abiraterone acetate + BKM120

**abiraterone acetate + BKM120** is an experimental combination therapy for **metastatic castration-resistant prostate cancer (mCRPC)**. **Abiraterone acetate** is an androgen biosynthesis inhibitor targeting the androgen receptor signaling axis, while **BKM120** (buparlisib) is a pan-class I phosphatidylinositol 3-kinase (PI3K) inhibitor. The rationale behind this combination is to simultaneously inhibit the androgen receptor and PI3K pathways, which are known to exhibit reciprocal feedback and cross-regulation in prostate cancer, especially in PTEN-deficient contexts. This dual targeting is hypothesized to overcome resistance mechanisms seen with AR inhibition alone. The combination has been investigated in early-phase clinical trials but was limited by tolerability concerns, with significant toxicities observed and studies terminated early due to safety reasons[5][2][1].

Other names

abiraterone + buparlisib