Degarelix (trade name Firmagon) is a synthetic decapeptide and a gonadotropin-releasing hormone (GnRH) receptor antagonist. Unlike GnRH agonists, it blocks the receptor directly and does not trigger an initial testosterone surge (flare). It is an approved prescription medicine for the treatment of advanced, hormone-dependent prostate cancer. This page neutrally summarizes the evidence base and legal status and is not a usage or dosing recommendation.
Degarelix is a competitive GnRH receptor antagonist. It binds reversibly and immediately to the pituitary GnRH receptors and blocks their activation. This rapidly suppresses the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), which in turn lowers testosterone production in the testes. Unlike GnRH agonists (e.g., leuprorelin), which first cause a transient stimulation with a testosterone surge (flare), this direct antagonism lacks the initial stimulation phase, so testosterone declines without a preceding rise. This mechanism underlies the literature-described use in hormone-dependent prostate cancer.
Theoretische concentratiecurve bij een halfwaardetijd van 1320 h. Puur farmacokinetisch model — geen doseringsaanbeveling.
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