buparlisib

Overview

Buparlisib (BKM-120) is an oral pan-class I PI3K inhibitor targeting PIK3CA, PIK3CB, PIK3CD, and PIK3CG. It was investigated clinically across multiple solid tumors but did not reach regulatory approval due to toxicity concerns (CNS effects, hepatotoxicity).

Evidence in the corpus

• AR-amplified MSK-PCa2 CRPC patient-derived organoid (PTEN loss + PIK3R1 mutation) was sensitive to buparlisib (BKM-120) in vitro; results support pan-PI3K inhibition as an approach in CRPC with PI3K-pathway co-activation alongside AR amplification PMID:25201530
• Nominated as a candidate PI3K-pathway therapy for the 4% of pancreatic ductal adenocarcinomas carrying activating PIK3CA mutations (mutually exclusive with KRAS), identified by WES of 109 resected PDA cases PMID:25855536

Resistance mechanisms

None yet recorded.

Cancer types (linked)

• PRAD — castration-resistant prostate cancer (CRPC); PI3K-pathway-altered subtype

Sources

• PMID:25201530

This page was processed by crosslinker on 2026-05-14. - PMID:25855536

This page was processed by crosslinker on 2026-05-14.