Compound Index

Triple agonist of the GIP, GLP-1, and glucagon receptors (investigational incretin/metabolic peptide)

Retatrutide is a single-molecule 'triple agonist' studied for chronic weight management and type 2 diabetes. In a published Phase 2 obesity trial it produced large dose-dependent weight reductions, and Phase 3 (TRIUMPH) trials are ongoing, with the first positive topline readout reported in late 2025. It remains experimental and is not authorized for clinical use.

Dual agonist of the GIP and GLP-1 receptors (incretin-based metabolic peptide)

Tirzepatide is an approved incretin therapy that combines GIP and GLP-1 receptor activity in a single molecule. Large randomized trials show substantial reductions in HbA1c and body weight, and a head-to-head trial (SURMOUNT-5) reported greater weight loss than semaglutide. It is a prescription medicine used under medical supervision.

Glucagon-like peptide-1 (GLP-1) receptor agonist

Semaglutide is an approved once-weekly injectable (and once-daily oral) GLP-1 therapy for type 2 diabetes and, at higher doses, for chronic weight management. Randomized trials demonstrate meaningful reductions in HbA1c and body weight, and the SELECT trial showed reduced cardiovascular events in people with overweight or obesity and established cardiovascular disease. It is a prescription medicine used under medical supervision.

Long-acting amylin (and calcitonin) receptor agonist / amylin analogue

Cagrilintide is an experimental amylin-based peptide developed to reduce appetite and body weight, studied both alone and combined with semaglutide (CagriSema). Phase 2 monotherapy data and Phase 3 CagriSema data (REDEFINE in obesity, REIMAGINE in type 2 diabetes) report substantial weight reductions. It remains investigational and is not authorized for clinical use.

Synthetic stable gastric pentadecapeptide (15-amino-acid partial sequence derived from a protein in human gastric juice)

BPC-157 is a synthetic pentadecapeptide based on a fragment of a protein found in gastric juice. The bulk of its evidence is preclinical (rodent and in-vitro), with only very limited, uncontrolled human data; no regulator has approved it for any indication.

Synthetic peptide fragment (Ac-LKKTETQ) corresponding to the actin-binding region of thymosin beta-4; note it is NOT the same molecule as full-length recombinant thymosin beta-4

TB-500 is a short synthetic peptide based on the actin-binding portion of thymosin beta-4. Preclinical studies suggest roles in wound healing, angiogenesis and reduced fibrosis, but robust human trials exist only for full-length thymosin beta-4 (RGN-259), a distinct molecule.

Copper-binding tripeptide (glycyl-L-histidyl-L-lysine complexed with Cu2+); endogenous matrikine; cosmetic ingredient name Copper Tripeptide-1

GHK is a tripeptide present in human plasma that declines with age and binds copper to form GHK-Cu. It has extensive mechanistic and preclinical support for skin regeneration and wound healing and is used topically in cosmetics, but rigorous large-scale clinical trials are limited.

Tripeptide (Lys-Pro-Val); C-terminal fragment of alpha-melanocyte-stimulating hormone (alpha-MSH); melanocortin-derived anti-inflammatory peptide

KPV is the C-terminal tripeptide of alpha-MSH that retains much of the parent hormone's anti-inflammatory activity while being more stable. Its evidence base is preclinical (cell and rodent inflammatory-disease models); it is unapproved and, in the US, has been the subject of FDA compounding review.

Growth hormone-releasing hormone (GHRH) analog

Originally developed by ConjuChem, CJC-1295 is a tetrasubstituted 29-amino-acid analog of GHRH(1-29); the DAC (Drug Affinity Complex) version binds serum albumin to extend its half-life to roughly 6-8 days. Available human evidence is limited to early-phase pharmacokinetic/pharmacodynamic data showing raised GH and IGF-1; no efficacy or long-term safety has been established.

Growth hormone secretagogue; ghrelin (GHS-R1a) receptor agonist (pentapeptide)

First described by Raun and colleagues at Novo Nordisk (1998) as 'the first selective growth hormone secretagogue' because it releases GH without meaningfully raising ACTH, cortisol or prolactin. Human evidence is confined to phase 1/2 studies and there is no approved therapeutic indication.

