abiraterone acetate + BEZ235

The combination of **abiraterone acetate** (an androgen biosynthesis inhibitor) and **BEZ235 (dactolisib)** (a dual pan-class I PI3K and mTORC1/2 inhibitor) was investigated for the treatment of metastatic castration-resistant prostate cancer (mCRPC). **Abiraterone acetate** blocks androgen biosynthesis by inhibiting CYP17A1, a key enzyme in steroidogenesis, thereby decreasing androgen production essential for tumor growth in prostate cancer. **BEZ235** inhibits PI3K and mTOR serine/threonine kinases, important in the PI3K-AKT-mTOR pathway frequently dysregulated in advanced prostate cancer. The rationale was to target both androgen signaling and a key compensatory growth/survival pathway, as these axes interact in resistance mechanisms. The combination, however, was poorly tolerated, resulting in frequent dose-limiting toxicities (including severe mucositis, hypotension, and pneumonitis) and was not developed further for prostate cancer[1][2][3].

Other names

abiraterone acetate and BEZ235abiraterone acetate plus BEZ235abiraterone + BEZ235