmHg versus placebo in the 4 h after dosing, with peaks usually under 15 minutes. At 1.75 mg, heart rate fell by 4.6–4.7 bpm. |
| Clayton AH et al.2016 · Womens Health (Lond) · DOIBremelanotide for female sexual dysfunctions in premenopausal women: a randomized, placebo-controlled dose-finding trial. | PT-141 | Human, randomised placebo-controlled dose-finding trial (efficacy n=327; premenopausal women) | 0.75, 1.25 or 1.75 mg subcutaneous, as desired | 12 weeks | For the pooled 1.25/1.75 mg groups, satisfying sexual events rose by 0.7 a month versus 0.2 on placebo (p=0.0180), with better sexual function and distress scores. Adverse events were nausea, flushing and headache. |
| Safarinejad MR et al.2008 · J Urol · DOISalvage of sildenafil failures with bremelanotide: a randomized, double-blind, placebo controlled study. | PT-141 | Human, randomised double-blind placebo-controlled trial (n=342 men with erectile dysfunction not responding to sildenafil) | 10 mg intranasal, 45 minutes to 2 hours before sexual stimulation | At least 16 attempts at home | Positive clinical results were reported in 33.5% on bremelanotide versus 8.5% on placebo (p=0.03), with greater intercourse satisfaction. Drug-related adverse effects were more frequent with bremelanotide. |
| Diamond LE et al.2006 · J Sex Med · DOIAn effect on the subjective sexual response in premenopausal women with sexual arousal disorder by bremelanotide (PT-141), a melanocortin receptor agonist. | PT-141 | Human, randomised double-blind crossover trial (n=18 premenopausal women with sexual arousal disorder) | 20 mg intranasal, single dose | Single session, 24-hour follow-up | More women reported moderate or high desire after bremelanotide than after placebo (P=0.0114). Vaginal vasocongestion did not change significantly. |
| Diamond LE et al.2005 · Urology · DOICo-administration of low doses of intranasal PT-141, a melanocortin receptor agonist, and sildenafil to men with erectile dysfunction results in an enhanced erectile response. | PT-141 | Human, randomised crossover trial (n=19 men with erectile dysfunction) | 7.5 mg intranasal PT-141 with 25 mg sildenafil | Single doses; 6-hour post-dose assessment | PT-141 plus sildenafil produced a significantly greater erectile response than sildenafil alone. The combination did not bring new or more frequent adverse events. |
| Rosen RC et al.2004 · Int J Impot Res · DOIEvaluation of the safety, pharmacokinetics and pharmacodynamic effects of subcutaneously administered PT-141, a melanocortin receptor agonist, in healthy male subjects and in patients with an inadequate response to Viagra. | PT-141 | Human, phase 1/2 randomised trials (healthy men; men with inadequate response to Viagra) | 0.3–10 mg subcutaneous in healthy men; 4 or 6 mg in ED patients (crossover) | Single doses | Doses above 1.0 mg produced a significant erectile response on RigiScan in healthy men, and both 4 and 6 mg worked in ED patients. PT-141 was well tolerated in both studies. |
| Bajaj HS et al.2026 · Lancet · DOIEfficacy and safety of retatrutide, a GIP, GLP-1, and glucagon receptor agonist, in people with type 2 diabetes and inadequate glycaemic control with diet and exercise (TRANSCEND-T2D-1): a double-blind, randomised, phase 3 trial. | Retatrutide | Human, phase 3 randomised controlled trial in adults with type 2 diabetes (n=537) | 4, 9 or 12 mg once weekly, subcutaneous, vs placebo | 40 weeks | HbA1c fell by 1.69%, 1.86% and 1.94% with 4, 9 and 12 mg vs 0.81% with placebo, and body weight changed by −11.5%, −13.9% and −15.3% vs −2.6%. Discontinuation for adverse events was 2–5% with retatrutide and 0% with placebo. |
| Coskun T et al.2025 · Lancet Diabetes Endocrinol · DOIEffects of retatrutide on body composition in people with type 2 diabetes: a substudy of a phase 2, double-blind, parallel-group, placebo-controlled, randomised trial. | Retatrutide | Human, phase 2 randomised controlled body-composition substudy in type 2 diabetes (n=189 enrolled; 103 with both DXA scans) | 0.5, 4, 8 or 12 mg once weekly, subcutaneous, vs placebo or dulaglutide 1.5 mg | 36 weeks | Total fat mass measured by DXA fell by 4.9% (0.5 mg), 15.2% (4 mg), 26.1% (8 mg) and 23.2% (12 mg), compared with 2.6% on dulaglutide and 4.5% on placebo. |
| Kanu C et al.2025 · Diabetes Obes Metab · DOIAppetite, eating attitudes, and eating behaviours during treatment with retatrutide in adults with type 2 diabetes: Results of a phase 2 study. | Retatrutide | Human, exploratory analysis of a phase 2 randomised controlled trial in type 2 diabetes (n=275) | 0.5, 4, 8 or 12 mg once weekly, vs placebo or dulaglutide 1.5 mg | 24 and 36 weeks | Participants on 4 mg or more reported greater reductions in overall appetite, hunger and prospective food consumption than placebo at week 24. Lower perceived hunger and disinhibition correlated with weight reduction at week 36. |
| Sanyal AJ et al.2024 · Nat Med · DOITriple hormone receptor agonist retatrutide for metabolic dysfunction-associated steatotic liver disease: a randomized phase 2a trial. | Retatrutide | Human, phase 2a randomised controlled substudy in adults with MASLD and ≥10% liver fat (n=98) | 1, 4, 8 or 12 mg once weekly, subcutaneous, vs placebo | 48 weeks (liver fat primary endpoint at 24 weeks) | Mean relative change in liver fat at 24 weeks was −42.9% (1 mg), −57.0% (4 mg), −81.4% (8 mg) and −82.4% (12 mg) vs +0.3% with placebo. Normal liver fat (<5%) was reached by 27% to 86% of the retatrutide groups and 0% on placebo. |
| Jastreboff AM et al.2023 · N Engl J Med · DOITriple-Hormone-Receptor Agonist Retatrutide for Obesity - A Phase 2 Trial. | Retatrutide | Human, phase 2 randomised controlled trial in adults with obesity (n=338) | 1, 4, 8 or 12 mg once weekly, subcutaneous (4 and 8 mg arms started at 2 or 4 mg; 12 mg started at 2 mg), vs placebo | 48 weeks | Mean body weight change at 48 weeks was −8.7% (1 mg), −17.1% (4 mg), −22.8% (8 mg) and −24.2% (12 mg) vs −2.1% with placebo. The most common adverse events were gastrointestinal, dose-related and mostly mild to moderate. |
| Urva S et al.2022 · Lancet · DOILY3437943, a novel triple GIP, GLP-1, and glucagon receptor agonist in people with type 2 diabetes: a phase 1b, multicentre, double-blind, placebo-controlled, randomised, multiple-ascending dose trial. | Retatrutide | Human, phase 1b randomised multiple-ascending dose trial in type 2 diabetes (n=72) | 0.5, 1.5, 3, 3/6 or 3/6/9/12 mg once weekly, subcutaneous, vs placebo or dulaglutide 1.5 mg | 12 weeks | Treatment-emergent adverse events were reported by 63% of participants on LY3437943, 60% on dulaglutide and 54% on placebo, with gastrointestinal disorders the most frequent. The primary outcome was safety and tolerability. |
