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Afamelanotide
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Afamelanotide
Afamelanotide, sold under the brand name Scenesse, is a medication used to prevent phototoxicity and to reduce pain from light exposure for people with erythropoietic protoporphyria. It is a melanocortin 1 receptor (MC1 receptor) agonist and a synthetic peptide and analogue of α-melanocyte stimulating hormone. It is administered as subcutaneous implant.
The US Food and Drug Administration (FDA) considers it to be a first-in-class medication.
In the European Union, afamelanotide is indicated for the prevention of phototoxicity in adults with erythropoietic protoporphyria.
In the United States, afamelanotide is indicated for increasing pain-free light exposure in adults with a history of reactions to light (phototoxicity) from erythropoietic protoporphyria.
Very common adverse effects include nausea and headache (may affect more than 10% of people). Common adverse effects include injection site reactions, back pain, upper respiratory tract infections, melanocyte naevus, decreased appetite, migraine, dizziness, weakness, fatigue, lethargy, sleepiness, hot flashes, abdominal pain, diarrhea, vomiting, flushing, development of warts, spots, and freckles, and itchy skin (between 1% and 10% of people). Uncommon and rare adverse effects include cystitis, folliculitis, gastrointestinal infections, hypersensitivity reactions, changes in appetite, depression, insomnia, balance disorders, lethargy, restless leg syndrome, syncope, photophobia, presbyopia, tinnitus, confusion, palpitations, hypertension, hypercholesterolaemia, and weight gain.
Afamelanotide is a synthetic tridecapeptide and a structural analogue of α-melanocyte stimulating hormone (α-MSH). It is a melanocortin receptor agonist and binds predominantly to the MC1 receptor. Its binding lasts longer than that of α-MSH. This results in part from afamelanotide's resistance to immediate degradation by serum or proteolytic enzymes. It is thought to cause skin darkening by binding to the MC1 receptor which in turn drives melanogenesis.
It has a short half-life of approximately 30 minutes. After administration with implantation into the skin, the majority of the drug is released within two days, with 90% released by the fifth day. By the tenth day, no drug is detectable in plasma.
Drug distribution, metabolism and excretion were not understood as of 2017.
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Afamelanotide
Afamelanotide, sold under the brand name Scenesse, is a medication used to prevent phototoxicity and to reduce pain from light exposure for people with erythropoietic protoporphyria. It is a melanocortin 1 receptor (MC1 receptor) agonist and a synthetic peptide and analogue of α-melanocyte stimulating hormone. It is administered as subcutaneous implant.
The US Food and Drug Administration (FDA) considers it to be a first-in-class medication.
In the European Union, afamelanotide is indicated for the prevention of phototoxicity in adults with erythropoietic protoporphyria.
In the United States, afamelanotide is indicated for increasing pain-free light exposure in adults with a history of reactions to light (phototoxicity) from erythropoietic protoporphyria.
Very common adverse effects include nausea and headache (may affect more than 10% of people). Common adverse effects include injection site reactions, back pain, upper respiratory tract infections, melanocyte naevus, decreased appetite, migraine, dizziness, weakness, fatigue, lethargy, sleepiness, hot flashes, abdominal pain, diarrhea, vomiting, flushing, development of warts, spots, and freckles, and itchy skin (between 1% and 10% of people). Uncommon and rare adverse effects include cystitis, folliculitis, gastrointestinal infections, hypersensitivity reactions, changes in appetite, depression, insomnia, balance disorders, lethargy, restless leg syndrome, syncope, photophobia, presbyopia, tinnitus, confusion, palpitations, hypertension, hypercholesterolaemia, and weight gain.
Afamelanotide is a synthetic tridecapeptide and a structural analogue of α-melanocyte stimulating hormone (α-MSH). It is a melanocortin receptor agonist and binds predominantly to the MC1 receptor. Its binding lasts longer than that of α-MSH. This results in part from afamelanotide's resistance to immediate degradation by serum or proteolytic enzymes. It is thought to cause skin darkening by binding to the MC1 receptor which in turn drives melanogenesis.
It has a short half-life of approximately 30 minutes. After administration with implantation into the skin, the majority of the drug is released within two days, with 90% released by the fifth day. By the tenth day, no drug is detectable in plasma.
Drug distribution, metabolism and excretion were not understood as of 2017.
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