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Home/Skin, Hair & Cosmetic/Melanotan 1 (Afamelanotide)

Melanotan 1 (Afamelanotide)

Synthetic alpha-MSH analog (afamelanotide) that stimulates eumelanin production; approved to reduce phototoxicity in porphyria.

Overview

Melanotan 1, known pharmaceutically as afamelanotide, is a synthetic linear analog of alpha-melanocyte-stimulating hormone (alpha-MSH) created by substituting norleucine at position 4 and D-phenylalanine at position 7 of the native sequence. It is a potent melanocortin-1 receptor (MC1R) agonist that stimulates eumelanin synthesis, giving skin a tan in the absence of ultraviolet exposure. Unlike the unregulated research versions, afamelanotide is an approved pharmaceutical: a controlled-release subcutaneous implant (marketed as Scenesse) is approved in the EU and the US to reduce phototoxic reactions in erythropoietic protoporphyria.

Mechanism

Binding to MC1R on melanocytes activates cAMP signaling and the melanogenic enzyme cascade, shifting production toward photoprotective eumelanin. The resulting skin darkening is used therapeutically to raise the light tolerance of patients with erythropoietic protoporphyria, who suffer severe pain on sun exposure.

Dosing

The approved product is administered as a subcutaneous implant at the dosing interval specified in the approved labeling for erythropoietic protoporphyria. Research-grade injectable forms used outside approved indications have no approved dose and are associated with significant unregulated-use risks.

Expected Effects

  • increased eumelanin and visible skin darkening
  • improved light tolerance and reduced phototoxic pain in erythropoietic protoporphyria patients (approved use)
  • proposed cosmetic tanning use is not an approved indication

Side Effects & Tolerability

Approved-use safety data describe nausea, headache, fatigue, injection or implant-site reactions, and darkening or new appearance of nevi (moles), which requires dermatologic monitoring. Unregulated injectable use adds contamination, dosing-error, and counterfeit risks.

Storage

The approved implant is stored per its pharmaceutical labeling. Unregulated lyophilized research material should be kept frozen, desiccated, and protected from light.

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