Degarelix (214766-78-6) video
Degarelix (214766-78-6) Description
Degarelix, also known as Degarelix acetate and FE-200486, a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR) antagonist. It binds reversibly to the pituitary GnRH receptors, thereby reducing the release of gonadotropins and consequently testosterone. Degarelix is specifically indicated for the treatment of advanced prostate cancer.
Degarelix is supplied as a powder to be reconstituted with sterile water for subcutaneous administration in the abdomen. The recommended initial dose of the drug is 240 mg given as two subcutaneous injections of 120 mg at a concentration of 40 mg/mL. The recommended maintenance dose of Degarelix is 80 mg given as one subcutaneous injection at a concentration of 20 mg/mL, every 28 days. Chemically, it is a synthetic linear decapeptide amide with seven unnatural amino acids, five of which are D-amino acids. FDA approved on December 24, 2008.
Degarelix (214766-78-6) Specifications
|Chemical Name||Degarelix acetate; FE-200486; UNII-SX0XJI3A11; SX0XJI3A11; CS-5350; Z-3147; CHEMBL415606; Ac-D-Nal-[D-(pCl)Phe]-D-Pal-Ser-[Aph(DHor)]-D-[Aph(Cbm)]-Leu-ILys-Pro-DAla-NH2;|
|Drug Class||Antineoplastic Agents|
|Monoisotopic Mass||1630.75 g/mol g·mol−1|
|Biological Half-Life||23~61 days|
|Color||White to off-white solid powder|
|Solubility||H2O: ≥ 500 mg/mL|
|Application||Used to treat patients with advanced prostate cancer|