| Bajaj HS et al.2026 · Lancet · DOIEfficacy and safety of retatrutide, a GIP, GLP-1, and glucagon receptor agonist, in people with type 2 diabetes and inadequate glycaemic control with diet and exercise (TRANSCEND-T2D-1): a double-blind, randomised, phase 3 trial. | Retatrutide + Cagrilintide | Human, phase 3 randomised controlled trial in adults with type 2 diabetes (n=537) | 4, 9 or 12 mg once weekly, subcutaneous, vs placebo | 40 weeks | HbA1c fell by 1.69%, 1.86% and 1.94% with 4, 9 and 12 mg vs 0.81% with placebo, and body weight changed by −11.5%, −13.9% and −15.3% vs −2.6%. Discontinuation for adverse events was 2–5% with retatrutide and 0% with placebo. |
| Garvey WT et al.2025 · N Engl J Med · DOICoadministered Cagrilintide and Semaglutide in Adults with Overweight or Obesity. | Retatrutide + Cagrilintide | Human, phase 3a randomised controlled trial (REDEFINE 1), CagriSema vs each component vs placebo, adults with overweight or obesity without diabetes (n=3417) | Cagrilintide 2.4 mg + semaglutide 2.4 mg, semaglutide 2.4 mg, cagrilintide 2.4 mg, or placebo, once weekly | 68 weeks | Mean body weight change was −20.4% with CagriSema (cagrilintide with semaglutide) versus −3.0% with placebo. The abstract does not report the result for the cagrilintide-alone arm. |
| Sanyal AJ et al.2024 · Nat Med · DOITriple hormone receptor agonist retatrutide for metabolic dysfunction-associated steatotic liver disease: a randomized phase 2a trial. | Retatrutide + Cagrilintide | Human, phase 2a randomised controlled substudy in adults with MASLD and ≥10% liver fat (n=98) | 1, 4, 8 or 12 mg once weekly, subcutaneous, vs placebo | 48 weeks (liver fat primary endpoint at 24 weeks) | Mean relative change in liver fat at 24 weeks was −42.9% (1 mg), −57.0% (4 mg), −81.4% (8 mg) and −82.4% (12 mg) vs +0.3% with placebo. |
| Gabe MBN et al.2024 · Diabetes Obes Metab · DOICagrilintide is not associated with clinically relevant QTc prolongation: A thorough QT study in healthy participants. | Retatrutide + Cagrilintide | Human, randomised double-blind thorough QT study, cagrilintide alone, healthy participants (n=105) | Cagrilintide once weekly subcutaneous, escalated to 4.5 mg; placebo arms received moxifloxacin 400 mg as a positive control | Not stated in the abstract | No clinically relevant QTcF prolongation occurred after the last 4.5 mg dose; the upper limits of the 90% confidence intervals of the placebo-adjusted changes were below 10 ms at all time points. |
| Jastreboff AM et al.2023 · N Engl J Med · DOITriple-Hormone-Receptor Agonist Retatrutide for Obesity - A Phase 2 Trial. | Retatrutide + Cagrilintide | Human, phase 2 randomised controlled trial in adults with obesity (n=338) | 1, 4, 8 or 12 mg once weekly, subcutaneous (4 and 8 mg arms started at 2 or 4 mg; 12 mg started at 2 mg), vs placebo | 48 weeks | Mean body weight change at 48 weeks was −8.7% (1 mg), −17.1% (4 mg), −22.8% (8 mg) and −24.2% (12 mg) vs −2.1% with placebo. The most common adverse events were gastrointestinal, dose-related and mostly mild to moderate. |
| Frias JP et al.2023 · Lancet · DOIEfficacy and safety of co-administered once-weekly cagrilintide 2·4 mg with once-weekly semaglutide 2·4 mg in type 2 diabetes: a multicentre, randomised, double-blind, active-controlled, phase 2 trial. | Retatrutide + Cagrilintide | Human, phase 2 randomised double-blind trial, CagriSema (cagrilintide + semaglutide) vs semaglutide vs cagrilintide, type 2 diabetes on metformin (n=92) | CagriSema, semaglutide or cagrilintide, each escalated to 2.4 mg once weekly subcutaneous | 32 weeks | HbA1c fell by 2.2 points with CagriSema, 1.8 with semaglutide and 0.9 with cagrilintide alone. Body weight fell by 15.6%, 5.1% and 8.1% respectively. The partner drug in this trial was semaglutide, not retatrutide. |
| Urva S et al.2022 · Lancet · DOILY3437943, a novel triple GIP, GLP-1, and glucagon receptor agonist in people with type 2 diabetes: a phase 1b, multicentre, double-blind, placebo-controlled, randomised, multiple-ascending dose trial. | Retatrutide + Cagrilintide | Human, phase 1b randomised multiple-ascending dose trial in type 2 diabetes (n=72) | 0.5, 1.5, 3, 3/6 or 3/6/9/12 mg once weekly, subcutaneous, vs placebo or dulaglutide 1.5 mg | 12 weeks | Treatment-emergent adverse events were reported by 63% of participants on LY3437943, 60% on dulaglutide and 54% on placebo, with gastrointestinal disorders the most frequent. |
| Lau DCW et al.2021 · Lancet · DOIOnce-weekly cagrilintide for weight management in people with overweight and obesity: a multicentre, randomised, double-blind, placebo-controlled and active-controlled, dose-finding phase 2 trial. | Retatrutide + Cagrilintide | Human, phase 2 randomised controlled trial, cagrilintide alone, adults with overweight or obesity without diabetes (n=906 randomised: 706 cagrilintide, 99 liraglutide, 101 placebo) | Cagrilintide 0.3, 0.6, 1.2, 2.4 or 4.5 mg once weekly, subcutaneous; comparator liraglutide 3.0 mg once daily | 26 weeks treatment (including up to 6 weeks escalation), plus 6 weeks follow-up | Mean weight reduction was 6.0%–10.8% across the cagrilintide doses versus 3.0% with placebo. Cagrilintide 4.5 mg reduced weight by 10.8% compared with 9.0% for liraglutide 3.0 mg. |
| Konstantinopolsky MA et al.2022 · Bull Exp Biol Med · DOISelank, a Peptide Analog of Tuftsin, Attenuates Aversive Signs of Morphine Withdrawal in Rats. | Selank | Rat (outbred), naloxone-precipitated morphine withdrawal model | 0.3 mg/kg, intraperitoneal (diazepam 2 mg/kg as comparator) | Single injection | Selank reduced the total morphine withdrawal index by 39.6% and raised the tactile sensitivity threshold 9-fold, slightly less than diazepam (49.3% and 13-fold). |
| Panikratova YR et al.2020 · Dokl Biol Sci · DOIFunctional Connectomic Approach to Studying Selank and Semax Effects. | Selank | Human, placebo-controlled resting-state fMRI study in healthy participants (n=52, Selank, Semax or placebo) | Not stated in the abstract | Single administration; scans before and 5 and 20 min after | Differences were found in connectivity between the right amygdala and the right temporal cortex, with both general and specific effects of Selank and Semax. |
