Vial Guide

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.

CompoundWhat it isApprovalEvidenceHow oftenHalf-lifeSport
Melanotan 1Melanocortin agonist (tanning)Approved in the USApproved drugDaily while loading, then 2–3× per weekabout 15 hours LabelNot banned
Melanotan 2Melanocortin agonist (tanning)Not approvedHuman studiesDaily while loading, then 1–2× per weekNot measuredLikely banned

Sexual desire

Bremelanotide (Vyleesi), approved in 2019 for low sexual desire in premenopausal women. It differs from Melanotan 2 only at one end.

CompoundWhat it isApprovalEvidenceHow oftenHalf-lifeSport
PT-141Melanocortin-receptor agonistApproved in the USApproved drugAs needed (max 8 a month)about 2.7 hours LabelNot 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.

CompoundWhat it isApprovalEvidenceHow oftenHalf-lifeSport
KPVAnti-inflammatory peptideNot approvedPreclinicalOnce dailyNot measuredLikely 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

What they have in common

Darker skin and moles

Label

Members that reach MC1 darken skin. Scenesse’s label lists darker skin and new or darker moles (4% each) and recommends a full-body skin exam twice a year. Vyleesi’s reports dark patches in 1% of users at up to 8 doses a month but 38% after 8 daily doses, and Melanotan 2 can bring out new moles within days.

Nausea and flushing

Label

Nausea is common across the group: 40% vs 1.3% on placebo with bremelanotide, 19% vs 14% with the afamelanotide implant, and frequent in Melanotan 2’s small trials. Flushing affected 20% on bremelanotide.

Blood pressure

Label

Each bremelanotide dose briefly raises blood pressure, usually for up to 12 hours, and its label rules it out with uncontrolled high blood pressure or known heart disease. Melanotan 2 is nearly identical, so its page applies the same caution; one overdose case report described a racing heart and raised blood pressure.

Melanoma

Precaution

Case reports describe melanomas in Melanotan 2 users, but no controlled study has tested the risk, so whether it raises it is unknown. Scenesse’s EU label urges special caution with a personal or family history of melanoma, inherited atypical-mole syndromes or past skin cancers.

Combining members

Label

The stack check flags any two of Melanotan 1, Melanotan 2 and PT-141, since all act on melanocortin receptors. Vyleesi’s label warns that doses close together can add up on blood pressure and that more frequent dosing raises the risk of dark skin patches. KPV isn’t flagged.

Pregnancy

Label

Vyleesi’s label advises birth control and stopping if pregnancy is suspected; in dogs, bremelanotide raised pregnancy loss. Scenesse’s EU label rules out pregnancy and breastfeeding and asks for birth control during treatment and for 3 months after. Melanotan 2 and KPV have no human safety data.

Approval and evidence

Label

Only two uses are approved: the afamelanotide implant for EPP and bremelanotide for acquired low desire in premenopausal women. Injected powders sold for tanning aren’t Scenesse and fall outside its label, Melanotan 2 was never approved, and KPV has no human data.

How they differ

Receptors

Label

Afamelanotide 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

Label

Scenesse 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

Trial

Afamelanotide: 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

  1. 1957The amino acid sequence of alpha-MSH, the tanning hormone, was published.
  2. 1992The first melanocortin receptors were cloned: the MSH receptor, now called MC1, and the ACTH receptor, which controls the adrenal glands.
  3. 1996A three-man pilot of Melanotan 2 reported tanning in two men and spontaneous erections after doses.
  4. 2014The EU approved afamelanotide as an implant to prevent light-induced pain in adults with EPP.
  5. 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.