Mitochondrial-derived peptide (MDP); AMPK activator / exercise mimetic

Identified by Lee and colleagues (2015, Cell Metabolism) as a mitochondrial-to-nucleus signalling peptide regulating metabolism. It has been investigated for obesity, insulin resistance and age-related decline, but only in laboratory and animal models; it is not an approved drug or recognized therapy.

Modified C-terminal fragment of human growth hormone (tyrosine-modified hGH 176-191); lipolytic peptide

Developed by Metabolic Pharmaceuticals (Australia) with Monash University, AOD-9604 was designed to stimulate lipolysis and inhibit fat formation without the IGF-1, blood-glucose or growth effects of full-length human growth hormone. It was later promoted in some markets as a food/nutraceutical ingredient on the basis of self-affirmed GRAS safety data, but it has never been approved as a drug for obesity or any indication.

Synthetic pineal tetrapeptide bioregulator (Ala-Glu-Asp-Gly / AEDG); studied as a telomerase-related peptide

Epithalon was created at the St. Petersburg Institute of Bioregulation and Gerontology by the Khavinson group and has been investigated for effects on telomerase, melatonin/circadian rhythm and aging, mainly in cell cultures, rodents and small cohorts. Rigorous, independently replicated human trials are lacking, and it remains an unapproved research compound worldwide.

Melanocortin receptor agonist; synthetic cyclic analog of alpha-melanocyte-stimulating hormone (alpha-MSH)

Bremelanotide is a synthetic cyclic analog of alpha-MSH that non-selectively activates melanocortin receptors. FDA approval rested on the two phase-3 RECONNECT randomized, double-blind, placebo-controlled trials; commonly reported adverse effects include nausea, flushing, injection-site reactions and headache, and it can cause transient increases in blood pressure.

Synthetic tuftsin analog (heptapeptide, Thr-Lys-Pro-Arg-Pro-Gly-Pro); anxiolytic/nootropic neuropeptide

Selank was engineered as a more stable analog of tuftsin and studied primarily in Russia for generalized anxiety disorder and neurasthenia. Small Russian trials report anxiolytic effects broadly comparable to benzodiazepines such as medazepam with additional antiasthenic effects, but these studies are small and have not been independently replicated in large Western trials; it remains unapproved outside Russia/Ukraine.

Synthetic ACTH(4-10) analog (heptapeptide, Met-Glu-His-Phe-Pro-Gly-Pro); nootropic/neuroprotective neuropeptide

Semax was developed in Russia and is used there for indications including stroke, transient ischemic attack and cognitive/memory disorders; it was added to Russia's government-approved list of vital and essential drugs in December 2011. Outside Russia and some CIS countries it has not been evaluated, approved or marketed, and the Western-quality evidence base remains limited and largely preclinical.

Glucagon-like peptide-1 (GLP-1) receptor agonist (acylated GLP-1 analogue)

Liraglutide is an approved GLP-1 therapy used for type 2 diabetes (Victoza) and, at a higher dose, for chronic weight management (Saxenda). Randomized trials show meaningful reductions in HbA1c and body weight, and the LEADER cardiovascular outcomes trial demonstrated a reduction in major adverse cardiovascular events in people with type 2 diabetes at high cardiovascular risk. It is a prescription medicine used under medical supervision.

Long-acting glucagon-like peptide-1 (GLP-1) receptor agonist (GLP-1 analogue fused to a modified human IgG4 Fc fragment)

Dulaglutide is an approved once-weekly GLP-1 therapy for type 2 diabetes. It is a GLP-1 analogue fused to an antibody (IgG4 Fc) fragment, a design that extends its half-life. Randomized trials in the AWARD program show reductions in HbA1c and body weight, and the REWIND trial demonstrated a reduction in major adverse cardiovascular events in a broad type 2 diabetes population. It is not approved as a stand-alone weight-management medicine.

Glucagon-like peptide-1 (GLP-1) receptor agonist; synthetic exendin-4

Exenatide is an approved GLP-1 therapy for type 2 diabetes and was the first drug in its class. It is a synthetic form of exendin-4, a peptide originally identified in the saliva of the Gila monster, that shares partial sequence homology with human GLP-1. Immediate-release (Byetta) and once-weekly extended-release (Bydureon) formulations lower HbA1c and body weight; the EXSCEL cardiovascular outcomes trial found it did not increase cardiovascular risk. In recent years the originator has discontinued supply of some exenatide formulations in certain markets.