| Kolik LG et al.2019 · Bull Exp Biol Med · DOISelank, Peptide Analogue of Tuftsin, Protects Against Ethanol-Induced Memory Impairment by Regulating of BDNF Content in the Hippocampus and Prefrontal Cortex in Rats. | Selank | Rat (outbred), 30 weeks of 10% ethanol as the only fluid; object recognition test | 0.3 mg/kg a day, intraperitoneal | 7 days | Selank prevented ethanol-induced memory and attention disturbances during withdrawal and prevented the ethanol-induced rise in BDNF in the hippocampus and frontal cortex. |
| Medvedev VE et al.2015 · Zh Nevrol Psikhiatr Im S S Korsakova · DOI[Optimization of the treatment of anxiety disorders with selank]. | Selank | Human, randomised controlled trial, anxiety disorders (n=70: 30 phenazepam alone, 40 Selank plus phenazepam) | Not stated in the abstract | Not stated in the abstract | Adding Selank brought on the effect of phenazepam earlier on the HDRS and reduced phenazepam side effects such as attention and memory impairment, sedation and asthenia, during treatment and after withdrawal. Quality of life on the SF-36 improved. |
| Medvedev VE et al.2014 · Zh Nevrol Psikhiatr Im S S Korsakova[A comparison of the anxiolytic effect and tolerability of selank and phenazepam in the treatment of anxiety disorders]. | Selank | Human, comparative clinical trial versus phenazepam, phobic-anxiety and somatoform disorders (n=60) | Not stated in the abstract | Not stated in the abstract | The authors report a pronounced anxiolytic and mild nootropic effect of Selank, lasting a week after the last dose, and a positive effect on quality of life. |
| Zozulia AA et al.2008 · Zh Nevrol Psikhiatr Im S S Korsakova[Efficacy and possible mechanisms of action of a new peptide anxiolytic selank in the therapy of generalized anxiety disorders and neurasthenia]. | Selank | Human, randomised controlled trial, generalised anxiety disorder and neurasthenia (n=62: 30 Selank, 32 medazepam) | Not stated in the abstract | Not stated in the abstract | Anxiolytic effects of Selank and medazepam were similar on Hamilton, Zung and CGI scales, and Selank also showed anti-asthenic and psychostimulant effects. Serum leu-enkephalin half-life, low at baseline, rose during Selank treatment, mostly in patients with GAD. |
| Uchakina ON et al.2008 · Zh Nevrol Psikhiatr Im S S Korsakova[Immunomodulatory effects of selank in patients with anxiety-asthenic disorders]. | Selank | Human, generalised anxiety disorder and neurasthenia, plus cell culture (patient peripheral blood) | 10⁻⁷ M in vitro; in-vivo dose not stated in the abstract | 14 days (in vivo) | In vitro, Selank completely suppressed IL-6 gene expression in blood cells from patients with depression but not healthy controls. In treated patients, the serum Th1/Th2 cytokine balance changed. |
| Sokolov OY et al.2002 · Bull Exp Biol Med · DOIEffects of Selank on behavioral reactions and activities of plasma enkephalin-degrading enzymes in mice with different phenotypes of emotional and stress reactions. | Selank | Mouse (BALB/c and C57Bl/6), open-field test and plasma enzyme assay | 100 mcg/kg | Not stated in the abstract | Selank had an anxiolytic effect in the open-field test and lengthened plasma leu-enkephalin half-life in BALB/c mice, with no effect on behaviour or enkephalinase activity in C57Bl/6 mice. |
| Liu R et al.2025 · Br J Pharmacol · DOISemax peptide targets the μ opioid receptor gene Oprm1 to promote deubiquitination and functional recovery after spinal cord injury in female mice. | Semax | Mouse (female C57BL/6), spinal cord injury at T9-T10; PC12 cell neuroinflammation model | Not stated in the abstract | Not stated in the abstract | Semax improved functional recovery scores and reduced lysosomal membrane permeabilisation-related pyroptosis and oxidative stress. The authors link the effect to the μ-opioid receptor and the deubiquitinase USP18. |
| Filippenkov IB et al.2020 · Genes (Basel) · DOINovel Insights into the Protective Properties of ACTH(4-7)PGP (Semax) Peptide at the Transcriptome Level Following Cerebral Ischaemia-Reperfusion in Rats. | Semax | Rat, transient middle cerebral artery occlusion (tMCAO) model | Not stated in the abstract | Brain tissue analysed 24 h after tMCAO | RNA-Seq found 394 differentially expressed genes with Semax versus saline. Semax suppressed inflammation-related genes and activated neurotransmission-related genes, the reverse of the pattern seen with ischaemia-reperfusion alone. |
| Gusev EI et al.2018 · Zh Nevrol Psikhiatr Im S S Korsakova · DOI[The efficacy of semax in the tretament of patients at different stages of ischemic stroke]. | Semax | Human, controlled clinical study, ischaemic stroke rehabilitation (n=110) | 6000 mcg/day | Two 10-day courses with a 20-day interval; patients followed for about 5 months | Semax raised plasma BDNF, which stayed high through the study, regardless of when rehabilitation started. Semax and high BDNF were associated with faster improvement and a better final Barthel index score. |
| Lebedeva IS et al.2018 · Bull Exp Biol Med · DOIEffects of Semax on the Default Mode Network of the Brain. | Semax | Human, placebo-controlled resting-state fMRI study in healthy volunteers (n=24: 14 Semax, 10 placebo) | Intranasal 1% Semax (volume not stated in the abstract) | Single administration; scans before and 5 and 20 min after | The Semax group showed a greater volume of the rostral (medial frontal cortex) subcomponent of the default mode network than the placebo group. |
| Shadrina M et al.2010 · J Mol Neurosci · DOIComparison of the temporary dynamics of NGF and BDNF gene expression in rat hippocampus, frontal cortex, and retina under Semax action. | Semax | Rat (male Wistar), gene expression in hippocampus, frontal cortex and retina | Not stated in the abstract | Tissue sampled from 20 min to 24 h after administration | NGF and BDNF expression moved in different directions by tissue: both fell in the hippocampus and retina at 20 min and rose in the frontal cortex, and retinal BDNF rose significantly by 90 min. |
| Gusev EI et al.2005 · Zh Nevrol Psikhiatr Im S S Korsakova[Semax in prevention of disease progress and development of exacerbations in patients with cerebrovascular insufficiency]. | Semax | Human, comparative study, cerebrovascular insufficiency (n=187) | Not stated in the abstract | Not stated in the abstract | Semax was associated with clinical improvement, stabilisation of disease progress and a reduced risk of stroke and transient ischaemic attack. The authors report a minor percentage of side effects and good tolerability, including in older patients. |
