COMPOUND

Compounds / Sexual health

Afamelanotide

Afamelanotide / Scenesse (synthetic alpha-MSH analog tridecapeptide; selective MC1R agonist)

Sexual health SubQ FDA approved

Synthetic alpha-melanocyte stimulating hormone analog (tridecapeptide). FDA-approved October 2019 (NDA 210797) as Scenesse implant for erythropoietic protoporphyria (EPP): increases pain-free light exposure in patients with this rare phototoxic disease. Manufacturer: Clinuvel Pharmaceuticals.\n\nDISTINCT FROM MELANOTAN II (MT-II): Afamelanotide is selective for MC1R; MT-II is a non-selective melanocortin agonist (MC1R + MC3R + MC4R + MC5R), which is why MT-II has more side effects (nausea, libido changes, BP). Afamelanotide is sometimes referred to as Melanotan-1 / MT-I in research peptide community. Off-label biohacker SubQ use is for tanning enhancement and as a lower-side-effect MT-II alternative.

At a glance

Routes
SubQ
Vial sizes
10 mg · 16 mg
Evidence base
2 studies 2 human

Mechanism

Selective MC1R agonist with much higher affinity than endogenous α-MSH. Activation produces increased eumelanin (the photoprotective melanin form) production in melanocytes, independent of UV exposure (acts directly on melanocytes). Skin darkening / tanning effect; photoprotection in EPP without sun exposure trigger. Long-term safety confirmed across 115 patients up to 8 years. Selectivity: MC1R >> MC3R/MC4R/MC5R (unlike MT-II).

Dosing

Any amounts shown here are reported from published studies only. 2 of 2 catalogued studies involved human subjects. COMPOUND does not publish its own dosing guidance.

Where a study reports an amount, it appears in that study's entry below, attributed to the source.

Published evidence

  1. Human RCT 2015

    Afamelanotide for erythropoietic protoporphyria

    Langendonk JG, Balwani M, Anderson KE, et al. N Engl J Med

    Afamelanotide 16 mg SubQ implant every 2 months significantly increased pain-free sun exposure in EPP patients (primary endpoint met). Median 64h vs 41h placebo.

    PMID 26132941

  2. Human observational 2015

    Long-term observational study of afamelanotide in 115 patients with erythropoietic protoporphyria

    Biolcati G, Marchesini E, Sorge F, et al. Br J Dermatol

    Long-term safety and efficacy in EPP confirmed across 115 patients up to 8 years of follow-up.

    PMID 25494545

Reported side effects

Implant site reaction
Very common Mild · Local skin reaction at implant site; expected. FDA label.
Skin hyperpigmentation / new nevi
Very common Mild · Intended effect plus diffuse darkening; new nevi may develop. FDA label requires twice-yearly full body skin exam.
Nausea
Common Mild · Notably less than MT-II due to MC1R selectivity. FDA label.
Headache
Common Mild · FDA label.
Fatigue / somnolence
Common Mild · FDA label.
Skin examination required
Very common Mild · FDA label requires twice-yearly full body skin exam due to nevi changes.

Interactions

  • Melanotan II Redundant

    Both MC1R agonists; Afamelanotide selective, MT-II non-selective.

Reconstitution and storage

FDA implant: pre-prepared, no reconstitution. Research peptide form: lyophilized; reconstitute with BAC water typical 1-2 mg/mL.

Refrigerated reconstituted; lyophilized stable.

Open the reconstitution calculator for Afamelanotide