Relugolix: A Review in Advanced Prostate Cancer

Area of Science:

• Oncology
• Endocrinology
• Pharmacology

Background:

• Advanced prostate cancer treatment often involves androgen deprivation therapy (ADT).
• Gonadotropin-releasing hormone (GnRH) receptor antagonists offer an alternative to traditional ADT methods.
• Relugolix is an oral GnRH antagonist developed for advanced prostate cancer.

Purpose of the Study:

• To evaluate the efficacy and safety of oral relugolix compared to leuprolide in men with advanced prostate cancer.
• To assess the rate and sustainability of testosterone suppression with relugolix.

Main Methods:

• The pivotal Phase III HERO trial involved men with advanced prostate cancer.
• Participants received once-daily oral relugolix with a loading dose or intramuscular leuprolide every 3 months.
• Efficacy was measured by sustained castration rate over 48 weeks.

Main Results:

• Relugolix achieved a sustained castration rate of over 90% at 48 weeks, demonstrating non-inferiority to leuprolide.
• An exploratory analysis suggested potential superiority of relugolix over leuprolide.
• Relugolix was well-tolerated, with an adverse event profile consistent with testosterone suppression.
• Relugolix may be associated with a lower risk of major adverse cardiac events compared to leuprolide.

Conclusions:

• Oral relugolix provides rapid and sustained testosterone suppression for advanced prostate cancer.
• Relugolix offers advantages including oral administration, no initial testosterone surge, and potentially improved cardiac safety.
• Relugolix represents a valuable oral treatment option for advanced prostate cancer requiring ADT.