Guide

Peptide Category Explainers: How Every Compound Class on This Site Is Defined

This site tracks dozens of compounds, and each one is assigned to a category that reflects its primary biological mechanism and intended research context. These categories are not rigid pharmacological classifications — some compounds could reasonably be placed in more than one group — but they provide a consistent framework for understanding why certain compounds are grouped together and how they relate to each other. This guide explains each of the nine categories used on the site: what the category means, the shared mechanism across its members, which compounds are currently tracked within it, and a summary of the regulatory landscape. The categories are: GLP-1 receptor agonists, growth hormone releasing peptides (GHRP), growth hormone releasing hormones (GHRH), recovery peptides, cognitive peptides, immune peptides, skin and cosmetic peptides, longevity compounds, and small molecules. For each category, the goal is to give readers a clear mental model so that when they encounter a compound name elsewhere on the site, they can immediately place it in context.

Last reviewed 2026-07-08 Next review 2027-07-08 42 sources
Metabolic

GLP-1 Receptor Agonists

GLP-1 receptor agonists are compounds that mimic or enhance the action of glucagon-like peptide-1, an incretin hormone naturally secreted by L-cells in the intestine in response to food. GLP-1 stimulates insulin secretion, suppresses glucagon, slows gastric emptying, and promotes satiety — all in a glucose-dependent manner. Native GLP-1 has a half-life of approximately two minutes due to rapid degradation by the DPP-4 enzyme, so pharmaceutical GLP-1 agonists are engineered for extended half-lives through amino acid modifications, fatty acid conjugation, or albumin binding. This category on the site includes both single GLP-1 receptor agonists and multi-receptor agonists that also target GIP and/or glucagon receptors, since they are commonly grouped together in public discussion and share overlapping clinical contexts. These are among the most heavily researched and widely prescribed compounds tracked on this site, with multiple FDA approvals for Type 2 diabetes and chronic weight management.

Key points

  • GLP-1 receptor agonists mimic the incretin hormone GLP-1, which stimulates insulin secretion, suppresses glucagon, slows gastric emptying, and promotes satiety — all in a glucose-dependent manner.
  • Semaglutide (Ozempic, Wegovy, Rybelsus) is FDA-approved for Type 2 diabetes and chronic weight management, with the STEP 1 trial showing approximately 15% weight loss at 68 weeks.
  • Tirzepatide (Mounjaro, Zepbound) is a dual GIP/GLP-1 receptor agonist FDA-approved for Type 2 diabetes and chronic weight management, with the SURMOUNT-1 trial showing weight loss exceeding 20% at 72 weeks.
  • Retatrutide is an investigational triple GLP-1/GIP/glucagon receptor agonist not yet FDA-approved; Phase 2 data showed dose-dependent weight loss up to 17.5% at 48 weeks, with Phase 3 trials ongoing.
  • These compounds have generated enormous public discussion and social media attention, requiring careful separation of clinical trial data from community claims about off-label and compounded use.
  • The FDA has issued warning letters related to compounded and research-use-only GLP-1 peptide marketing, and the regulatory landscape for compounded GLP-1 products remains active.

Retatrutide for Obesity — A Phase 2 Trial

New England Journal of Medicine · Peer reviewed · 2023-06-26 · accessed 2026-07-01

Phase 2 randomized trial of retatrutide (LY3437943), a triple GLP-1/GIP/glucagon receptor agonist, showing dose-dependent weight loss up to 17.5% at 48 weeks in adults with obesity.

TRIUMPH Phase 3 Trial Program for Retatrutide — ClinicalTrials.gov

ClinicalTrials.gov / U.S. National Library of Medicine · Primary regulatory · 2023-07-01 · accessed 2026-07-01

ClinicalTrials.gov registry entry for the TRIUMPH Phase 3 trial program evaluating retatrutide for obesity, sponsored by Eli Lilly. Retatrutide is not FDA-approved for any indication.

Warning Letter: Gram Peptides

U.S. Food and Drug Administration · Primary regulatory · 2026-03-31 · accessed 2026-06-30

FDA warning letter discussing peptide products marketed online and the limits of research-use-only positioning.

GH Secretagogue

Growth Hormone Releasing Peptides (GHRP)

Growth hormone releasing peptides (GHRPs) are a class of synthetic peptides that stimulate growth hormone release through the ghrelin receptor — also called the growth hormone secretagogue receptor (GHS-R). This is a different pathway from growth hormone releasing hormone (GHRH), which acts through its own dedicated receptor. GHRPs mimic the action of ghrelin, the endogenous ligand for the GHS-R, and were among the first compounds identified that could stimulate GH release without directly administering growth hormone itself. Despite extensive pharmacological characterization, no GHRP has ever received FDA approval for any indication. The most widely discussed GHRP on this site is ipamorelin, a first-generation pentapeptide identified in the late 1990s. MK-677 (ibutamoren) is mechanistically related — it is an orally active, non-peptide ghrelin receptor agonist — and is often discussed alongside GHRPs despite not being a peptide itself. AOD-9604, an HGH fragment peptide, is also grouped nearby because it relates to the growth hormone axis, though it acts through a lipolytic mechanism rather than GH release.

