GSK525762 + abiraterone

GSK525762 + abiraterone is a combination of two investigational drugs primarily studied for metastatic castrate-resistant prostate cancer (mCRPC) in individuals who have progressed after prior androgen deprivation or androgen receptor–targeted therapies. GSK525762 (also known as molibresib) is an oral small-molecule pan-bromodomain and extraterminal (BET) inhibitor. BET proteins, particularly BRD4, cooperate with the androgen receptor (AR) to drive transcriptional programs crucial for prostate cancer cell growth and proliferation. GSK525762 suppresses BET-dependent, AR-driven transcription. Abiraterone is a CYP17A1 inhibitor that suppresses androgen biosynthesis, thereby lowering androgen levels and impeding AR signaling. The combination is hypothesized to overcome resistance to AR-directed therapies or enhance their efficacy by targeting parallel and complementary signaling axes in prostate cancer cells. The drug combination has undergone Phase 1 studies to determine safety, tolerability, pharmacokinetics, and early clinical activity, especially for patients who failed abiraterone or enzalutamide[1][3][5].

Brand names

none

Other names

molibresib + abiraterone