| Ivanikov IO et al.2002 · Bull Exp Biol Med · DOITherapy of peptic ulcer with semax peptide. | Semax | Human, controlled clinical study, refractory peptic ulcer (n not stated in the abstract) | Intranasal 1% solution, 2–4 drops three times a day, alongside omeprazole, De-Nol and Solcoseryl | 10 days; healing assessed on day 14 | Ulcer healing on day 14 was seen in 89.5% of patients given intranasal Semax versus 30.8% of controls. The authors call for further clinical studies. |
| Gusev EI et al.1997 · Zh Nevrol Psikhiatr Im S S Korsakova[Effectiveness of semax in acute period of hemispheric ischemic stroke (a clinical and electrophysiological study)]. | Semax | Human, controlled clinical trial, acute hemispheric ischaemic stroke (n=30 Semax, 80 conventional-therapy controls) | 12 mg/day (moderate stroke) and 18 mg/day (severe stroke) were reported as the most effective daily doses | 5- and 10-day courses | Adding Semax to standard intensive therapy had some influence on the rate of recovery of neurological function, particularly motor deficits, assessed with clinical scales, EEG mapping and somatosensory evoked potentials. |
| Panikratova YR et al.2020 · Dokl Biol Sci · DOIFunctional Connectomic Approach to Studying Selank and Semax Effects. | Semax + Selank | Human, placebo-controlled resting-state fMRI study in healthy participants (n=52); separate Semax, Selank and placebo groups | Not stated in the abstract | Single administration; scans before and 5 and 20 min after | Differences were found in connectivity between the right amygdala and the right temporal cortex, with both general and specific effects of Selank and Semax. Each participant received one peptide or placebo, not both. |
| Gusev EI et al.2018 · Zh Nevrol Psikhiatr Im S S Korsakova · DOI[The efficacy of semax in the tretament of patients at different stages of ischemic stroke]. | Semax + Selank | Human, controlled clinical study, ischaemic stroke rehabilitation (n=110) | 6000 mcg/day | Two 10-day courses with a 20-day interval | Semax raised plasma BDNF, which stayed high through the study, regardless of when rehabilitation started. Semax and high BDNF were associated with faster improvement and a better final Barthel index score. |
| Lebedeva IS et al.2018 · Bull Exp Biol Med · DOIEffects of Semax on the Default Mode Network of the Brain. | Semax + Selank | Human, placebo-controlled resting-state fMRI study in healthy volunteers (n=24: 14 Semax, 10 placebo) | Intranasal 1% Semax (volume not stated in the abstract) | Single administration; scans before and 5 and 20 min after | The Semax group showed a greater volume of the rostral (medial frontal cortex) subcomponent of the default mode network than the placebo group. |
| Medvedev VE et al.2015 · Zh Nevrol Psikhiatr Im S S Korsakova · DOI[Optimization of the treatment of anxiety disorders with selank]. | Semax + Selank | Human, randomised controlled trial, anxiety disorders (n=70: 30 phenazepam alone, 40 Selank plus phenazepam) | Not stated in the abstract | Not stated in the abstract | Adding Selank brought on the effect of phenazepam earlier on the HDRS and reduced phenazepam side effects such as attention and memory impairment, sedation and asthenia. Quality of life on the SF-36 improved. |
| Zozulia AA et al.2008 · Zh Nevrol Psikhiatr Im S S Korsakova[Efficacy and possible mechanisms of action of a new peptide anxiolytic selank in the therapy of generalized anxiety disorders and neurasthenia]. | Semax + Selank | Human, randomised controlled trial, generalised anxiety disorder and neurasthenia (n=62: 30 Selank, 32 medazepam) | Not stated in the abstract | Not stated in the abstract | Anxiolytic effects of Selank and medazepam were similar on Hamilton, Zung and CGI scales, and Selank also showed anti-asthenic and psychostimulant effects. Serum leu-enkephalin half-life, low at baseline, rose during Selank treatment, mostly in patients with GAD. |
| Sokolov OY et al.2002 · Bull Exp Biol Med · DOIEffects of Selank on behavioral reactions and activities of plasma enkephalin-degrading enzymes in mice with different phenotypes of emotional and stress reactions. | Semax + Selank | Mouse (BALB/c and C57Bl/6), open-field test and plasma enzyme assay | 100 mcg/kg | Not stated in the abstract | Selank had an anxiolytic effect in the open-field test and lengthened plasma leu-enkephalin half-life in BALB/c mice, with no effect on behaviour or enkephalinase activity in C57Bl/6 mice. |
| Kost NV et al.2001 · Bioorg Khim · DOI[Semax and selank inhibit the enkephalin-degrading enzymes from human serum]]. | Semax + Selank | Enzyme assay in vitro (enkephalin-degrading enzymes from human serum); Semax and Selank tested separately | Dose-dependent; IC50 10 µM for Semax and 20 µM for Selank | Not applicable (enzyme assay) | Both heptapeptides inhibited the enkephalin-degrading enzymes of human serum more strongly than puromycin (IC50 10 mM) and bacitracin. Their pentapeptide fragments also inhibited the enzymes; tri-, tetra- and hexapeptide fragments did not. |
| Gusev EI et al.1997 · Zh Nevrol Psikhiatr Im S S Korsakova[Effectiveness of semax in acute period of hemispheric ischemic stroke (a clinical and electrophysiological study)]. | Semax + Selank | Human, controlled clinical trial, acute hemispheric ischaemic stroke (n=30 Semax, 80 conventional-therapy controls) | 12 mg/day (moderate stroke) and 18 mg/day (severe stroke) were reported as the most effective daily doses | 5- and 10-day courses | Adding Semax to standard intensive therapy had some influence on the rate of recovery of neurological function, particularly motor deficits, assessed with clinical scales, EEG mapping and somatosensory evoked potentials. |
| Okda HE et al.2026 · Int J Biol Macromol · DOIChemical optimization of the exercise mimetic SLU-PP-332 enables insight into estrogen-related receptor signaling. | SLU-PP-332 | Cell culture, cell-based functional assays with computational modelling (structure-activity study) | Not stated in the abstract | Not stated in the abstract | The first full structure-activity analysis of the SLU-PP-332 scaffold identified the structural features that control ERRα and ERRγ agonism. Several analogues matched it with better ligand efficiency, solubility or metabolic stability, and SLU-PP-332 remained a benchmark for ERR activation. |
| Avliyakulov NK et al.2026 · Drug Test Anal · DOIAnalysis and Identification of In Vitro Metabolites of Exercise Mimetic SLU-PP-332 ERRα/β/γ Agonist for Doping-Control Purposes. | SLU-PP-332 | In vitro, pooled human liver S9 fractions (metabolite identification) | Not stated in the abstract | Not stated in the abstract | 22 Phase I and II metabolites were identified by LC-MS/HRMS, including hydroxylated, glucuronidated and sulfated forms. Eight of them were the most abundant and potentially useful for doping control. |