Key points

  • GHRPs stimulate growth hormone release through the ghrelin receptor (GHS-R), a distinct pathway from GHRH analogs which act through the GHRH receptor.
  • Ipamorelin is a synthetic pentapeptide GHRP widely discussed in fitness and anti-aging communities, often described as the 'safest GHS' based on preclinical selectivity data — this framing is a community interpretation, not a regulatory consensus.
  • MK-677 (ibutamoren) is an oral, non-peptide ghrelin receptor agonist developed by Merck with published Phase 2 data showing IGF-1 increases, but it was never submitted for FDA approval and development was discontinued.
  • AOD-9604 is a C-terminal fragment of human growth hormone (residues 177-191) designed for lipolytic activity; its Phase 2 obesity trials failed to meet primary weight loss endpoints and development was discontinued.
  • No GHRP or GHS-class compound has received FDA approval for any indication.
  • The CJC-1295 + ipamorelin combination is one of the most discussed peptide stacks in online fitness and telehealth communities, based on theoretical synergy between GHRH and GHS pathways, but lacks clinical trial data for the combination.

Ipamorelin, the First Selective Growth Hormone Secretagogue — Pharmacology

European Journal of Endocrinology (PubMed) · Peer reviewed · 1998-12-01 · accessed 2026-07-01

Raun et al. (1998) original pharmacology publication (PMID 9860070) describing ipamorelin as a pentapeptide growth hormone secretagogue with selectivity for GH release over cortisol and prolactin in animal models.

Oral Ghrelin Mimetic MK-677 Stimulates Pulsatile GH Secretion

Journal of Clinical Endocrinology & Metabolism (PubMed) · Peer reviewed · 2000-02-01 · accessed 2026-07-01

Svensson et al. (2000) study (PMID 10674575) demonstrating that oral MK-677 replicated the pulsatile GH profile seen with IV secretagogues in healthy older adults, with sustained IGF-1 increases over 4 weeks.

A 12-Month Study of the GH-Releasing Compound MK-677 in Hip Fracture Recovery

Journal of the American Geriatrics Society (PubMed) · Peer reviewed · 2002-03-01 · accessed 2026-07-01

Bach et al. (2002) 12-month Phase 2 trial (PMID 12004295) showing MK-677 improved functional status in elderly patients with hip fracture. Despite positive pharmacodynamic data, Merck did not advance MK-677 to FDA approval.

MK-677 Hip Fracture Recovery Trial — ClinicalTrials.gov

ClinicalTrials.gov / U.S. National Library of Medicine · Primary regulatory · 2009-11-01 · accessed 2026-07-01

ClinicalTrials.gov registry entry (NCT01016781) for the MK-677 hip fracture recovery trial sponsored by Merck. MK-677 is not FDA-approved for any indication.

AOD-9604 Clinical Trial Registry Entries — ClinicalTrials.gov

ClinicalTrials.gov / U.S. National Library of Medicine · Primary regulatory · 2026-07-01 · accessed 2026-07-01

ClinicalTrials.gov registry search for AOD-9604 clinical trials, including the Phase 2 obesity program by Metabolic Pharmaceuticals that failed to meet primary weight loss endpoints. AOD-9604 is not FDA-approved.

Warning Letter: Gram Peptides

U.S. Food and Drug Administration · Primary regulatory · 2026-03-31 · accessed 2026-06-30

FDA warning letter discussing peptide products marketed online and the limits of research-use-only positioning.

GH Secretagogue

Growth Hormone Releasing Hormones (GHRH)

Growth hormone releasing hormone (GHRH) is a peptide hormone produced in the hypothalamus that stimulates the anterior pituitary gland to secrete growth hormone. Synthetic GHRH analogs are designed to mimic this endogenous hormone and stimulate endogenous GH release, which in turn increases IGF-1 levels. This category includes the only growth hormone secretagogue-class peptide with current FDA approval: tesamorelin (Egrifta), approved for HIV-associated lipodystrophy. It also includes CJC-1295, a synthetic GHRH analog developed with drug affinity complex (DAC) technology for extended half-life that was never submitted for FDA approval, and sermorelin, a formerly FDA-approved diagnostic agent for pediatric growth hormone deficiency whose brand product (Geref) was discontinued by the manufacturer. GHRH analogs are mechanistically distinct from GHRPs — they act through a different receptor — and the two classes can have additive effects on GH release when studied together, which is the rationale for the common CJC-1295 + ipamorelin community protocol.

