FDA-Approved (Scenesse)Research Use OnlyWADA Prohibited

Melanotan I

Afamelanotide — MC1R-selective alpha-MSH analog. FDA and EU-approved as Scenesse for erythropoietic protoporphyria (EPP) photoprotection. Stimulates eumelanin production with significantly less off-target activity than Melanotan II.

SpecialtyMelanocortinMC1R AgonistPhotoprotectionInjectable
QUICK FACTS
GENERIC NAMEAfamelanotide
CLASSAlpha-MSH analog — MC1R selective
APPROVALFDA 2019 + EMA 2014 — EPP photoprotection
VS MT-IIMore selective — fewer sexual/appetite side effects
WADA STATUSProhibited — S4 Hormone class
Overview

Melanotan I (afamelanotide) is a synthetic analog of alpha-melanocyte stimulating hormone (α-MSH) with selective affinity for the melanocortin 1 receptor (MC1R). MC1R activation drives eumelanin synthesis in skin melanocytes — the dark pigment form that provides photoprotection against UV-induced damage.

Compared to Melanotan II (a non-selective melanocortin agonist), MT-I’s selectivity for MC1R substantially reduces activity at MC3R and MC4R, minimizing the sexual arousal and appetite suppression effects seen with MT-II. This improved selectivity profile supported clinical development for photoprotection without the off-target safety concerns.

Scenesse (afamelanotide 16mg bioresorbable implant) received EMA approval in 2014 and FDA approval in 2019 for prevention of phototoxicity in adults with EPP — the first drug approved for this indication. Research vial use is off-label; the approved formulation is a subcutaneous implant, not an injectable solution.

Research Areas
MC1R pharmacologyPhotoprotection researchMelanogenesis researchEPP managementEumelanin inductionMelanocortin selectivity
Available Evidence3 categories
Human (FDA + EU Approved)Phase III data: significant reduction in phototoxic events in EPP. Approved by EMA (2014) and FDA (2019). Most robust melanocortin clinical dataset outside PT-141.
MechanisticMC1R selective agonism — eumelanin synthesis pathway well-characterized. Selectivity advantage over MT-II pharmacologically confirmed.
Off-label Injectable ResearchResearch-vial injection differs from approved implant formulation. Off-label use lacks Phase III backing for alternative delivery or non-EPP indications.
Documented Research Benefits6 documented
EPP photoprotection
FDA + EMA approved
Eumelanin induction
clinical
Reduced phototoxic events
Phase III
MC1R selective profile
pharmacological
Skin pigmentation research
clinical
Fewer off-target effects vs MT-II
comparative pharmacology

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Safety & Regulatory Status

Phase III safety data from Scenesse trials. Common effects: nausea, fatigue, headache, injection site reactions. Hyperpigmentation. The approved formulation is a bioresorbable implant — injectable research-vial use is off-label. WADA-prohibited (S4 Hormone class). Not for use in individuals with a history of melanoma or suspicious lesions. All information for educational reference only.

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