Melanotan 1（阿法美拉诺肽）

产品概览

Afamelanotide is a first-in-class MC1R agonist medication approved in the US and EU. In the EU, it prevents phototoxicity in adults with EPP. In the US, it increases pain-free light exposure in adults with EPP-related phototoxicity. It stimulates eumelanin production (the "tanning" pigment) independently of UV exposure, while also enhancing antioxidant activities, DNA repair processes, and anti-inflammatory signaling. Designed to resist enzymatic breakdown, it has a prolonged duration of action compared to natural α-MSH.

作用机制

Afamelanotide binds to MC1R on melanocytes, increasing cAMP and tyrosinase activity to stimulate eumelanin synthesis. Eumelanin provides photoprotection by absorbing UV radiation and scavenging reactive oxygen species. The peptide also enhances DNA repair (reducing thymine dimers and sunburn cells) and modulates inflammatory pathways through melanocortin signaling.

主要优势

Sunless Tanning & Photoprotection — Stimulates eumelanin production for a controlled, natural-looking tan without UV exposure. Increased melanin acts as an "internal sunscreen" absorbing harmful UV rays and reducing oxidative stress.

EPP Treatment — FDA-approved to reduce pain and increase light tolerance in EPP patients. Provides meaningful quality of life improvement for this rare, debilitating condition.

DNA Repair Enhancement — Reduces UV-induced DNA damage markers including thymine dimer formation and sunburn cells. Supports the skin's natural defense against photoaging and UV-related damage.

Repigmentation Support — Shows potential for vitiligo repigmentation when used alongside phototherapy. Also being researched for polymorphic light eruption and solar urticaria.

Anti-Inflammatory Effects — Melanocortin pathway activation modulates inflammation, showing preliminary benefit in reducing inflammatory skin lesions including acne.

参考资料

1. Scenesse: Summary of Product Characteristics. *European Medicines Agency.* 2016.
2. Haylett AK, et al. Systemic photoprotection in solar urticaria with α-MSH analogue. *Br J Dermatol.* 2011;164(2):407–414.
3. McNeil MM, et al. Afamelanotide in the treatment of dermatologic disease. *Skin Therapy Lett.* 2018;23(6):6–10.