Degarelix (Firmagon)
Overview
Degarelix is a synthetic decapeptide gonadotropin-releasing hormone (GnRH) receptor antagonist used in the treatment of advanced prostate cancer. Unlike GnRH agonists, degarelix competitively blocks GnRH receptors in the anterior pituitary without causing an initial testosterone surge, achieving rapid suppression of luteinizing hormone and testosterone. This immediate pharmacological castration provides therapeutic benefit in androgen-dependent malignancies. The peptide consists of unnatural amino acids to resist enzymatic degradation and prolong activity.
Key Research Findings
Degarelix received FDA approval in 2008 based on phase 3 trials demonstrating non-inferiority to leuprolide in maintaining castrate testosterone levels, with superior suppression of follicle-stimulating hormone. A cardiovascular substudy published in BMJ Open (2014) suggested a potential advantage in reducing cardiovascular events compared to GnRH agonists, though this remains an area of ongoing investigation. The CS21 trial established its efficacy in maintaining testosterone suppression over 12 months.
Subcutaneous injection
FDA Approved
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