Melanotan II is a synthetic cyclic analogue of alpha-melanocyte stimulating hormone with agonist activity across multiple melanocortin receptor subtypes. Its effect on melanogenesis is real and dose-dependent, and the melanocortin-4 receptor activity accounts for the reported effects on erectile function and appetite. It is, however, the compound in this portfolio requiring the most careful handling. Unlike afamelanotide, which is a selective analogue that completed formal development and holds authorisation for a narrow rare-disease indication, Melanotan II has never been through regulated development. The published clinical literature consists largely of case reports describing adverse outcomes, including new and changing melanocytic naevi, melanoma diagnosed following use, priapism, and rhabdomyolysis. Several regulators have issued formal safety warnings against it. PHI supplies it only where a practitioner has made a documented clinical judgement, and it should not be presented as a lifestyle or cosmetic product.
Active Compound: Melanotan II (afamelanotide analogue, non-selective melanocortin agonist)
Permitted Claim GuidelinesA melanocortin receptor agonist. Supplied only on documented practitioner direction. Regulatory safety warnings have been issued in several markets and are set out in the product safety information.
Mechanism of ActionNon-selective agonist at melanocortin receptors MC1R through MC5R. MC1R activation on melanocytes stimulates eumelanin synthesis, producing pigmentation independent of ultraviolet exposure. MC4R activation in the central nervous system underlies the reported effects on erectile function and appetite suppression. The lack of receptor selectivity is the source of both its breadth of effect and its adverse event profile.
Evidence Grade: C - Early human pharmacological data; adverse event literature predominates. No controlled efficacy trials.
Clinical Evidence BaseEarly human studies confirmed dose-dependent melanogenesis and erectile response. The subsequent clinical literature is dominated by case reports of adverse outcomes rather than efficacy trials. The related selective analogue afamelanotide has completed controlled trials and holds authorisation for erythropoietic protoporphyria; those data do not transfer to Melanotan II.
Literature & ReferencesWessells H et al. J Urol, 1998 - synthetic melanotropic peptide initiates erections in men. | Langan EA et al. Br J Dermatol, 2010 - melanotan use and the emergence of adverse reactions. | Cardones AR, Grichnik JM. Arch Dermatol, 2009 - alpha-MSH analogues and melanoma risk. | Ong S, Bowling J. Clin Exp Dermatol, 2012 - melanotan-associated melanoma.
Safety & PrecautionsThis compound carries the highest risk profile in the range and must be flagged as such. Reported effects include nausea, flushing, spontaneous erections and priapism, appetite suppression, and darkening or enlargement of existing naevi. Case reports describe melanoma diagnosed in users and at least one case of rhabdomyolysis. Multiple national regulators have issued public safety warnings. Full dermatological assessment and documented naevus mapping before use, with periodic skin surveillance, should be treated as a minimum standard. Absolutely contraindicated where there is any personal or family history of melanoma or atypical naevus syndrome. Patients must be told that pigmentation does not remove the need for sun protection.
ContraindicationsPersonal or family history of melanoma or skin cancer; atypical or dysplastic naevus syndrome; multiple or changing naevi; pregnancy and breastfeeding; cardiovascular disease; known hypersensitivity. Not appropriate for cosmetic tanning purposes.
Storage & HandlingStore lyophilised vial at 2-8 C, protected from light.
Regulatory StatusNot authorised as a medicine in the UK, EU or US and the subject of published safety warnings from multiple national regulators, including the MHRA. Sale for cosmetic tanning is unlawful in several jurisdictions. Supply must be strictly limited to documented practitioner-led clinical use where permitted.