Dual agonist of the glucagon-like peptide-1 (GLP-1) and glucagon receptors (investigational metabolic peptide)

Survodutide is an experimental single-molecule dual agonist of the GLP-1 and glucagon receptors studied for chronic weight management and for MASH (formerly NASH). A published Phase 2 trial in MASH reported improvements in liver histology, and Phase 2 obesity data showed substantial weight reductions; a Phase 3 program (SYNCHRONIZE) is ongoing. It remains investigational and is not authorized for clinical use.

Dual agonist of the glucagon-like peptide-1 (GLP-1) and glucagon receptors; a synthetic oxyntomodulin analogue

Mazdutide is a dual agonist of the GLP-1 and glucagon receptors based on the gut hormone oxyntomodulin, developed mainly for the Chinese market by Innovent Biologics (in-licensed from Eli Lilly). Clinical trials, conducted largely in China, report dose-dependent reductions in body weight and blood glucose. China's National Medical Products Administration (NMPA) approved mazdutide in 2025, first for chronic weight management and subsequently for glycemic control in adults with type 2 diabetes. It is not approved by the FDA, EMA, or Australia's TGA, and in those jurisdictions it remains investigational.

Oral small-molecule (non-peptide) agonist of the glucagon-like peptide-1 (GLP-1) receptor

Orforglipron is an oral small-molecule GLP-1 receptor agonist that, unlike peptide GLP-1 drugs, can be taken as a daily tablet without strict food and water restrictions. Published Phase 2 trials in obesity and type 2 diabetes showed reductions in body weight and HbA1c, and the Phase 3 program (ATTAIN in obesity and ACHIEVE in type 2 diabetes) reported positive results. On the basis of the ATTAIN obesity program, the US FDA approved orforglipron (Foundayo) in April 2026 for chronic weight management. It is not yet approved for type 2 diabetes and is not yet authorized by the EMA or Australia's TGA.

Synthetic analogue of growth hormone-releasing hormone (GHRH); approved for HIV-associated lipodystrophy

Tesamorelin is an approved GHRH analogue used specifically to reduce excess visceral (abdominal) fat in adults with HIV-associated lipodystrophy. Its approval rested on two pivotal Phase 3 randomized trials, and it has since been studied for non-alcoholic fatty liver disease in people with HIV. It is not approved for general weight loss, bodybuilding, or anti-aging use, and its FDA-approved indication is narrow.

Synthetic analogue of growth hormone-releasing hormone comprising its first 29 amino acids (GHRH 1-29); formerly FDA-approved (Geref), later withdrawn from the US market

Sermorelin is a GHRH(1-29) analogue with a documented history as an approved medicine (Geref) used for diagnosis of growth hormone secretory capacity and treatment of growth hormone deficiency. The manufacturer discontinued and withdrew Geref from the US market around 2008 for commercial reasons; no FDA-approved sermorelin product is currently marketed, and it is now supplied primarily via compounding pharmacies, often promoted off-label for anti-aging and growth-hormone-related uses without support from large modern trials.

Synthetic growth hormone secretagogue; ghrelin receptor (GHS-R1a) agonist; growth hormone-releasing peptide (GHRP) hexapeptide

Hexarelin is a synthetic hexapeptide growth hormone secretagogue studied in the 1990s and 2000s for its ability to release growth hormone and for possible direct cardiovascular effects. Human evidence is limited to small pharmacology and early-phase studies; no regulator has approved it for any indication, and diminishing response with repeated dosing (tachyphylaxis) was noted during its development.

Synthetic growth hormone secretagogue; ghrelin receptor (GHS-R1a) agonist; growth hormone-releasing peptide (GHRP)

GHRP-2, also called pralmorelin, is a synthetic growth hormone secretagogue. In Japan it received approval as an injectable diagnostic agent to test pituitary growth hormone reserve, but it is not approved as a treatment in the United States, the EU or Australia. Human data outside its diagnostic use are limited to early-phase pharmacology studies.

