Degarelix

Degarelix is a gonadotropin-releasing hormone receptor antagonist used for the treatment of advanced hormone-dependent prostate cancer in adult men. By binding to GnRH receptors in the pituitary, it rapidly suppresses luteinizing hormone and follicle-stimulating hormone secretion, lowering testosterone to castration levels without the initial testosterone surge seen with GnRH agonists.

Degarelix is a synthetic peptide administered by subcutaneous injection. The recommended regimen begins with a loading dose of 240 mg, followed by 80 mg given subcutaneously every 28 days. It provides rapid testosterone suppression, typically reaching castration levels within a few days and maintaining suppression with regular dosing.

Clinical studies indicate that degarelix achieves comparable reductions in testosterone and PSA and similar progression-free outcomes to GnRH agonists, while avoiding a flare in testosterone at treatment initiation. It may be preferred in patients where testosterone flare would be detrimental.

Common adverse effects include hot flashes, sweating, injection-site reactions, weight gain, edema, and reduced sexual function. Hepatic safety concerns on rare occasions include elevations of liver enzymes and cholestasis; liver function tests should be monitored before and during treatment. Other safety considerations include hypersensitivity reactions and potential cardiovascular events, though incidence is not clearly higher than with other androgen-deprivation therapies. Degarelix is approved for adult men with advanced hormone-dependent prostate cancer; it is not indicated for women or pediatric patients. Brand-name formulations include Firmagon in many markets.