Degarelix
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.
Mechanism of action
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.
L'evidenza in sintesi
Cosa mostrano gli studi
Dove gli studi divergono
Does the GnRH antagonist degarelix lower cardiovascular risk compared with GnRH agonists?
Farmacocinetica
Curva teorica di concentrazione con un'emivita di 1320 h. Modello puramente farmacocinetico — non una raccomandazione di dose.
Open in PK tool →Vie di somministrazione nella letteratura
Uso più sicuro e rischi
Eventi avversi noti dagli studi
Interazioni e combinazioni
Osservazioni aneddotiche
Di cosa si discute nelle comunità online
Stato legale per paese
Calcolatore di ricostituzione
I peptidi arrivano come polvere secca. Una volta disciolti in un liquido (ricostituzione), questo calcolatore risponde a una sola domanda: quanta sostanza c'è in un millilitro di soluzione dopo?
- 1Inserisci la quantità di sostanza del flacone (riportata sull'etichetta).
- 2Inserisci quanto solvente aggiungi.
- 3Risultato = concentrazione in mg per mL.
Registro degli studi
The efficacy and safety of degarelix: a 12-month, comparative, randomized, open-label, parallel-group phase III study in patients with prostate cancer
Additional analysis of the secondary end point of biochemical recurrence rate in a phase 3 trial (CS21) comparing degarelix 80 mg versus leuprolide in prostate cancer patients segmented by baseline characteristics
The effect of baseline testosterone on the efficacy of degarelix and leuprolide: further insights from a 12-month, comparative, phase III study in prostate cancer patients
Cardiovascular morbidity associated with gonadotropin releasing hormone agonists and an antagonist
Fonti e metodologia
Ricevi nuovi studi su Degarelix
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