relugolix + abiraterone + prednisone

**Relugolix + abiraterone + prednisone** is a triple oral combination regimen under investigation for the treatment of advanced prostate cancer. - **Relugolix** is an oral small molecule antagonist of the gonadotropin-releasing hormone (GnRH) receptor, leading to rapid suppression of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), thereby reducing testosterone production to castrate levels. - **Abiraterone** is a small molecule inhibitor of cytochrome P450 17A1 (CYP17A1), preventing androgen biosynthesis in the testes, adrenal glands, and prostate tumor tissue. - **Prednisone** is a synthetic glucocorticoid corticosteroid co-administered to manage side effects of abiraterone, such as mineralocorticoid excess, and to provide additional anti-inflammatory effects. Combination therapy of androgen deprivation (relugolix) with androgen biosynthesis inhibition (abiraterone) and glucocorticoid (prednisone) targets two key mechanisms in prostate cancer progression, improving clinical outcomes in both metastatic castration-sensitive and castration-resistant prostate cancer. Clinical trials show the regimen is generally well tolerated, with adverse event profiles consistent with those of the individual drugs. Studies specifically validate sustained testosterone suppression and disease control when switching from standard ADT approaches to oral relugolix. The therapy is being developed and investigated by the manufacturers of the constituent agents, and recommended in practice guidelines as a therapeutic strategy for advanced prostate cancer[1][2][3][4].