| Möller T et al.2026 · Rapid Commun Mass Spectrom · DOIIn Vitro Metabolism and Analytical Characterization of SLU-PP-332 and SLU-PP-915: Novel Pan-ERR Agonists With Doping Potential. | SLU-PP-332 | In vitro, human liver S9 fraction and human liver microsomes (analytical characterisation) | Not stated in the abstract | Not stated in the abstract | Nine metabolites were identified for SLU-PP-332: six Phase I metabolites and three Phase II conjugates. The authors describe the data as a basis for detecting its misuse as a performance-enhancing substance. |
| Billon C et al.2024 · J Pharmacol Exp Ther · DOIA Synthetic ERR Agonist Alleviates Metabolic Syndrome. | SLU-PP-332 | Mouse, diet-induced obese and ob/ob models of obesity and metabolic syndrome | Not stated in the abstract | Not stated in the abstract | SLU-PP-332 increased energy expenditure and fatty acid oxidation and decreased fat mass accumulation. It reduced obesity and improved insulin sensitivity in the metabolic syndrome models. |
| Xu W et al.2024 · Circulation · DOINovel Pan-ERR Agonists Ameliorate Heart Failure Through Enhancing Cardiac Fatty Acid Metabolism and Mitochondrial Function. | SLU-PP-332 | Mouse, pressure overload-induced heart failure; cardiomyocyte cell work in vitro | Not stated in the abstract | 6-week pressure overload (treatment length not stated in the abstract) | SLU-PP-332 and SLU-PP-915 improved ejection fraction, reduced fibrosis and increased survival without affecting cardiac hypertrophy. They activated fatty acid and mitochondrial genes, and genetic dependency experiments showed ERRγ as the main mediator. |
| Vieira Neto E et al.2026 · J Inherit Metab Dis · DOIElamipretide Improves Mitochondrial Function in Mitochondrial Trifunctional Protein-Deficient Mice and Human Fibroblasts. | SS-31 | Mouse, βTFP-deficient (mitochondrial trifunctional protein deficiency); patient-derived fibroblasts | Delivered by osmotic minipump; amount not stated in the abstract | Not stated in the abstract | Treated βTFP-deficient mice showed better exercise endurance but no change in cold tolerance, and liver mitochondria had improved FAO-ETC enzyme activity. Cardiolipin content and composition did not change. |
| Xie M et al.2026 · Lung · DOIMechanisms of Anti-Oxidants, N-Acetylcysteine and Elamipretide (SS-31), on Ozone-Induced Airway Hyperresponsiveness and Mucus Hypersecretion. | SS-31 | Mouse, ozone-induced airway injury (C57BL/6J); BEAS-2B airway cells | Intraperitoneal, 1 h before ozone exposure; amount not stated in the abstract | Single ozone exposure | SS-31 and N-acetylcysteine comparably reduced airway hyperresponsiveness, inflammatory cell influx and mucus hypersecretion. Both lowered ROS and malondialdehyde and improved SOD activity and GSH/GSSG. |
| Karaa A et al.2024 · Orphanet J Rare Dis · DOIGenotype-specific effects of elamipretide in patients with primary mitochondrial myopathy: a post hoc analysis of the MMPOWER-3 trial. | SS-31 | Human, post hoc analysis of the MMPOWER-3 randomised trial by genotype | Not stated in the abstract (MMPOWER-3 treatment arms) | 24 weeks | Patients with mtDNA replisome variants improved 25.2 m on the 6-minute walk test versus 2.0 m on placebo (p = 0.06). Within that group, those with CPEO improved 37.3 m versus -8.0 m (p = 0.0024). |
| Thompson WR et al.2024 · Genet Med · DOILong-term efficacy and safety of elamipretide in patients with Barth syndrome: 168-week open-label extension results of TAZPOWER. | SS-31 | Human, open-label extension of the TAZPOWER randomised trial, Barth syndrome (n=10 entered, 8 reached week 168) | 40 mg subcutaneous daily | 168-week open-label extension after a 28-week randomised phase | The 6-minute walk test improved at every time point, by a cumulative 96.1 m at week 168 (P = .003), and fatigue scores stayed below baseline. Injection-site reactions were the most common adverse events. |
| Karaa A et al.2023 · Neurology · DOIEfficacy and Safety of Elamipretide in Individuals With Primary Mitochondrial Myopathy: The MMPOWER-3 Randomized Clinical Trial. | SS-31 | Human, phase 3 randomised double-blind placebo-controlled trial, primary mitochondrial myopathy (n=218) | 40 mg/day subcutaneous | 24 weeks | The trial did not meet its primary endpoints: the difference from placebo was -3.2 m on the 6-minute walk test (p = 0.69) and -0.07 on total fatigue (p = 0.37). Elamipretide was well tolerated, with most adverse events mild to moderate. |
| Hornby B et al.2022 · Orphanet J Rare Dis · DOINatural history comparison study to assess the efficacy of elamipretide in patients with Barth syndrome. | SS-31 | Human, retrospective natural history comparison, Barth syndrome (8 treated patients vs 19 untreated controls) | 40 mg daily | Compared at weeks 64 and 76 | The 6-minute walk test favoured elamipretide by 79.7 m at week 64 and 91.0 m at week 76, with gains in handheld muscle strength. Left ventricular stroke volume rose in treated patients and fell in the untreated controls. |
| Tse BC et al.2020 · Exp Eye Res · DOIMitochondrial targeted therapy with elamipretide (MTP-131) as an adjunct to tumor necrosis factor inhibition for traumatic optic neuropathy in the acute setting. | SS-31 | Mouse, sonication-induced traumatic optic neuropathy | Intravitreal and/or subcutaneous MTP-131; amount not stated in the abstract | Not stated in the abstract | Subcutaneous MTP-131 alone raised retinal ganglion cell survival by 17% over controls (p < 0.01). Combining it with etanercept gave no synergistic effect. |
| Maar K et al.2025 · Int J Mol Sci · DOIThymosin Beta-4 Modulates Cardiac Remodeling by Regulating ROCK1 Expression in Adult Mammals. | TB-500 | Mouse, permanent coronary ligation (heart attack) model; human cardiac cells | Systemic TB4 injection; amount not stated in the abstract | Not stated in the abstract | TB4 raised miR139-5p expression and modulated ROCK1 protein levels in mouse hearts and human cardiac cells, and may reverse or inhibit fibroblast-to-myofibroblast transformation. |
| Li Y et al.2025 · J Allergy Clin Immunol · DOIPlasmacytoid dendritic cells alleviate allergic asthma via airway epithelial cell-dependent thymosin β4 expression. | TB-500 | Mouse, house dust mite allergic asthma model (BDCA2-DTR mice); cell experiments | Tβ4 supplementation; amount not stated in the abstract | Not stated in the abstract | Tβ4 supplementation reversed the worsened asthma phenotype in mice depleted of plasmacytoid dendritic cells. Tβ4 inhibited IL-4/IL-13-induced JAK1/STAT6 signalling and CCL2 expression in macrophages. Serum Tβ4 was lower in mice and humans with ongoing allergic asthma. |
