Melanotan-1

FDA-approved context Skin & Hair 2 sources

Melanotan-1 is a synthetic analogue of alpha-melanocyte-stimulating hormone (α-MSH) that stimulates melanin production. It is clinically approved (as afamelanotide) to treat erythropoietic protoporphyria (EPP) by providing photoprotection against UV radiation.

01Dosing reference

Amount

1-2 mg/day (research cosmetic dosing)

Frequency

Daily until desired pigmentation is reached, then 1-2x/week for maintenance

Cycle

4-8 weeks

Reference figures, not a recommendationThese values reflect amounts described in the literature and vendor documentation this database indexes. Use the reconstitution calculator to convert them into syringe units.

02Mechanism of action

MC1R Activation

Melanotan-1 binds selectively to the melanocortin-1 receptor (MC1R) on the surface of melanocytes.

Melanogenesis Stimulation

Activation of MC1R triggers a signaling cascade that increases the production of eumelanin, the dark pigment in skin.

Photoprotection

The increased melanin density absorbs and scatters UV radiation, protecting skin cells from DNA damage and phototoxicity.

03Human evidence

Afamelanotide (Melanotan-1) significantly increased pain-free time in sunlight for patients with erythropoietic protoporphyria (EPP).

Phase 3 randomized, double-blind, placebo-controlled trials leading to FDA approval.

Melanotan-1 safely induced skin pigmentation in healthy volunteers without the need for concurrent UV exposure.

Early clinical studies assessing the tanning efficacy and safety profile in healthy adults.

04Preclinical evidence

Melanotan-1 reduced UV-induced DNA damage and sunburn cell formation in animal models.

Murine models exposed to UV radiation to assess photoprotective capabilities.

Increased tyrosinase activity and melanin synthesis in cultured melanocytes.

In vitro studies demonstrating the direct mechanism of action on pigment-producing cells.

05What is known vs. unknown

Reasonably established

Approved by the FDA under the brand name Scenesse (afamelanotide) for EPP.
Induces skin pigmentation (tanning) by mimicking the body's natural α-MSH.
Has a highly selective binding profile for MC1R, resulting in fewer systemic side effects compared to Melanotan-2.
Provides measurable photoprotection against UV-induced skin damage.

Unknowns & limits

Long-term safety of unregulated, recreational use for cosmetic tanning remains unverified.
Potential effects on existing nevi (moles) and the risk of melanoma with prolonged, unsupervised use require further study.

06Safety & regulatory context

Regulatory statusAfamelanotide is FDA-approved as a subcutaneous implant (Scenesse) for the treatment of erythropoietic protoporphyria (EPP). However, Melanotan-1 is frequently sold on the unregulated market as an injectable peptide for cosmetic tanning. Common side effects include nausea, flushing, headache, and the darkening of existing moles or freckles. Unregulated use carries significant risks, including product contamination, inaccurate dosing, and unknown long-term dermatological effects.

07Compared with Melanotan-2

Melanotan-1 vs. Melanotan-2

Key difference

Melanotan-1 is highly selective for MC1R and primarily affects pigmentation, whereas Melanotan-2 binds to multiple melanocortin receptors (including MC3R and MC4R), causing additional effects like increased libido and appetite suppression.

When researchers discuss each

Melanotan-1 is discussed for targeted photoprotection and clinical use in EPP, while Melanotan-2 is often discussed in the context of sexual dysfunction and cosmetic tanning, despite its higher side effect profile.

08Glossary

α-MSH

Alpha-melanocyte-stimulating hormone, an endogenous peptide that naturally stimulates melanin production in the body.

Melanogenesis

The biological process by which melanocytes produce melanin, the pigment responsible for skin, hair, and eye color.

Eumelanin

A dark brown to black type of melanin that provides the most effective photoprotection against UV damage.

Erythropoietic Protoporphyria (EPP)

A rare genetic metabolic disorder that causes severe, painful skin reactions upon exposure to sunlight.

09Knowledge check

Q1What is the primary receptor targeted by Melanotan-1 to induce pigmentation?

Q2How does Melanotan-1 primarily differ from Melanotan-2 in its effects?

Q3Which statement best reflects a documented limitation in the evidence about Melanotan-1 use for cosmetic tanning?

Q4According to the dossier, in which research contexts are Melanotan-1 and Melanotan-2 primarily discussed?

Q5Which of the following accurately reflects the safety and regulatory context provided in the dossier?

10Sources

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Research and educational use onlyNothing on this site is medical advice, a prescription, or a recommendation for human use. Compounds documented here are research chemicals. Consult a qualified clinician before making any health decision.