Key points

  • GHRH analogs stimulate endogenous growth hormone release through the GHRH receptor in the pituitary — a different receptor from GHRPs, which act through the ghrelin receptor.
  • Tesamorelin (Egrifta) is the only GHRH/GHS-class peptide with current FDA approval, indicated for reduction of excess visceral abdominal fat in HIV-infected patients with lipodystrophy, based on a Phase 3 trial published in NEJM (2010).
  • CJC-1295 is a synthetic GHRH analog with DAC technology for extended half-life; it was developed by ConjuChem but clinical development was discontinued and it was never submitted for FDA approval.
  • Sermorelin is a 29-amino-acid GHRH fragment that was formerly FDA-approved as Geref for diagnostic use in pediatric growth hormone deficiency; the manufacturer discontinued the brand product, and it is now widely compounded by telehealth clinics for off-label adult use.
  • Two forms of CJC-1295 exist in community discussions: with DAC (extended half-life) and without DAC (modified GRF 1-29); both are research-use-only and not FDA-approved.
  • The GHRH + GHRP combination (e.g., CJC-1295 + ipamorelin) is based on theoretical receptor synergy but has no FDA-approved clinical data for the combination.

Egrifta (tesamorelin) — FDA Drug Label

U.S. Food and Drug Administration · Primary regulatory · 2010-06-18 · accessed 2026-07-01

FDA-approved drug label for Egrifta (tesamorelin for injection), indicated for the reduction of excess visceral abdominal fat in HIV-infected patients with lipodystrophy. The only GHRH/GHS-class peptide with FDA approval.

Tesamorelin Clinical Trial Registry Entries — ClinicalTrials.gov

ClinicalTrials.gov / U.S. National Library of Medicine · Primary regulatory · 2010-01-01 · accessed 2026-07-01

ClinicalTrials.gov registry entries for tesamorelin clinical trials, including the pivotal Phase 3 trials for HIV-associated lipodystrophy that supported FDA approval of Egrifta.

Pharmacokinetics and Pharmacodynamics of CJC-1295, a Long-Acting GHRH Analog

Journal of Clinical Endocrinology & Metabolism (PubMed) · Peer reviewed · 2006-05-01 · accessed 2026-07-01

Teichman et al. (2006) pharmacokinetic study (PMID 16569233) showing that CJC-1295 increased GH and IGF-1 levels in healthy subjects for up to 6 days after a single dose. The primary published human data for CJC-1295.

Sermorelin (Geref) for Diagnosis of Growth Hormone Deficiency

PubMed — National Library of Medicine · Peer reviewed · 1997-01-01 · accessed 2026-07-01

PubMed index of clinical literature on sermorelin (Geref) for diagnostic testing of growth hormone deficiency in pediatric patients. Sermorelin was formerly FDA-approved as Geref; the brand product has been discontinued by the manufacturer.

Warning Letter: Gram Peptides

U.S. Food and Drug Administration · Primary regulatory · 2026-03-31 · accessed 2026-06-30

FDA warning letter discussing peptide products marketed online and the limits of research-use-only positioning.

Recovery

Recovery Peptides

Recovery peptides are a functional grouping rather than a single receptor family — these are compounds discussed primarily in the context of tissue repair, injury recovery, and wound healing. On this site, the two primary recovery peptides are BPC-157 and TB-500. BPC-157 is a pentadecapeptide derived from human gastric juice that has been studied in animal models for tendon, ligament, and muscle healing, but has no published human clinical trials and no FDA approval. TB-500 is a synthetic version of a fragment of thymosin beta-4, a naturally occurring peptide involved in actin binding and cell migration, and is similarly discussed in injury recovery contexts without FDA approval. Both compounds are widely sold as research-use-only chemicals and are among the most discussed peptides in online fitness and recovery communities. Several recovery peptides, including BPC-157 and TB-500, were scheduled for discussion at the July 2026 FDA Pharmacy Compounding Advisory Committee meeting, reflecting regulatory interest in the compounding of these substances.

Key points

  • Recovery peptides are grouped by functional context (tissue repair, injury recovery) rather than a shared receptor or mechanism.
  • BPC-157 is a pentadecapeptide derived from human gastric juice discussed in online recovery communities; it has no published human clinical trials and no FDA approval.
  • TB-500 is a synthetic fragment of thymosin beta-4, a peptide involved in actin binding and cell migration; it is also not FDA-approved and has no published human clinical trials for recovery.
  • Both BPC-157 and TB-500 were scheduled for FDA Pharmacy Compounding Advisory Committee discussion in July 2026, indicating active regulatory scrutiny.
  • The FDA has identified certain bulk peptide substances as potentially presenting significant safety risks in compounding contexts, which applies to these recovery peptides.
  • Online claims about recovery peptides should be treated as source-discovery signals, not proof of efficacy — the evidence base is predominantly preclinical.

Warning Letter: Gram Peptides

U.S. Food and Drug Administration · Primary regulatory · 2026-03-31 · accessed 2026-06-30

FDA warning letter discussing peptide products marketed online and the limits of research-use-only positioning.