| Sun YS et al.2025 · World J Gastroenterol · DOIThymosin β4 released by mast cells under stress conditions impairs intestinal epithelial barrier via IL22RA1/JAK1/STAT3 signaling in irritable bowel syndrome. | TB-500 | Human colonic mucus (IBS patients); mouse and rat (Tβ4-deficient) models | Not stated in the abstract | Not stated in the abstract | Tβ4 treatment of mice reduced tight junction proteins in the gut lining, and Tβ4 released from mast cells under stress disrupted the intestinal epithelial barrier. Tβ4-deficient rats were resistant to stress-induced barrier disturbance. |
| Jin Z et al.2025 · Cell Signal · DOIMechanistic study of the Tβ4/SLC7A11 signaling pathway regulating breast cancer evolution. | TB-500 | Human breast cancer tissue and cell lines; mouse (in vivo) | Not stated in the abstract | Not stated in the abstract | Tβ4 was upregulated in breast cancer tissue, and high expression correlated with poor clinical outcomes. Tβ4 promoted cancer cell proliferation, migration and angiogenesis by regulating SLC7A11 and inhibiting ferroptosis. |
| Bako P et al.2023 · Int Immunopharmacol · DOIThymosin beta-4 - A potential tool in healing middle ear lesions in adult mammals. | TB-500 | Mouse tympanic membrane (eardrum) explants, ex vivo and on collagen gels | Not stated in the abstract | Not stated in the abstract | TB4 affected the migration and proliferation of epidermal and epithelial cells of the tympanic membrane in vitro, most likely acting on local epidermal progenitor cells. |
| Li H et al.2018 · J Gene Med · DOIThymosin β4 suppresses CCl4 -induced murine hepatic fibrosis by down-regulating transforming growth factor β receptor-II. | TB-500 | Mouse, CCl4-induced liver fibrosis model (gene delivery, not peptide); liver cells in vitro | Intraperitoneal adeno-associated virus encoding Tβ4 (AAV-Tβ4); amount not stated in the abstract | Not stated in the abstract | AAV-Tβ4 pre-treatment significantly reduced liver injury, collagen deposition, stellate cell activation and pro-fibrotic cytokines, partly by down-regulating TGF-β receptor II. |
| Drum CL et al.2017 · J Am Heart Assoc · DOIThymosin Beta-4 Is Elevated in Women With Heart Failure With Preserved Ejection Fraction. | TB-500 | Human, observational biomarker study (HFpEF n=219, HFrEF n=219, controls n=219); circulating TB4 measured, none given | None given (the body's own plasma TB4 was measured) | Not stated in the abstract | Plasma TB4 was higher in HFpEF than in controls (1401 vs 985 ng/mL, P<0.001), an effect seen in women only. In women with heart failure, elevated TB4 carried a higher hazard ratio for all-cause death (1.668, P=0.036). |
| Ellis RJ et al.2025 · J Infect Dis · DOIEffects of Tesamorelin on Neurocognitive Impairment in Persons With HIV and Abdominal Obesity. | Tesamorelin | Human, randomised, open-label phase 2 trial vs standard of care, people with HIV, abdominal obesity and neurocognitive impairment (n=73) | 2 mg s.c. daily | 6 months | Waist circumference fell more with tesamorelin (median difference −2.7 cm; P = .015), but the change in neurocognitive performance did not differ between groups (P = .673). |
| Stanley TL et al.2019 · Lancet HIV · DOIEffects of tesamorelin on non-alcoholic fatty liver disease in HIV: a randomised, double-blind, multicentre trial. | Tesamorelin | Human, randomised, double-blind, multicentre trial, people with HIV and non-alcoholic fatty liver disease (n=61) | 2 mg once daily | 12 months, then a 6-month open-label phase | Hepatic fat fraction fell by an absolute 4.1% more than with placebo (p = 0.018), a 37% relative reduction. After 12 months 35% on tesamorelin and 4% on placebo had a fat fraction under 5%; fasting glucose and HbA1c did not differ between groups. |
| Adrian S et al.2019 · J Frailty Aging · DOIThe Growth Hormone Releasing Hormone Analogue, Tesamorelin, Decreases Muscle Fat and Increases Muscle Area in Adults with HIV. | Tesamorelin | Human, secondary analysis of two randomised trials, people with HIV and abdominal obesity (193 tesamorelin responders, 148 placebo) | Not stated in the abstract | 26 weeks | Among responders, tesamorelin was associated with significantly greater increases in the density of four trunk muscle groups and in lean muscle area (all p < 0.005) compared with placebo. |
| Clemmons DR et al.2017 · PLoS One · DOISafety and metabolic effects of tesamorelin, a growth hormone-releasing factor analogue, in patients with type 2 diabetes: A randomized, placebo-controlled trial. | Tesamorelin | Human, randomised, placebo-controlled trial, patients with type 2 diabetes (n=53) | 1 or 2 mg | 12 weeks | There were no significant differences between groups in relative insulin response, fasting glucose, HbA1c or overall diabetes control. Total and non-HDL cholesterol fell significantly in the 2 mg group. |
| Stanley TL et al.2014 · JAMA · DOIEffect of tesamorelin on visceral fat and liver fat in HIV-infected patients with abdominal fat accumulation: a randomized clinical trial. | Tesamorelin | Human, randomised, double-blind, placebo-controlled trial, people with HIV and abdominal fat accumulation (n=50) | 2 mg s.c. once daily | 6 months | Visceral fat changed by −34 cm² with tesamorelin vs +8 cm² with placebo (P = .005), and liver fat fell by a median 2.0% vs a rise of 0.9% (P = .003). Fasting glucose rose at 2 weeks, but glucose changes over 6 months were not significant. |
| Makimura H et al.2014 · J Clin Endocrinol Metab · DOIThe effects of tesamorelin on phosphocreatine recovery in obese subjects with reduced GH. | Tesamorelin | Human, randomised, double-blind, placebo-controlled trial, obese adults with reduced GH secretion (n=39) | Not stated in the abstract | 12 months | IGF-I rose by 102.9 μg/L with tesamorelin vs 22.8 μg/L with placebo (P = .02). Increases in IGF-I correlated with faster phosphocreatine recovery after exercise, a marker the authors link to mitochondrial function. |
| Falutz J et al.2010 · J Acquir Immune Defic Syndr · DOIEffects of tesamorelin, a growth hormone-releasing factor, in HIV-infected patients with abdominal fat accumulation: a randomized placebo-controlled trial with a safety extension. | Tesamorelin | Human, randomised, double-blind, placebo-controlled trial with a safety extension, people with HIV and excess abdominal fat (n=404) | 2 mg s.c. once daily | 6 months, then a 6-month rerandomised extension | Visceral fat fell by 10.9% with tesamorelin vs 0.6% with placebo over 6 months (P < 0.0001), and by about 18% in those continuing for 12 months. IGF-I rose with no change in glucose parameters; the gains were rapidly lost in those switched to placebo. |
