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1. What is Degarelix? Degarelix powder is used for the treatment of advanced prostate cancer. It sold under the brand name Firmagon among others. Degarelix powder (214766-78-6) is a synthetic peptide derivative powder, degarelix peptide sequence is Ac-D2Nal-D4Cpa-D3Pal-Ser-4Aph(L-Hor)-D4Aph(Cbm)-Leu-Lys(Ipr)-Pro-DAla-NH2. Degarelix binds to gonadotropin-releasing hormone (GnRH) receptors in the pituitary gland and blocks interaction with GnRH. This antagonism reduces luteinising hormone (LH) and follicle-stimulating hormone (FSH) which ultimately causes testosterone suppression. Reduction in testosterone is important in treating men with advanced prostate cancer.
2. Degarelix mechanism of action Degarelix is a GnRH antagonist. In general, an antagonist drug blocks the receptor by binding to it and counteracts its function.
Degarelix inhibits GnRH from binding to its receptors and stops the release of gonadotropin. By blocking the GnRH receptors, degarelix inhibits the sex hormones' activity and decreases the production of testosterone. Since testosterone stimulates the growth of prostate cancer, the reduction of testosterone improves the prognosis of prostate cancer and decreases its size.
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