Synthetic growth hormone secretagogue; ghrelin receptor (GHS-R1a) agonist; first-described growth hormone-releasing hexapeptide (His-D-Trp-Ala-Trp-D-Phe-Lys)

GHRP-6 is a synthetic hexapeptide that helped establish the growth hormone secretagogue field after its description in the 1980s. It reliably releases growth hormone and strongly stimulates appetite via ghrelin-receptor activation, but it has never been approved for any therapeutic indication; human data come mainly from pharmacology and physiology studies.

Long-acting insulin-like growth factor-1 analogue (Long R3 IGF-1); recombinant IGF-1 with an Arg3 substitution and a 13-amino-acid N-terminal extension; sold as a laboratory research reagent

IGF-1 LR3 is a recombinant analogue of insulin-like growth factor-1 engineered for greater potency and a longer half-life, chiefly by reducing its binding to IGF-binding proteins. It is manufactured and marketed as a research-use-only reagent to stimulate cell growth in laboratory culture; it has not undergone human clinical development and is not an approved therapeutic.

Endogenous activin-binding glycoprotein; myostatin/activin antagonist (studied as recombinant protein and via gene therapy, e.g., FS-344)

Follistatin is an endogenous activin-binding glycoprotein that antagonises myostatin (GDF-8) and activins, and it has been studied as a way to increase muscle mass in muscle-wasting diseases. Human experience is limited to early-phase gene-therapy trials (for example, AAV-delivered follistatin for Becker muscular dystrophy and inclusion body myositis); no follistatin product is approved for any indication.

Synthetic cyclic analogue of alpha-melanocyte-stimulating hormone (alpha-MSH); non-selective melanocortin receptor agonist

Melanotan II is a synthetic cyclic analogue of alpha-MSH that stimulates melanin production (tanning) and can trigger erections; the melanocortin research on sexual function later led to the separately approved drug bremelanotide (PT-141). Melanotan II itself has only limited early human study data, is not approved by any regulator, and is widely sold through unregulated channels despite official safety warnings.

Synthetic linear analogue of alpha-melanocyte-stimulating hormone (alpha-MSH); melanocortin-1 receptor (MC1R) agonist ([Nle4-D-Phe7]-alpha-MSH, NDP-MSH)

Afamelanotide is a linear analogue of alpha-melanocyte-stimulating hormone developed by the Australian company Clinuvel. By activating the melanocortin-1 receptor it increases skin eumelanin, providing photoprotection. It is approved for erythropoietic protoporphyria on the basis of Phase 3 randomized trials and is administered as a controlled-release implant by trained physicians.

Reproductive neuropeptide; KISS1 gene product and endogenous agonist of the kisspeptin receptor (KISS1R/GPR54); upstream stimulator of GnRH neurons

Kisspeptin, signalling through the KISS1R (GPR54) receptor, is a key upstream regulator of gonadotropin-releasing hormone (GnRH) neurons; loss-of-function mutations in its receptor cause absent puberty. Human experimental-medicine studies, notably kisspeptin-54 to trigger oocyte maturation in IVF and to probe reproductive disorders, have shown promising physiology, but kisspeptin remains investigational and unapproved.

Synthetic gonadotropin-releasing hormone (GnRH/LHRH); decapeptide identical to endogenous GnRH; GnRH receptor agonist

Gonadorelin is the decapeptide identical to natural GnRH. It was approved and marketed as a diagnostic agent (for example, Factrel) to assess pituitary gonadotropin reserve, and, delivered in a pulsatile fashion (for example, Lutrepulse), to induce ovulation in women with hypothalamic amenorrhea. Many branded gonadorelin products have since been discontinued in some markets, and it is now frequently supplied through pharmacy compounding; approval status differs across regions.

Synthetic 28-amino-acid thymic peptide (thymalfasin); immunomodulator

Thymosin alpha-1 is one of the most clinically studied thymic peptides, used in a number of countries to modulate immune responses in viral hepatitis, as a vaccine adjuvant, and as adjunctive therapy in sepsis and some cancers. The evidence base is substantial but mixed: multiple randomized trials and meta-analyses exist, yet results are heterogeneous and it has not achieved approval by the FDA or the EMA. Where it is marketed it is a prescription medicine used under medical supervision.