| Falutz J et al.2008 · AIDS · DOILong-term safety and effects of tesamorelin, a growth hormone-releasing factor analogue, in HIV patients with abdominal fat accumulation. | Tesamorelin | Human, randomised, placebo-controlled trial and extension, people with HIV and central fat accumulation (n=410) | 2 mg s.c. once daily | 26 weeks, then a 26-week extension (52 weeks total) | The drop in visceral fat was sustained at 18% over 52 weeks, with triglycerides down 51 mg/dl (both P < 0.001 vs baseline). Adverse events were comparable between phases and glucose changes were not clinically significant; visceral fat reaccumulated after stopping. |
| Wu J et al.2025 · BMJ · DOIThe efficacy and safety of thymosin α1 for sepsis (TESTS): multicentre, double blinded, randomised, placebo controlled, phase 3 trial. | Thymosin Alpha-1 | Human, multicentre double-blind randomised placebo-controlled phase 3 trial, adults with sepsis (n=1106 randomised; 1089 analysed) | Not stated in the abstract (subcutaneous injection) | Every 12 hours for seven days | 28-day all-cause mortality was 23.4% with thymosin α1 and 24.1% with placebo (hazard ratio 0.99, P=0.93). No secondary or safety outcome differed significantly; subgroup analyses suggested a possible difference by age and diabetes status. |
| Wu X et al.2018 · Expert Opin Biol Ther · DOICombination of entecavir with thymosin alpha-1 in HBV-related compensated cirrhosis: a prospective multicenter randomized open-label study. | Thymosin Alpha-1 | Human, multicentre randomised open-label trial, HBV-related compensated cirrhosis (n=690) | Not stated in the abstract (added to entecavir) | 52 weeks, after 26 weeks of entecavir; median follow-up 38.2 months | Cumulative incidence of liver decompensation, liver cancer (HCC) or death was similar between groups. HCC incidence during combination treatment was 1.7% versus 2.1% with entecavir alone; both therapies were well tolerated. |
| Maio M et al.2010 · J Clin Oncol · DOILarge randomized study of thymosin alpha 1, interferon alfa, or both in combination with dacarbazine in patients with metastatic melanoma. | Thymosin Alpha-1 | Human, randomised trial with five arms, metastatic melanoma (n=488) | 1.6, 3.2 or 6.4 mg, combined with dacarbazine with or without interferon alfa | Primary end point at 12 months; observed for up to 24 months | The 3.2 mg arms had 10 and 12 tumour responses versus four in the control group. Median overall survival was 9.4 versus 6.6 months (hazard ratio 0.80, P=.08), and adding Tα1 did not add toxicity. |
| You J et al.2006 · World J Gastroenterol · DOIEfficacy of thymosin alpha-1 and interferon alpha in treatment of chronic viral hepatitis B: a randomized controlled study. | Thymosin Alpha-1 | Human, randomised controlled trial versus interferon alpha, with a historical control group, HBeAg-positive chronic hepatitis B (n=62; 30 historical controls) | 1.6 mg subcutaneously | Twice a week for six months, then six months of follow-up | Complete response at the end of follow-up was 48.3% (14 of 29) with Tα1 versus 27.3% with interferon alpha, a difference that was not statistically significant (P>0.05); against historical controls it was significantly higher. No side effects appeared in the Tα1 group. |
| Saruc M et al.2003 · J Pharm Sci · DOILong-term outcomes of thymosin-alpha 1 and interferon alpha-2b combination therapy in patients with hepatitis B e antigen (HBeAg) negative chronic hepatitis B. | Thymosin Alpha-1 | Human, non-randomised comparative study, HBeAg-negative chronic hepatitis B (n=52; 27 in the Tα1 group) | 1.6 mg subcutaneously, twice a week, combined with interferon alpha-2b | 26 weeks of combination, then 26 weeks of interferon alone; follow-up to 18 months after treatment | Sustained response was 74% in the Tα1 plus interferon group versus 40% and 53.3% in the comparison groups (p = 0.13). At 18 months after treatment, 71.4% of the Tα1 group kept their response versus 10% and 20% (p = 0.0003). |
| Jastreboff AM et al.2025 · N Engl J Med · DOITirzepatide for Obesity Treatment and Diabetes Prevention. | Tirzepatide | Human, phase 3 randomised controlled trial, obesity with prediabetes (n=1032 of 2539) — SURMOUNT-1, 3-year analysis | 5, 10 or 15 mg once weekly, vs placebo | 176 weeks, then 17 weeks off treatment | Weight change at 176 weeks was −12.3% to −19.7% vs −1.3% with placebo, and type 2 diabetes was diagnosed in 1.3% vs 13.3% (hazard ratio 0.07). No new safety signals were identified. |
| Packer M et al.2025 · N Engl J Med · DOITirzepatide for Heart Failure with Preserved Ejection Fraction and Obesity. | Tirzepatide | Human, randomised controlled trial in heart failure with preserved ejection fraction and obesity (n=731) — SUMMIT | Up to 15 mg once weekly, subcutaneous, vs placebo | At least 52 weeks (median follow-up 104 weeks) | Cardiovascular death or worsening heart failure occurred in 9.9% on tirzepatide vs 15.3% on placebo (hazard ratio 0.62). Adverse events leading to discontinuation were 6.3% vs 1.4%. |
| Aronne LJ et al.2024 · JAMA · DOIContinued Treatment With Tirzepatide for Maintenance of Weight Reduction in Adults With Obesity: The SURMOUNT-4 Randomized Clinical Trial. | Tirzepatide | Human, phase 3 randomised withdrawal trial in obesity, without diabetes (n=670 randomised) — SURMOUNT-4 | Maximum tolerated dose of 10 or 15 mg once weekly, subcutaneous, then continued or switched to placebo | 36-week open-label lead-in plus 52 weeks double-blind | After a mean 20.9% reduction in the lead-in, weight changed by −5.5% with continued tirzepatide vs +14.0% after switching to placebo from week 36 to 88. Withdrawal led to substantial regain of lost weight. |
| Malhotra A et al.2024 · N Engl J Med · DOITirzepatide for the Treatment of Obstructive Sleep Apnea and Obesity. | Tirzepatide | Human, two phase 3 randomised controlled trials in moderate-to-severe obstructive sleep apnoea with obesity — SURMOUNT-OSA | Maximum tolerated dose of 10 or 15 mg, vs placebo | 52 weeks | The apnoea-hypopnoea index fell by 25.3 and 29.3 events per hour with tirzepatide vs 5.3 and 5.5 with placebo in the two trials. Adverse events were mostly gastrointestinal and mild to moderate. |
