Relugolix: A Novel Gonadotropin-Releasing Hormone Antagonist for Prostate Cancer

ABSTRACT

Androgen deprivation therapy (ADT) is currently the mainstay of treatment for advanced prostate cancer. The peptide formulations of gonadotropin-releasing hormone (GnRH) antagonists need to be given subcutaneously every month. This led to the development of an oral, nonpeptide GnRH antagonist formulation relugolix which promptly lowers the levels of testosterone, luteinizing hormone, and follicular-stimulating hormone. On December 18, 2020, the US Food and Drug Administration approved relugolix for the treatment of adult advanced prostate cancer. The recommended loading dose of 360 mg on the 1st day of treatment, followed by 120 mg once daily orally, approximately the same time each day. The maximum plasma concentration (Tmax) is obtained within 2.25 h and is metabolized to a major extent by CYP3A mediated mechanism. Hot flushes, musculoskeletal pain, and fatigue are some of its common adverse effects. High rates of testosterone suppression with a limited adverse event profile make it an ideal therapy for the treatment of advanced prostate cancer.