Endocrine & Melanocortin · 10mg × 10 vials
MC1R agonist (afamelanotide analog). Studied for melanogenesis without UV exposure.
Melanotan I (afamelanotide, brand name Scenesse) is a synthetic 13-amino-acid linear analogue of alpha-melanocyte-stimulating hormone, built on the [Nle4, D-Phe7]-alpha-MSH scaffold first published by Mac Hadley and Victor Hruby at the University of Arizona in the early 1980s. Unlike the cyclic heptapeptide Melanotan II from the same programme, MT1 retains strong selectivity for the melanocortin-1 receptor (MC1R) on melanocytes. MC1R activation drives the cAMP-PKA cascade in pigment cells, upregulating tyrosinase and MITF and shifting melanocyte output from lighter pheomelanin toward darker eumelanin.
UV exposure still triggers the pigmentation cascade; afamelanotide raises the gain of the melanocyte response, so pigmentation develops with lower cumulative UV dose. Because MT1 has much weaker affinity at MC3R, MC4R, and MC5R than MT2, the central nervous system effects associated with MT2 (nausea, flushing, yawning, sexual arousal) are minimal or absent in the trial data. Afamelanotide is the only melanocortin analogue with full regulatory approval: EMA approval in 2014 and FDA approval in October 2019 as Scenesse, a subcutaneous controlled-release implant for prevention of phototoxicity in adults with erythropoietic protoporphyria.
What the published studies measured.
Peer-reviewed studies and clinical guidelines - tap any to read the source.
original Hadley/Levine UA Tucson phase 1 in humans, NDP-alpha-MSH (MT1) dose-response established 250-500 mcg range
Read study ↗PubMedDorr RT, Dvorakova K, Brooks C, et al, Increased eumelanin expression and tanning is induced by an infusion of afamelanotide, Photochem Photobiol 2004eumelanin shift mechanism confirmed in human subjects
Read study ↗PubMedLim HW et al, Afamelanotide and narrowband UV-B phototherapy for the treatment of vitiligo, JAMA Dermatol 2015vitiligo Phase 2, off-EPP indication data
Read study ↗PubMedLangendonk JG et al, Afamelanotide for erythropoietic protoporphyria, NEJM 2015pivotal Phase 3 efficacy for FDA submission, AE profile
Read study ↗PubMedBiolcati G et al, Long-term observational study of afamelanotide in 115 EPP patients, Br J Dermatol 2015long-term safety, melanoma rate not elevated vs background
Read study ↗PubMedMinder EI, Schneider-Yin X, A safety profile of afamelanotide-based therapy, Expert Opin Drug Saf 2015safety review across approved indication
Read study ↗Storage: refrigerated, stable 30-45 days reconstituted. Unmixed vials stable at room temp short-term; refrigerate for long storage. Light-sensitive, keep in original box.