relugolix + androgen receptor pathway inhibitor

Relugolix + androgen receptor pathway inhibitor (ARPI) is a combination therapy regimen being investigated for the treatment of metastatic hormone-sensitive prostate cancer (mHSPC). Relugolix is an orally administered, highly selective gonadotropin-releasing hormone (GnRH) receptor antagonist that rapidly suppresses testosterone production by blocking GnRH receptors in the anterior pituitary gland. ARPIs, a class of drugs including enzalutamide, apalutamide, darolutamide, and abiraterone acetate, work by either directly antagonizing the androgen receptor or inhibiting androgen biosynthesis. This combination is the focus of the OPTIMAS trial, a Phase II study led by the University of Utah, which evaluates the efficacy and safety of intermittent versus continuous administration of these agents in patients who achieve an optimal prostate-specific antigen (PSA) response. The use of relugolix in this setting is particularly notable due to its rapid testosterone recovery profile upon treatment cessation, which is advantageous for intermittent therapy strategies aimed at improving patient quality of life.

Brand names

Orgovyx

Other names

Relugolix + ARPIOPTIMAS regimen