Afamelanotide acetate

Uses

Afamelanotide promotes skin pigmentation and provides protection from the sun. In dermatology, afamelanotide appears to be effective in treating polymorphic light eruption, solar urticaria, erythropoietic protoporphyria (EPP), Heili-Heili disease, vitiligo, and acne vulgaris. Afamelanotide may also be used non-medically to achieve quick and easy skin tanning^[2].

General Description

Afamelanotide, a synthetic α-melanocyte stimulating hormone analog and first-in-class melanocortin-1 receptor agonist, has been approved in the EU for the prevention of phototoxicity in adults with erythropoietic protoporphyria (EPP)^[1].

Side effects

Common adverse reactions to afamelanotide include headache and implant site reactions. Other adverse reactions include the development and aggravation of melanocytic nevi, degeneration of melanocytic nevi into melanoma, dark spots, systemic toxicity, rhabdomyolysis, posterior reversible encephalopathy syndrome, acromegaly, and oral soft tissue pigmentation. In addition, dentists should be alert to oral soft tissue pigmentation caused by afamelanotide^[2].

IC 50

MC1R

References

[1] ESTHER S. KIM; Karly P G J. Afamelanotide: A Review in Erythropoietic Protoporphyria[J]. American Journal of Clinical Dermatology, 2016, 17 2: 179-185. DOI:10.1007/s40257-016-0184-6.
[2] C DE BAAT. [Medicaments and oral healthcare. Hyperpigmentation of oral soft tissues due to afamelanotide].[J]. Nederlands tijdschrift voor tandheelkunde, 2020, 127 4: 237-243. DOI:10.5177/ntvt.2020.04.19115.
[3] HASKELLLUEVANO C. Binding and cAMP Studies of Melanotropin Peptides with the Cloned Human Peripheral Melanocortin Receptor, hMC1R[J]. Biochemical and biophysical research communications, 1994, 204 3: Pages 1137-1142. DOI: 10.1006/bbrc.1994.2581
[4] T K SAWYER. 4-Norleucine, 7-D-phenylalanine-alpha-melanocyte-stimulating hormone: a highly potent alpha-melanotropin with ultralong biological activity.[J]. Proceedings of the National Academy of Sciences of the United States of America, 1980, 77 10: 5754-5758. DOI: 10.1073/pnas.77.10.5754
[5] MAC E. HADLEY. Calcium-Dependent Prolonged Effects on Melanophores of [4-Norleucine, 7-D-Phenylalanine]-α-Melanotropin[J]. Science, 1981, 213 4511. DOI: 10.1126/science.6973820