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.
Теоретическая кривая концентрации при периоде полувыведения 1320 h. Чисто фармакокинетическая модель — не рекомендация по дозировке.
Open in PK tool →Пептиды поставляются в виде сухого порошка. После растворения в жидкости (восстановление) этот калькулятор отвечает на единственный вопрос: сколько вещества содержится в одном миллилитре раствора после этого?
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