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Afamelanotide acetate

(Nle4,D-Phe7)-α-MSH; NDP-MSH; Melanotan 1; CUV1647;Melanotan-1;MT-1;MT1;MT 1;MBJ 05
75921-69-6 (net)
Ac-Ser-Tyr-Ser-Nle-Glu-His-D-Phe-Arg-Trp-Gly-Lys-Pro-Val-NH2 acetate salt
Molecular Formula
Afamelanotide is a synthetic analog of α-melanocyte stimulating hormone (α-MSH). It act as a photoprotective agent by inducing skin pigmentation through melanogenesis.

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Afamelanotide is a synthetic peptide analogue of the naturally occurring alpha-melanocyte stimulating hormone (a-MSH) with potential photoprotective activity. Mimicking the action of a-MSH, afamelanotide stimulates melanocytes to increase the production and release of melanin. Increased melanocyte melanin may protect against ultraviolet radiation (UVR)-initiated cellular DNA damage, oxidation of membrane proteins, and alterations in intracellular signaling processes in epidermal cells. Endogenously, a-MSH is released by skin cells in response to UVR exposure, stimulating melanocytes to produce and release melanin.

Vitiligo is characterized by depigmented patches of skin due to loss of cutaneous melanocytes. Many recent studies have demonstrated defects in the melanocortin system in patients with vitiligo, including decreased circulating and lesional skin levels of α-melanocyte-stimulating hormone (α-MSH). Afamelanotide is a potent and longer-lasting synthetic analogue of naturally occurring α-MSH.

Grimes P E, Hamzavi I, Lebwohl M, et al. The efficacy of afamelanotide and narrowband UV-B phototherapy for repigmentation of vitiligo[J]. JAMA dermatology, 2013, 149(1): 68-73.

Narrowband UV-B (NB-UV-B) phototherapy is used extensively to treat vitiligo. Afamelanotide, an analogue of α-melanocyte-stimulating hormone, is known to induce tanning of the skin.

Lim H W, Grimes P E, Agbai O, et al. Afamelanotide and narrowband UV-B phototherapy for the treatment of vitiligo: a randomized multicenter trial[J]. JAMA dermatology, 2015, 151(1): 42-50.

Erythropoietic protoporphyria is a severe photodermatosis that is associated with acute phototoxicity. Patients with this condition have excruciating pain and a markedly reduced quality of life. We evaluated the safety and efficacy of an α-melanocyte-stimulating hormone analogue, afamelanotide, to decrease pain and improve quality of life.

Langendonk J G, Balwani M, Anderson K E, et al. Afamelanotide for erythropoietic protoporphyria[J]. New England Journal of Medicine, 2015, 373(1): 48-59.

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