| Loomba R et al.2024 · N Engl J Med · DOITirzepatide for Metabolic Dysfunction-Associated Steatohepatitis with Liver Fibrosis. | Tirzepatide | Human, phase 2 randomised controlled trial in biopsy-confirmed MASH with F2–F3 fibrosis (n=190) — SYNERGY-NASH | 5, 10 or 15 mg once weekly, subcutaneous, vs placebo | 52 weeks | Resolution of MASH without worsening of fibrosis was seen in 44%, 56% and 62% on 5, 10 and 15 mg vs 10% on placebo. The authors state that larger and longer trials are needed. |
| Jastreboff AM et al.2022 · N Engl J Med · DOITirzepatide Once Weekly for the Treatment of Obesity. | Tirzepatide | Human, phase 3 randomised controlled trial in adults with obesity, without diabetes (n=2539) — SURMOUNT-1 | 5, 10 or 15 mg once weekly, subcutaneous, vs placebo | 72 weeks, including a 20-week dose-escalation period | Mean weight change at week 72 was −15.0% (5 mg), −19.5% (10 mg) and −20.9% (15 mg) vs −3.1% with placebo. Adverse events, mostly gastrointestinal, led to discontinuation in 4.3% to 7.1% on tirzepatide vs 2.6% on placebo. |
| Rosenstock J et al.2021 · Lancet · DOIEfficacy and safety of a novel dual GIP and GLP-1 receptor agonist tirzepatide in patients with type 2 diabetes (SURPASS-1): a double-blind, randomised, phase 3 trial. | Tirzepatide | Human, phase 3 randomised controlled trial in type 2 diabetes on diet and exercise alone (n=478) — SURPASS-1 | 5, 10 or 15 mg once weekly, vs placebo | 40 weeks | HbA1c fell by 1.87%, 1.89% and 2.07% with 5, 10 and 15 mg vs a rise of 0.04% with placebo. An HbA1c below 7.0% was reached by 87–92% on tirzepatide vs 20% on placebo. |
| Frías JP et al.2021 · N Engl J Med · DOITirzepatide versus Semaglutide Once Weekly in Patients with Type 2 Diabetes. | Tirzepatide | Human, phase 3 open-label randomised trial vs semaglutide 1 mg in type 2 diabetes (n=1879) — SURPASS-2 | 5, 10 or 15 mg once weekly, vs semaglutide 1 mg once weekly | 40 weeks | HbA1c fell by 2.01 to 2.30 percentage points with tirzepatide vs 1.86 with semaglutide, and weight loss was 1.9 to 5.5 kg greater. Nausea was reported by 17–22% on tirzepatide and 18% on semaglutide. |
| Lee E et al.2025 · Altern Ther Health MedSafety of Intravenous Infusion of BPC157 in Humans: A Pilot Study. | Wolverine blend (BPC-157 + TB-500) | Human, safety pilot (n=2 adults), private clinic | 10 mg in 250 cc normal saline over one hour on day 1, then 20 mg on day 2 (intravenous) | 3 days | The infusions produced no measurable effects on the tested heart, liver, kidney and thyroid biomarkers or blood glucose, and no side effects were reported. |
| Maar K et al.2025 · Int J Mol Sci · DOIThymosin Beta-4 Modulates Cardiac Remodeling by Regulating ROCK1 Expression in Adult Mammals. | Wolverine blend (BPC-157 + TB-500) | Mouse, permanent coronary ligation (heart attack) model; human cardiac cells | Systemic TB4 injection; amount not stated in the abstract | Not stated in the abstract | TB4 raised miR139-5p expression and modulated ROCK1 protein levels in mouse hearts and human cardiac cells, and may reverse or inhibit fibroblast-to-myofibroblast transformation. |
| Li Y et al.2025 · J Allergy Clin Immunol · DOIPlasmacytoid dendritic cells alleviate allergic asthma via airway epithelial cell-dependent thymosin β4 expression. | Wolverine blend (BPC-157 + TB-500) | Mouse, house dust mite allergic asthma model (BDCA2-DTR mice); cell experiments | Tβ4 supplementation; amount not stated in the abstract | Not stated in the abstract | Tβ4 supplementation reversed the worsened asthma phenotype in mice depleted of plasmacytoid dendritic cells, and Tβ4 inhibited IL-4/IL-13-induced JAK1/STAT6 signalling in macrophages. |
| Sun YS et al.2025 · World J Gastroenterol · DOIThymosin β4 released by mast cells under stress conditions impairs intestinal epithelial barrier via IL22RA1/JAK1/STAT3 signaling in irritable bowel syndrome. | Wolverine blend (BPC-157 + TB-500) | Human colonic mucus (IBS patients); mouse and rat (Tβ4-deficient) models | Not stated in the abstract | Not stated in the abstract | Tβ4 treatment of mice reduced tight junction proteins in the gut lining, and Tβ4 released from mast cells under stress disrupted the intestinal epithelial barrier. |
| Lee E et al.2024 · Altern Ther Health MedEffect of BPC-157 on Symptoms in Patients with Interstitial Cystitis: A Pilot Study. | Wolverine blend (BPC-157 + TB-500) | Human, uncontrolled pilot study (n=12 women with interstitial cystitis), private clinic | 10 mg total, given by injection around the inflamed area of the bladder during cystoscopy | Single procedure; follow-up period not stated in the abstract | Ten of 12 patients reported complete resolution of symptoms and 2 of 12 rated their success at 80%. No adverse events were reported. The study had no control group. |
| Lee E et al.2021 · Altern Ther Health MedIntra-Articular Injection of BPC 157 for Multiple Types of Knee Pain. | Wolverine blend (BPC-157 + TB-500) | Human, retrospective chart review with phone survey (n=16, knee pain); 4 of the 16 received BPC-157 and TB4 | Intra-articular BPC-157 alone (n=12) or BPC-157 and TB4 as two peptide injections (n=4); amounts not stated in the abstract | Most patients surveyed 6 months to 1 year after the injection | Eleven of 12 given BPC-157 alone reported significant improvement in knee pain. Of the 4 given both peptides, 75% reported significant improvement and 25% had no relief. No specific tools were used to measure function or quality of life, and there was no control group. |
| Perovic D et al.2019 · J Orthop Surg Res · DOIStable gastric pentadecapeptide BPC 157 can improve the healing course of spinal cord injury and lead to functional recovery in rats. | Wolverine blend (BPC-157 + TB-500) | Rat, spinal cord compression injury model | 200 or 2 μg/kg, one intraperitoneal injection 10 min after injury | Assessed at 1, 4, 7, 15, 30, 90, 180 and 360 days | Injured rats given BPC-157 showed better tail motor function, no autotomy and resolved spasticity by day 15, with less axon loss, oedema and motoneuron loss on microscopy. |
| Li H et al.2018 · J Gene Med · DOIThymosin β4 suppresses CCl4 -induced murine hepatic fibrosis by down-regulating transforming growth factor β receptor-II. | Wolverine blend (BPC-157 + TB-500) | Mouse, CCl4-induced liver fibrosis model (gene delivery, not peptide); liver cells in vitro | Intraperitoneal adeno-associated virus encoding Tβ4 (AAV-Tβ4); amount not stated in the abstract | Not stated in the abstract | AAV-Tβ4 pre-treatment significantly reduced liver injury, collagen deposition, stellate cell activation and pro-fibrotic cytokines. |