Cognitive

Cognitive Peptides

Cognitive peptides are compounds discussed primarily in the context of cognitive enhancement, neuroprotection, and attention. This is a diverse group spanning different mechanisms and evidence levels. Semax is a heptapeptide ACTH analog registered as a medicine in Russia for cognitive and attention-enhancing effects, with studies primarily from Russian institutions and no FDA approval. Selank is a synthetic heptapeptide tuftsin analog registered in Russia as an anxiolytic, with predominantly Russian-language preclinical and limited clinical literature. Noopept is a dipeptide nootropic registered as a pharmaceutical in Russia for mild cognitive impairment, sold as a supplement in the US without FDA drug approval. Dihexa is an angiotensin IV analog developed to activate the HGF/c-Met receptor system, studied only in animal models with no human clinical trials. Cerebrolysin is a porcine brain-derived peptide preparation approved in over 40 countries for neurological indications including stroke and dementia, but not FDA-approved in the United States. The common thread is that all of these compounds are discussed in biohacking and cognitive enhancement communities, but their evidence bases vary widely — from small Russian clinical trials to purely preclinical animal data.

Key points

  • Cognitive peptides are grouped by functional context (cognitive enhancement, neuroprotection) rather than a shared mechanism — they span ACTH analogs, tuftsin analogs, dipeptide nootropics, angiotensin IV analogs, and brain-derived preparations.
  • Semax is an ACTH analog registered as a medicine in Russia; its clinical studies are primarily Russian-language and lack independent Western replication.
  • Selank is a tuftsin analog registered in Russia as an anxiolytic; its evidence base is predominantly preclinical with limited Russian clinical literature.
  • Noopept is a dipeptide nootropic registered as a pharmaceutical in Russia for mild cognitive impairment; it is sold as a dietary supplement in the US without FDA drug approval.
  • Dihexa is an angiotensin IV analog that activates the HGF/c-Met receptor system; it has been studied only in animal models with no human clinical trials. The widely circulated '10 million times stronger than BDNF' claim is an extrapolation from a single rat study and has not been validated in humans.
  • Cerebrolysin is a porcine brain-derived peptide preparation approved in 40+ countries for stroke and dementia but not FDA-approved in the United States; a Cochrane review noted inconsistent results for vascular dementia.
  • None of these compounds are FDA-approved for cognitive enhancement, and the evidence ranges from small Russian clinical trials to purely preclinical animal data.

Semax: cognitive and attention effects in clinical and preclinical studies

PubMed / NCBI · Peer reviewed · 2006-01-01 · accessed 2026-07-03

Russian-language clinical and preclinical publications on Semax (a heptapeptide ACTH analog) describing cognitive and attention-enhancing effects. Studies are primarily from Russian institutions and lack independent Western replication.

Immune

Immune Peptides

Immune peptides are compounds discussed primarily in the context of immune modulation, antimicrobial activity, and inflammatory response. This category includes thymosin alpha-1, LL-37, and KPV — three compounds with distinct mechanisms that share an immunological context. Thymosin alpha-1 is a naturally occurring thymic peptide that modulates immune function by enhancing T-cell maturation, dendritic cell activity, and cytokine production. It is marketed as Zadaxin and is approved in over 30 countries for chronic hepatitis B, hepatitis C, and as an immune adjuvant, but is not FDA-approved in the United States. LL-37 is the sole human cathelicidin antimicrobial peptide, with well-characterized broad-spectrum activity against bacteria, fungi, and enveloped viruses in laboratory studies, but no FDA-approved therapeutic products. KPV is a tripeptide (Lys-Pro-Val) derived from alpha-melanocyte-stimulating hormone (alpha-MSH) with reported anti-inflammatory effects in preclinical animal models, but no published human clinical trials. All three are tracked as regulatory watch items, with BPC-157 and several other peptides also scheduled for FDA advisory committee discussion.

Key points

  • Immune peptides are grouped by functional context (immune modulation, antimicrobial activity, anti-inflammatory effects) rather than a shared mechanism.
  • Thymosin alpha-1 is approved in 30+ countries as Zadaxin for hepatitis B/C and immune adjuvant use but has never received FDA approval in the United States, despite Fast Track designation for certain oncology indications and over 100 registered clinical trials.
  • LL-37 is the only human cathelicidin antimicrobial peptide, with broad-spectrum activity against bacteria, fungi, and viruses in laboratory studies, but no FDA-approved therapeutic products exist in the United States.
  • KPV is a tripeptide derived from alpha-MSH with reported anti-inflammatory effects in preclinical animal models; no human clinical trials have been published.
  • All three immune peptides are not FDA-approved and are sold as research-use-only chemicals; the biohacking community has adopted them for self-directed immune support despite the absence of clinical trial evidence.
  • KPV and several other peptides were scheduled for FDA Pharmacy Compounding Advisory Committee discussion in July 2026.

Thymosin Alpha-1 Clinical Trial Registry Entries — ClinicalTrials.gov

ClinicalTrials.gov / U.S. National Library of Medicine · Primary regulatory · 2026-07-01 · accessed 2026-07-01

ClinicalTrials.gov registry search showing 100+ interventional studies of thymosin alpha-1 across infectious disease, oncology, and immune support contexts, including COVID-19 trials.

