relugolix + enzalutamide

Relugolix + enzalutamide is a combination therapy under investigation for the treatment of advanced or metastatic prostate cancer, particularly hormone-sensitive and high-risk forms. Relugolix is an oral, nonpeptide gonadotropin-releasing hormone (GnRH) receptor antagonist that competitively binds to pituitary GnRH receptors, reducing the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), which in turn lowers testosterone production—a key driver of prostate cancer cell growth[5][1]. Enzalutamide is a second-generation androgen receptor inhibitor that blocks androgen binding to its receptor, inhibits androgen receptor nuclear translocation, and prevents DNA interaction required for oncogene activation[6][1]. The combination aims to achieve more complete suppression of androgen signaling than either agent alone. Clinical studies suggest this regimen is well tolerated and effective at maintaining castrate testosterone levels with stable PSA concentrations in patients with advanced prostate cancer[2][4][8].