Melanocortin peptides
These peptides are built on alpha-MSH, the body’s tanning hormone, which acts on a family of five melanocortin receptors. Two have narrow approvals, the afamelanotide implant and bremelanotide; Melanotan 2 was never approved, and KPV, a three-amino-acid fragment, has only animal data.
- Compounds
- 4
- Approved drug
- 2
- Human studies
- 1
- Preclinical
- 1
Members
Tanning and skin
Melanotan 1 is afamelanotide, approved only as a 16 mg implant for a rare light-sensitivity disorder; Melanotan 2 was never approved.
| Compound | What it is | Approval | Evidence | How often | Half-life | Sport |
|---|---|---|---|---|---|---|
| Melanotan 1 | Melanocortin agonist (tanning) | Approved in the US | Approved drug | Daily while loading, then 2–3× per week | about 15 hours Label | Not banned |
| Melanotan 2 | Melanocortin agonist (tanning) | Not approved | Human studies | Daily while loading, then 1–2× per week | Not measured | Likely banned |
Sexual desire
Bremelanotide (Vyleesi), approved in 2019 for low sexual desire in premenopausal women. It differs from Melanotan 2 only at one end.
| Compound | What it is | Approval | Evidence | How often | Half-life | Sport |
|---|---|---|---|---|---|---|
| PT-141 | Melanocortin-receptor agonist | Approved in the US | Approved drug | As needed (max 8 a month) | about 2.7 hours Label | Not banned |
Anti-inflammatory fragment
The last three amino acids of alpha-MSH. FDA’s 2026 review found melanocortin receptors are unlikely to be its target.
| Compound | What it is | Approval | Evidence | How often | Half-life | Sport |
|---|---|---|---|---|---|---|
| KPV | Anti-inflammatory peptide | Not approved | Preclinical | Once daily | Not measured | Likely banned |
Approval, evidence, half-life and sport status restate each compound’s own page, where the sources are listed. Select a name for doses, side effects and studies.
How they work
Melanocortins are hormones cut from one precursor protein, including alpha-MSH (alpha-melanocyte-stimulating hormone) and ACTH, the hormone that drives the adrenal glands. They act on five melanocortin receptors. MC1, on melanocytes, the skin’s pigment-making cells, drives production of eumelanin, the brown-black pigment. MC4, on nerve cells throughout the brain, is involved in appetite and sexual function, and the ACTH receptor (MC2) controls the adrenal glands. Label
The members differ in which receptors they reach. Afamelanotide (Melanotan 1) works mainly through MC1, and its label says it raises eumelanin without sun or UV exposure. Bremelanotide (PT-141) activates several receptors, MC1 and MC4 most at its dose, and its label says how it improves desire is unknown. Melanotan 2, which differs from bremelanotide only at one end, binds several receptors strongly in lab tests, so its tanning comes with erections, nausea and less appetite. Label
KPV is the last three amino acids of alpha-MSH: lysine, proline and valine. In cell and mouse studies it is carried into gut-lining and immune cells, where it damps inflammatory signaling, and oral KPV reduced colitis in two mouse models. FDA’s 2026 review concluded melanocortin receptors are unlikely to be its target, and it has never been tested in people. Animal
What’s shown in people is narrow. In two trials in erythropoietic protoporphyria (EPP), a rare disorder that makes light exposure painful, the afamelanotide implant gave more pain-free time in sunlight. In two 24-week trials, bremelanotide raised desire scores about a third of a point more than placebo in premenopausal women. Melanotan 2’s human record is three tiny trials with 23 men in total. Trial
How they differ
Receptors
LabelAfamelanotide works mainly through MC1, the pigment receptor. Bremelanotide activates MC1, MC4, MC3, MC5 and MC2, in that order of potency, with MC1 and MC4 most relevant at its dose. Melanotan 2 binds several receptors strongly in lab tests. KPV likely doesn’t act through melanocortin receptors at all.
Form and dosing
LabelScenesse is a 16 mg implant a clinician places under the skin every 2 months. Vyleesi is a 1.75 mg autoinjector used as needed, at most once in 24 hours; its label doesn’t recommend more than 8 doses a month. In community use, melanotan powders are injected daily at first, then 1–3 times a week, and KPV is taken daily.