Immune Modulation with Thymosin Alpha 1

Expert Review of Clinical Immunology (PubMed) · Peer reviewed · 2016-05-01 · accessed 2026-07-01

King R, Tuthill C (2016) comprehensive review (PMID 26653168) of thymosin alpha-1's immune-modulating mechanism, clinical development history, and therapeutic applications including hepatitis, oncology, and sepsis.

Zadaxin (thymosin alpha-1) Product Information

SciClone Pharmaceuticals · Primary regulatory · 2026-07-01 · accessed 2026-07-01

SciClone Pharmaceuticals product information for Zadaxin (thymosin alpha-1), approved in over 30 countries for chronic hepatitis B, hepatitis C, and immune adjuvant use. Not FDA-approved in the United States.

Little Peptide, Big Effects: Defining New Roles for LL-37 in Autoimmunity

Journal of Immunology (PubMed) · Peer reviewed · 2013-08-01 · accessed 2026-07-01

Kahlenberg JM, Kaplan MJ (2013) review (PMID 23836012) of LL-37's dual role in innate immunity and autoimmunity, describing both protective antimicrobial effects and pro-inflammatory potential in autoimmune disease.

LL-37 Clinical Trial Registry Entries — ClinicalTrials.gov

ClinicalTrials.gov / U.S. National Library of Medicine · Primary regulatory · 2026-07-01 · accessed 2026-07-01

ClinicalTrials.gov registry search for interventional studies involving LL-37/cathelicidin, showing limited clinical trial activity. LL-37 is not FDA-approved for any indication.

Cosmetic

Skin and Cosmetic Peptides

Skin and cosmetic peptides are compounds used primarily in topical skincare formulations for their proposed effects on collagen production, wrinkle reduction, and skin repair. These are the most commercially established peptide category in the consumer market, with widespread availability in over-the-counter cosmetic products. GHK-Cu (copper peptide) is a naturally occurring copper complex with proposed wound healing and skin repair properties based on in vitro and cosmetic research. Argireline (acetyl hexapeptide-8) is a synthetic hexapeptide fragment of SNAP-25, a protein involved in neurotransmitter release, marketed as a topical 'Botox alternative' that may inhibit SNARE complex formation and reduce wrinkle depth. Matrixyl (palmitoyl pentapeptide-4) is a matrikine peptide used in anti-wrinkle cosmetics that has shown modest improvements in fine lines and wrinkles in controlled clinical studies. All three are classified as cosmetic ingredients in the US with no FDA drug approval, though the FDA warning letter on peptide compounding applies to GHK-Cu products marketed beyond cosmetic use. The key distinction for this category is that cosmetic claims (wrinkle reduction, skin appearance) are regulated differently from medical claims, and these peptides should not be framed as treatments for medical conditions.

Key points

  • Skin and cosmetic peptides are the most commercially established peptide category, widely available in over-the-counter skincare products with no FDA drug approval.
  • GHK-Cu is a copper peptide with proposed wound healing and skin repair properties based on in vitro and cosmetic research; the Pickart et al. (2012) review is a comprehensive summary but originates from the peptide's discoverer.
  • Argireline (acetyl hexapeptide-8) is a SNAP-25 fragment marketed as a topical 'Botox alternative'; one RCT supports modest wrinkle reduction after 4 weeks of topical use, but it should not be equated to botulinum toxin injections.
  • Matrixyl (palmitoyl pentapeptide-4) is a matrikine peptide with clinical evidence for modest improvement in fine lines and wrinkles from a 12-week controlled study (Robinson et al., 2005).
  • All three cosmetic peptides are classified as OTC cosmetic ingredients in the US, not FDA-approved drugs; the FDA warning letter on peptide compounding applies to GHK-Cu products marketed beyond cosmetic use.
  • The palmitoyl chain in Matrixyl improves skin penetration of the peptide, as confirmed by in vitro permeation studies — this is mechanistic evidence, not proof of clinical efficacy.

GHK-Cu: A Human Skin Repair Peptide — Pickart et al. review

PubMed / NCBI · Peer reviewed · 2012-01-01 · accessed 2026-07-03

Pickart et al. (2012) comprehensive review of GHK-Cu (glycyl-L-histidyl-L-lysine copper complex) as a bioactive peptide with wound healing, skin repair, and anti-inflammatory properties, citing both in vitro and clinical cosmetic evidence.

The human skin repair peptide GHK-Cu and wound healing activity

PubMed / NCBI · Peer reviewed · 2014-01-01 · accessed 2026-07-03

Reviews and studies of GHK-Cu in wound healing contexts, describing its modulation of multiple gene pathways related to tissue repair, collagen synthesis, and anti-inflammatory responses. Primarily preclinical and cosmetic research.

