Afamelanotide (Melanotan-1)
A synthetic analogue of alpha-melanocyte-stimulating hormone (alpha-MSH) and the [Nle4, D-Phe7] linear form of what is loosely called Melanotan-1. Unlike the grey-market injectable, afamelanotide is an approved prescription drug (Scenesse), delivered as a subcutaneous slow-release implant to increase eumelanin and reduce phototoxicity in erythropoietic protoporphyria (EPP).
01 Overview
Afamelanotide binds the melanocortin-1 receptor (MC1R) on melanocytes, driving eumelanin synthesis and providing photoprotection independent of UV exposure. It is the only melanocortin analogue in this family to reach full marketing authorisation, approved by the EMA (2014) and FDA (2019) for EPP, a rare disorder in which sunlight causes severe pain.
Because it is an implant releasing peptide over days, dosing is standardised and supervised, unlike injectable Melanotan-1/2 sold for cosmetic tanning. Common on-treatment effects include skin darkening and new or darkened naevi; long-term melanoma surveillance is advised given the theoretical concern of stimulating pigmented lesions.
02 Mechanism
Agonist at the melanocortin-1 receptor (MC1R), increasing eumelanin production in melanocytes and conferring UV-independent photoprotection.
03 Dosing
| Tier | Dose | Route | Notes |
|---|---|---|---|
| Approved implant | 16 mg | SubQ | One 16 mg controlled-release implant every ~2 months during high-sunlight periods (EPP indication). |
04 Effects
| Effect | Magnitude | Evidence | |
|---|---|---|---|
| Increased skin pigmentationUV-independent eumelanin increase; the basis of both the medical photoprotection and the cosmetic tanning interest. | Measurable rise in melanin density | Clinical | |
| Reduced phototoxic pain in EPPRandomised trials showed longer tolerated sunlight exposure and improved quality of life in EPP patients. | More pain-free sun-exposure hours | Clinical |
05 Side effects
| Effect | Severity | Frequency | Evidence | Countermeasures |
|---|---|---|---|---|
| New or darkening melanocytic naeviExisting moles darken and new pigmented lesions can appear, complicating melanoma surveillance. | Moderate | Common | Clinical | |
| Nausea and headacheTransient nausea, headache and fatigue reported in trials, usually early and self-limiting. | Mild | Common | Clinical |