Main effects
TrialAfamelanotide: pigment and light tolerance, with implant-site reactions and nausea. Bremelanotide: desire, with nausea, flushing and blood pressure rises. Melanotan 2: tanning plus spontaneous erections and less appetite, with case reports of priapism (an erection lasting hours) and muscle breakdown. KPV: lower inflammation in animal models, with no human side-effect data.
Sport status
Melanotan 1 and PT-141 aren’t banned: as approved drugs they fall outside WADA’s S0 rule. Melanotan 2 and KPV aren’t named on the 2026 list but likely fall under S0, which bans drugs with no current human approval anywhere.
History
- 1957The amino acid sequence of alpha-MSH, the tanning hormone, was published.
- 1992The first melanocortin receptors were cloned: the MSH receptor, now called MC1, and the ACTH receptor, which controls the adrenal glands.
- 1996A three-man pilot of Melanotan 2 reported tanning in two men and spontaneous erections after doses.
- 2014The EU approved afamelanotide as an implant to prevent light-induced pain in adults with EPP.
- 2019FDA approved bremelanotide (Vyleesi) in June and the afamelanotide implant (Scenesse) in October.
Comparisons and guides
Questions
What are melanocortin peptides?
Peptides that copy or mimic alpha-MSH, a hormone that acts on a family of five melanocortin receptors. Depending on the receptor, they darken skin (MC1) or act in the brain on appetite and sexual function (MC4). Afamelanotide (Melanotan 1) and bremelanotide (PT-141) are approved for narrow uses; Melanotan 2 never was.
What’s the difference between Melanotan 1 and Melanotan 2?
Melanotan 1 is afamelanotide: it acts mainly on the pigment receptor MC1 and is approved as a 16 mg implant for EPP, a rare disorder that makes light painful. Melanotan 2 is a shorter, ring-shaped peptide that reaches several receptors, so tanning comes with nausea, spontaneous erections and less appetite. It was never approved, and case reports link it to melanoma, priapism and muscle breakdown.
Is PT-141 the same as Melanotan 2?
Nearly. Bremelanotide (PT-141) differs from Melanotan 2 only at one end of the chain. Bremelanotide went through Phase 3 trials and was approved in 2019 as Vyleesi for acquired low sexual desire in premenopausal women, while Melanotan 2 never got past three tiny trials. Vyleesi’s label warns of nausea, blood pressure rises and dark skin patches.
Do melanotans cause skin cancer?
It isn’t known. Case reports describe melanomas in Melanotan 2 users, but no controlled study has tested the risk. Both melanotans darken existing moles and can bring out new ones, and Scenesse’s label recommends a full-body skin exam twice a year; its EU label urges special caution with a personal or family history of melanoma.
Is KPV a melanocortin?
It comes from one: KPV is the last three amino acids of alpha-MSH. But FDA’s 2026 review concluded melanocortin receptors are unlikely to be its target; in cell and mouse studies it seems to act inside gut-lining and immune cells instead. It has never been tested in people, and the stack check doesn’t group it with the melanotans.
Sources
- Scenesse (afamelanotide) prescribing information (DailyMed, May 2026) and EU summary of product characteristics (EMA, Oct 2025); Drugs@FDA approval, October 2019
- Vyleesi (bremelanotide) prescribing information, sections 2, 4, 5, 6 and 12 (DailyMed, Nov 2025); Drugs@FDA approval, June 2019
- Cone, physiological functions of the melanocortin system, review (Endocr Rev 2006) PMID 17077189
- Harris and Lerner, amino acid sequence of alpha-MSH (Nature 1957) PMID 13451616
- Mountjoy et al., cloning of a family of genes that encode the melanocortin receptors (Science 1992) PMID 1325670
- Dorr et al., Melanotan-II in a pilot phase I clinical study (Life Sci 1996) PMID 8637402
- Minder et al., afamelanotide pharmacology and clinical use, including its 2014 EU approval, review (Clin Pharmacokinet 2017) PMID 28063031
- Langendonk et al., two randomized trials of afamelanotide in EPP (N Engl J Med 2015) PMID 26132941
- Kingsberg et al., bremelanotide for low sexual desire, two Phase 3 trials (Obstet Gynecol 2019) PMID 31599840
- FDA briefing document for KPV-related bulk drug substances, Pharmacy Compounding Advisory Committee (July 2026)
Each compound’s page lists the sources for its own doses, status and studies.