Warning Letter: Gram Peptides

U.S. Food and Drug Administration · Primary regulatory · 2026-03-31 · accessed 2026-06-30

FDA warning letter discussing peptide products marketed online and the limits of research-use-only positioning.

Longevity

Longevity Compounds

Longevity compounds are substances discussed primarily in the context of extending lifespan, delaying age-related disease, and promoting healthspan. This is a heterogeneous category that includes both peptides and non-peptide molecules, unified by their proposed geroprotective mechanisms rather than a shared receptor or pathway. Rapamycin (sirolimus) is an FDA-approved mTOR inhibitor used for transplant rejection prophylaxis and lymphangioleiomyomatosis (LAM); it is the most discussed longevity therapeutic based on robust lifespan extension in mice (NIA ITP studies) but has no FDA approval for aging. NAD+ precursors (NR and NMN) are widely promoted to restore declining NAD+ levels and support sirtuin-mediated longevity pathways; NR is FDA-GRAS as a supplement, while NMN is subject to an FDA DSHEA exclusion determination. Spermidine is a naturally occurring polyamine that induces autophagy and has shown preliminary cognitive benefits in the SmartAge trial. Epitalon is a Russian-developed peptide with telomerase activation claims from a single research group, lacking independent Western replication. Metformin, while technically a small molecule, is often discussed in longevity contexts due to its AMPK activation and the ongoing TAME trial. The key challenge for this category is separating biomarker changes (e.g., raised NAD+, increased telomerase) from proven clinical outcomes, and separating preclinical mouse data from human evidence.

Key points

  • Longevity compounds are grouped by proposed geroprotective function (lifespan extension, healthspan, age-related disease delay) rather than a shared mechanism — they include mTOR inhibitors, NAD+ precursors, polyamines, and peptides.
  • Rapamycin (sirolimus) is FDA-approved for transplant rejection prophylaxis and LAM, and is the most discussed longevity therapeutic based on NIA ITP mouse lifespan data, but off-label use for aging is not FDA-approved and remains controversial.
  • NAD+ precursors (NR and NMN) raise blood NAD+ in humans, but clinical outcome benefits remain inconsistent; NR is FDA-GRAS as a supplement, while NMN is subject to an FDA DSHEA exclusion determination.
  • Spermidine is a naturally occurring polyamine that induces autophagy; the SmartAge RCT showed memory improvements in older adults with subjective cognitive decline, but no human lifespan data exists.
  • Epitalon is a peptide with telomerase activation claims from the Khavinson research group; these claims lack independent Western replication and should not be presented as established anti-aging evidence.
  • No completed randomized controlled trial has demonstrated lifespan extension in humans for any compound in this category; the evidence base ranges from observational associations to preclinical mouse data to small human biomarker trials.

Rapamune (sirolimus) Label Information

U.S. Food and Drug Administration · Primary regulatory · 2023-09-01 · accessed 2026-07-01

FDA-approved prescribing label for Rapamune (sirolimus), indicated for prophylaxis of organ rejection in kidney transplant patients and for the treatment of lymphangioleiomyomatosis (LAM).

mTOR inhibition improves immune function in the elderly

Science Translational Medicine · Peer reviewed · 2014-12-24 · accessed 2026-07-01

Double-blind, placebo-controlled trial (Mannick et al.) showing that low-dose rapamycin analog (everolimus) improved immune response to influenza vaccine in older adults, providing early human translational evidence.

FDA GRAS Notice No. 733 — Nicotinamide Riboside (NR)

U.S. Food and Drug Administration · Primary regulatory · 2016-07-11 · accessed 2026-07-01

FDA GRAS (Generally Recognized As Safe) notice response for nicotinamide riboside (NR) chloride, the ingredient in Tru Niagen, supporting its use as a dietary supplement ingredient.

FDA response to NMN DSHEA exclusion question

U.S. Food and Drug Administration · Primary regulatory · 2022-11-02 · accessed 2026-07-01

FDA determination that NMN (nicotinamide mononucleotide) is excluded from the dietary supplement definition under DSHEA because it was first authorized for investigation as a new drug. This triggered marketplace disruption for NMN supplements.

Epitalon and geroprotective peptides — review of anti-aging claims

PubMed / NCBI · Peer reviewed · 2020-01-01 · accessed 2026-07-03

Reviews of Epitalon and related peptides in the context of aging biology, noting that telomerase and longevity claims rest on preclinical data from limited research groups without large-scale human clinical trials.

Small Molecule

Small Molecules

Small molecules on this site are non-peptide organic compounds that are tracked alongside peptides because they appear in the same research, biohacking, and longevity discussions. These compounds are not peptides — they are not chains of amino acids — but they share overlapping communities of interest and are often discussed in the same contexts. Metformin is an FDA-approved biguanide antidiabetic that activates AMPK and is sometimes called 'poor man's rapamycin' in longevity circles; the TAME trial is investigating whether it can delay age-related disease onset in non-diabetic adults. Methylene blue is an FDA-approved medication for methemoglobinemia that has gained biohacking attention for proposed cognitive and mitochondrial benefits at low doses, supported only by preclinical data. 5-Amino-1MQ is a small molecule inhibitor of nicotinamide N-methyltransferase (NNMT) that has been promoted as 'exercise in a pill' based on preclinical mouse studies showing reversal of diet-induced obesity; no human clinical trials exist. The regulatory status of these compounds varies widely — from FDA-approved drugs with established safety profiles to research chemicals with no human safety data.

