Degarelix is a gonadotropin-releasing hormone (GnRH) antagonist used primarily in the treatment of advanced hormone-dependent prostate cancer. Unlike GnRH agonists, degarelix provides a rapid suppression of testosterone without an initial surge, making it preferable for patients where immediate androgen deprivation is necessary.
It is administered as a subcutaneous injection in a monthly depot formulation.
Indications include:
∙ Advanced prostate cancer
∙ Off-label: Hormonal suppression in transgender care (under supervision)
Parent: Degarelix
As a synthetic decapeptide, degarelix is produced through solid-phase peptide synthesis (SPPS), where impurities can arise from incomplete coupling, deprotection, or degradation. Due to its parenteral administration and use in long-term therapy, stringent impurity control is required under ICH Q3A/B and peptide-specific guidelines.
Process-Related Impurities
Degradation Impurities
Elemental Impurities
Analytical Techniques for Impurity Detection
Degarelix is used for testosterone suppression in men with advanced prostate cancer, helping slow tumor growth and progression.
It blocks GnRH receptors in the pituitary gland, leading to immediate suppression of luteinizing hormone (LH) and testosterone production from the testes.
Degarelix should be stored refrigerated at 2–8°C, protected from light, and reconstituted only before use with appropriate diluent.
Degarelix provides a faster reduction in testosterone without the initial hormone surge (flare) seen with agonists, making it suitable for high-risk cases.
