Cetrorelix pamoate

Cetrorelix pamoate is a synthetic decapeptide and a potent gonadotropin-releasing hormone (GnRH) receptor antagonist. Developed by AEterna Zentaris, this specific pamoate salt formulation was designed as a sustained-release intramuscular injection for the treatment of hormone-dependent conditions, primarily benign prostatic hypertrophy (BPH). The drug works by competitively binding to GnRH receptors in the pituitary gland, which rapidly and reversibly suppresses the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This suppression leads to a significant reduction in serum testosterone levels, which was hypothesized to reduce prostate volume and improve lower urinary tract symptoms in men with BPH. Although it reached Phase 3 clinical testing in the Z-036 and Z-041 trials, development for BPH was ultimately terminated after the studies failed to meet their primary efficacy endpoints.

Brand names

Cetrotide

Other names

CetrorelixCetrorelix pamoate