Key points

  • Small molecules on this site are non-peptide organic compounds tracked alongside peptides because they appear in the same research and biohacking communities.
  • Metformin is an FDA-approved biguanide antidiabetic that activates AMPK; the TAME trial is testing whether it can delay age-related disease in non-diabetic adults, but no completed RCT has demonstrated lifespan extension in humans.
  • Methylene blue is FDA-approved for methemoglobinemia (Provayblue) but biohacking use for cognitive enhancement and mitochondrial function is off-label and supported only by preclinical data; non-pharmaceutical-grade products raise significant quality concerns.
  • 5-Amino-1MQ is an NNMT inhibitor promoted as 'exercise in a pill' based exclusively on mouse studies; no human clinical trials have been published and it is not FDA-approved.
  • The regulatory status of small molecules in this category ranges from FDA-approved drugs (metformin, methylene blue) to unapproved research chemicals (5-amino-1MQ).
  • Observational data for metformin (e.g., reduced mortality in diabetic patients) should not be presented as causal evidence of longevity benefit in non-diabetics — confounding is a significant limitation of retrospective studies.

GLUCOPHAGE (metformin hydrochloride) Label Information

U.S. Food and Drug Administration · Primary regulatory · 2017-01-01 · accessed 2026-07-01

FDA-approved prescribing label for Glucophage (metformin hydrochloride), indicated as an adjunct to diet and exercise to improve glycemic control in adults and children with type 2 diabetes mellitus.

Targeting Aging with Metformin (TAME) — ClinicalTrials.gov

ClinicalTrials.gov / U.S. National Library of Medicine · Primary regulatory · 2015-05-04 · accessed 2026-07-01

ClinicalTrials.gov registry entry for the TAME (Targeting Aging with Metformin) trial, a multi-center study investigating whether metformin can delay the onset of age-related diseases in non-diabetic adults.

Metformin as a Tool to Target Aging (TAME concept article)

Cell Metabolism / Elsevier · Peer reviewed · 2016-09-13 · accessed 2026-07-01

Nir Barzilai and colleagues outline the scientific rationale and design of the TAME trial, arguing that metformin's AMPK-activating, insulin-sensitizing effects make it a candidate to target aging biology.

Metformin and aging: A clinical review

Aging and Disease / Metabolism reviews · Peer reviewed · 2021-01-01 · accessed 2026-07-01

Clinical review summarizing metformin's proposed mechanisms (AMPK activation, mTOR inhibition, insulin sensitization) and the evidence base for and against its use as a geroprotective agent.

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Retatrutide for Obesity — A Phase 2 Trial

New England Journal of Medicine · Peer reviewed · 2023-06-26 · accessed 2026-07-01

Phase 2 randomized trial of retatrutide (LY3437943), a triple GLP-1/GIP/glucagon receptor agonist, showing dose-dependent weight loss up to 17.5% at 48 weeks in adults with obesity.

TRIUMPH Phase 3 Trial Program for Retatrutide — ClinicalTrials.gov

ClinicalTrials.gov / U.S. National Library of Medicine · Primary regulatory · 2023-07-01 · accessed 2026-07-01

ClinicalTrials.gov registry entry for the TRIUMPH Phase 3 trial program evaluating retatrutide for obesity, sponsored by Eli Lilly. Retatrutide is not FDA-approved for any indication.

Ipamorelin, the First Selective Growth Hormone Secretagogue — Pharmacology

European Journal of Endocrinology (PubMed) · Peer reviewed · 1998-12-01 · accessed 2026-07-01

Raun et al. (1998) original pharmacology publication (PMID 9860070) describing ipamorelin as a pentapeptide growth hormone secretagogue with selectivity for GH release over cortisol and prolactin in animal models.

Oral Ghrelin Mimetic MK-677 Stimulates Pulsatile GH Secretion

Journal of Clinical Endocrinology & Metabolism (PubMed) · Peer reviewed · 2000-02-01 · accessed 2026-07-01

Svensson et al. (2000) study (PMID 10674575) demonstrating that oral MK-677 replicated the pulsatile GH profile seen with IV secretagogues in healthy older adults, with sustained IGF-1 increases over 4 weeks.

A 12-Month Study of the GH-Releasing Compound MK-677 in Hip Fracture Recovery

Journal of the American Geriatrics Society (PubMed) · Peer reviewed · 2002-03-01 · accessed 2026-07-01

Bach et al. (2002) 12-month Phase 2 trial (PMID 12004295) showing MK-677 improved functional status in elderly patients with hip fracture. Despite positive pharmacodynamic data, Merck did not advance MK-677 to FDA approval.

