Peringatan Keamanan

Data regarding symptoms or treatment of afamelanotide overdose are currently unavailable.L9086

Afamelanotide

DB04931

small molecule approved investigational

Deskripsi

Afamelanotide is a first-in-class, synthetic, 13-amino acid peptide analogue of the endogenous alpha melanocyte-stimulating hormone (?-MSH).L9086 It differs structurally from its endogenous counterpart by only two amino acids - these structural differences improve biological efficacy by imparting a greater affinity for its target and a longer biological half-life.A187202,A187205 Afamelanotide is currently the only approved drug therapy used in the management of erythropoietic protoporphyria, having received approval in the EU in December 2014L9119 and subsequent FDA approval in October 2019.L9092 Despite its relatively recent approval, afamelanotide has been available for use as an orphan drug in both the US and EU since 2008.L9122,L9125

Struktur Molekul 2D

Berat 1646.8452
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half-life of afamelanotide is approximately 30 minutes.[L9086] The apparent half-life following administration of a slow-release subcutaneous implant is 15 hours.[L9134]
Volume Distribusi The apparent volume of distribution of afamelanotide following intravenous administration is approximately 0.54 L/kg.[A187202]
Klirens (Clearance) Data regarding plasma clearance of afamelanotide are limited. Plasma drug levels are typically undetectable at day 10 following subcutaneous administration of the afamelanotide implant.[L9086,A187205]

Absorpsi

Afamelanotide is administered as a subcutaneous implant that slowly elutes active drug. Most of the dose is released within the first 48 hours, with >90% released by day 5. Plasma levels of afamelanotide decrease slowly over the course of several days following administration - by day 10, plasma levels were undetectable in most clinical trial subjects.L9086 Following administration of a single subcutaneous implant, the median Tmax was 36 hours, the mean Cmax was 3.7 ± 1.3 ng/mL, and the mean AUC0-? was 138.9 ± 42.6 hr.ng/mL.L9134

Metabolisme

Details regarding the metabolism and metabolites of afamelanotide are sparse. The drug is more resistant to degradation by serum and proteolytic enzymes than its endogenous counterpart, ?-MSH, but presumably undergoes a relatively rapid hydrolysis given its short half-life.L9086,L9134 It has been suggested that afamelanotide may be degraded in the same manner as ?-MSH but at a much slower rate, or may instead be degraded intracellularly via endocytosis or non-specific proteases.A187202

Rute Eliminasi

Minimal amounts of unchanged afamelanotide are recovered in the urine following administration, suggesting the drug is extensively metabolized and most likely eliminated primarily via fecal or biliary route.A187202

Interaksi Obat

0 Data
Tidak ada data.

Target Protein

Melanocortin receptor 4 MC4R
Melanocyte-stimulating hormone receptor MC1R

Referensi & Sumber

Synthesis reference: Philippe Wolgen, "Alpha-MSH derivatives for the treatment of photodermatoses" E.U. Patent EP2865422A1, issued Oct. 18, 2017.
Artikel (PubMed)
  • PMID: 30704898
    Balwani M: Erythropoietic Protoporphyria and X-Linked Protoporphyria: pathophysiology, genetics, clinical manifestations, and management. Mol Genet Metab. 2019 Jan 24. pii: S1096-7192(18)30641-3. doi: 10.1016/j.ymgme.2019.01.020.
  • PMID: 28063031
    Minder EI, Barman-Aksoezen J, Schneider-Yin X: Pharmacokinetics and Pharmacodynamics of Afamelanotide and its Clinical Use in Treating Dermatologic Disorders. Clin Pharmacokinet. 2017 Aug;56(8):815-823. doi: 10.1007/s40262-016-0501-5.
  • PMID: 26979527
    Kim ES, Garnock-Jones KP: Afamelanotide: A Review in Erythropoietic Protoporphyria. Am J Clin Dermatol. 2016 Apr;17(2):179-85. doi: 10.1007/s40257-016-0184-6.

Contoh Produk & Brand

Produk: 3 • International brands: 0
Produk
  • Scenesse
    Implant • 16 mg/16mg • Subcutaneous • US • Approved
  • Scenesse
    Implant • 16 mg • Subcutaneous • EU • Approved
  • Scenesse
    Implant • 16 mg/16mg • Subcutaneous • US

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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