Afamelanotide

{{Drugbox | verifiedfields = changed | verifiedrevid = 477002091 | IUPAC_name = Acetyl-N-[[2-(1H-indol-3-yl)ethyl]carbamoyl]-L-histidyl-L-phenylalanyl-L-arginyl-L-tryptophyl-L-lysyl-L-prolyl-L-valinamide | image = Melanotan.png | image2 = | tradename = Scenesse | Drugs.com = | pregnancy_AU = | pregnancy_US = | legal_AU = | legal_CA = | legal_UK = | legal_US = | routes_of_administration = Subcutaneous | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number = 75921-69-6 | ATC_prefix = D02 | ATC_suffix = BB02 | PubChem = 16132342 | DrugBank = DB04908 | ChemSpiderID = 17286782 | UNII = 1YB13M08QJ | KEGG = D03252 | ChEBI = 131721 | ChEMBL = 2103870 | synonyms = NDP-MSH, Melanotan I }}

Afamelanotide is a synthetic peptide analogue of the naturally occurring alpha-Melanocyte-stimulating hormone (α-MSH). It is primarily used in the treatment of certain skin disorders, particularly erythropoietic protoporphyria (EPP), a rare genetic condition that causes severe photosensitivity.

Mechanism of Action

Afamelanotide works by mimicking the action of α-MSH, which binds to the melanocortin 1 receptor (MC1R) on melanocytes. This binding stimulates the production of eumelanin, a type of melanin that provides photoprotection by absorbing ultraviolet (UV) radiation and reducing the risk of DNA damage. By increasing eumelanin levels, afamelanotide helps to protect the skin from UV-induced damage, thereby reducing the symptoms of photosensitivity in patients with EPP.

Clinical Use

Afamelanotide is marketed under the brand name Scenesse and is administered as a subcutaneous implant. It is approved for use in the European Union and the United States for the prevention of phototoxicity in adult patients with EPP. The implant is typically inserted into the skin every two months, providing a sustained release of the drug.

Side Effects

Common side effects of afamelanotide include nausea, headache, and fatigue. Some patients may also experience skin darkening, which is a direct result of increased melanin production. Serious side effects are rare but can include allergic reactions and implant site reactions.

Research and Development

Afamelanotide was initially developed as a potential tanning agent due to its ability to increase melanin production. However, its development shifted towards therapeutic applications for skin disorders. Ongoing research is exploring its potential use in other conditions, such as vitiligo and polymorphous light eruption.

Related Pages

• Melanocyte-stimulating hormone
• Melanocortin receptor
• Erythropoietic protoporphyria
• Photosensitivity