Egrifta (tesamorelin) — FDA Drug Label

U.S. Food and Drug Administration · Primary regulatory · 2010-06-18 · accessed 2026-07-01

FDA-approved drug label for Egrifta (tesamorelin for injection), indicated for the reduction of excess visceral abdominal fat in HIV-infected patients with lipodystrophy. The only GHRH/GHS-class peptide with FDA approval.

Pharmacokinetics and Pharmacodynamics of CJC-1295, a Long-Acting GHRH Analog

Journal of Clinical Endocrinology & Metabolism (PubMed) · Peer reviewed · 2006-05-01 · accessed 2026-07-01

Teichman et al. (2006) pharmacokinetic study (PMID 16569233) showing that CJC-1295 increased GH and IGF-1 levels in healthy subjects for up to 6 days after a single dose. The primary published human data for CJC-1295.

Sermorelin (Geref) for Diagnosis of Growth Hormone Deficiency

PubMed — National Library of Medicine · Peer reviewed · 1997-01-01 · accessed 2026-07-01

PubMed index of clinical literature on sermorelin (Geref) for diagnostic testing of growth hormone deficiency in pediatric patients. Sermorelin was formerly FDA-approved as Geref; the brand product has been discontinued by the manufacturer.

Warning Letter: Gram Peptides

U.S. Food and Drug Administration · Primary regulatory · 2026-03-31 · accessed 2026-06-30

FDA warning letter discussing peptide products marketed online and the limits of research-use-only positioning.

Semax: cognitive and attention effects in clinical and preclinical studies

PubMed / NCBI · Peer reviewed · 2006-01-01 · accessed 2026-07-03

Russian-language clinical and preclinical publications on Semax (a heptapeptide ACTH analog) describing cognitive and attention-enhancing effects. Studies are primarily from Russian institutions and lack independent Western replication.

Thymosin Alpha-1 Clinical Trial Registry Entries — ClinicalTrials.gov

ClinicalTrials.gov / U.S. National Library of Medicine · Primary regulatory · 2026-07-01 · accessed 2026-07-01

ClinicalTrials.gov registry search showing 100+ interventional studies of thymosin alpha-1 across infectious disease, oncology, and immune support contexts, including COVID-19 trials.

Immune Modulation with Thymosin Alpha 1

Expert Review of Clinical Immunology (PubMed) · Peer reviewed · 2016-05-01 · accessed 2026-07-01

King R, Tuthill C (2016) comprehensive review (PMID 26653168) of thymosin alpha-1's immune-modulating mechanism, clinical development history, and therapeutic applications including hepatitis, oncology, and sepsis.

GHK-Cu: A Human Skin Repair Peptide — Pickart et al. review

PubMed / NCBI · Peer reviewed · 2012-01-01 · accessed 2026-07-03

Pickart et al. (2012) comprehensive review of GHK-Cu (glycyl-L-histidyl-L-lysine copper complex) as a bioactive peptide with wound healing, skin repair, and anti-inflammatory properties, citing both in vitro and clinical cosmetic evidence.

Rapamune (sirolimus) Label Information

U.S. Food and Drug Administration · Primary regulatory · 2023-09-01 · accessed 2026-07-01

FDA-approved prescribing label for Rapamune (sirolimus), indicated for prophylaxis of organ rejection in kidney transplant patients and for the treatment of lymphangioleiomyomatosis (LAM).

FDA GRAS Notice No. 733 — Nicotinamide Riboside (NR)

U.S. Food and Drug Administration · Primary regulatory · 2016-07-11 · accessed 2026-07-01

FDA GRAS (Generally Recognized As Safe) notice response for nicotinamide riboside (NR) chloride, the ingredient in Tru Niagen, supporting its use as a dietary supplement ingredient.

FDA response to NMN DSHEA exclusion question

U.S. Food and Drug Administration · Primary regulatory · 2022-11-02 · accessed 2026-07-01

FDA determination that NMN (nicotinamide mononucleotide) is excluded from the dietary supplement definition under DSHEA because it was first authorized for investigation as a new drug. This triggered marketplace disruption for NMN supplements.

GLUCOPHAGE (metformin hydrochloride) Label Information

U.S. Food and Drug Administration · Primary regulatory · 2017-01-01 · accessed 2026-07-01

FDA-approved prescribing label for Glucophage (metformin hydrochloride), indicated as an adjunct to diet and exercise to improve glycemic control in adults and children with type 2 diabetes mellitus.

Targeting Aging with Metformin (TAME) — ClinicalTrials.gov

ClinicalTrials.gov / U.S. National Library of Medicine · Primary regulatory · 2015-05-04 · accessed 2026-07-01

ClinicalTrials.gov registry entry for the TAME (Targeting Aging with Metformin) trial, a multi-center study investigating whether metformin can delay the onset of age-related diseases in non-diabetic adults.