Thymic polypeptide preparation (calf-thymus extract); immunomodulatory bioregulator

Thymalin is one of the original 'peptide bioregulators' associated with the Russian researcher Vladimir Khavinson. It has been used in Russia and some former-Soviet states to modulate immunity, and small, largely Russian-language studies have explored effects on immune function and ageing. High-quality, independently replicated trials are lacking, and it is an unapproved substance outside those markets.

Mitochondria-targeted tetrapeptide (cardiolipin-binding Szeto-Schiller peptide)

Elamipretide is designed to improve mitochondrial function by stabilising cardiolipin and the cristae architecture of the inner mitochondrial membrane. It has been evaluated across numerous conditions such as primary mitochondrial myopathy, Barth syndrome, Leber hereditary optic neuropathy, dry age-related macular degeneration and heart failure, with mixed results; its pivotal primary mitochondrial myopathy trial (MMPOWER-3) did not meet its primary endpoint. In September 2025 it received US FDA accelerated approval for Barth syndrome (as Forzinity) based on an improvement in knee-extensor muscle strength, with a confirmatory trial required; for all other indications it remains investigational.

Mitochondrial-derived peptide (24-residue; encoded in the mtDNA 16S rRNA region); cytoprotective

Humanin was the first recognised mitochondrial-derived peptide, encoded within the mitochondrial 16S rRNA gene. It has been investigated preclinically for neuroprotection (particularly against amyloid-beta toxicity), insulin sensitivity and cardioprotection, and more-potent analogues such as HNG have been studied in the laboratory. Human data are essentially observational (for example, circulating humanin levels), there are no completed controlled efficacy trials, and it remains experimental.

Delta sleep-inducing peptide; endogenous neuromodulatory nonapeptide (Trp-Ala-Gly-Gly-Asp-Ala-Ser-Gly-Glu)

DSIP is an endogenous neuropeptide historically studied for roles in sleep regulation, stress adaptation, pain and neuroendocrine function. Findings across studies have been inconsistent and much of the work is old and of limited quality; there are no completed modern controlled efficacy trials and no regulatory approval. It remains a research compound.

Human cathelicidin antimicrobial peptide (37-residue C-terminal fragment of hCAP18); host-defence peptide

LL-37 is a naturally occurring antimicrobial peptide derived from the protein hCAP18 (the CAMP gene product). Beyond killing microbes, it modulates inflammation, chemotaxis, angiogenesis and wound healing, and its expression is induced by vitamin D. It has a dual nature: it is also implicated in inflammatory skin diseases and some cancers. Synthetic LL-37 has been explored in early clinical research (for example in wound healing), but it is not an approved therapeutic.

Angiotensin IV-derived peptide (metabolically stabilised); investigational nootropic / HGF-Met modulator

Dihexa is a small, metabolically stabilised angiotensin IV analogue studied in the laboratory for effects on synapse formation and memory, with proposed relevance to neurodegenerative disease. Its evidence base is entirely preclinical, it has no completed human clinical trials, and it is not an approved therapeutic.

Topical cosmetic peptide (Acetyl Hexapeptide-8); SNAP-25 N-terminal fragment mimetic

Argireline (acetyl hexapeptide-8, formerly acetyl hexapeptide-3) is a widely used topical cosmetic peptide marketed for the temporary appearance of reduced expression lines. It is applied to the skin in cosmetic formulations and is often described as a 'topical alternative' to injectable neuromodulators. Independent, high-quality efficacy evidence is limited and comes mainly from small cosmetic studies; it is a cosmetic ingredient, not an approved therapeutic.

Senolytic peptide (FOXO4 D-retro-inverso peptide); disrupts the FOXO4-p53 interaction

FOXO4-DRI (a D-retro-inverso peptide, sometimes called proxofim) came to prominence with a 2017 study showing it could selectively clear senescent cells and improve markers of health and fitness in aged and progeroid mice. It is a preclinical research tool in the senolytics field; it has not been evaluated in completed human clinical trials and is not an approved therapeutic.