Drug intelligence / Profile preview

buparlisib + carboplatin

Development stage
Phase 1
Lead developer
Adlai Nortye
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Buparlisib (BKM120) plus carboplatin is an investigational combination therapy studied primarily in advanced solid tumors. Buparlisib is an orally available pan-class I phosphatidylinositol-3-kinase (PI3K) inhibitor that targets all class IA PI3K paralogues (p110α, β, and δ), disrupting the PI3K/AKT signaling pathway involved in cancer cell growth and survival. Carboplatin is a platinum-based chemotherapeutic agent that induces DNA crosslinking and apoptosis in rapidly dividing cells. The rationale for combining these agents is based on preclinical evidence that PI3K inhibition can sensitize tumor cells to platinum-based chemotherapy. This combination has been evaluated in phase I clinical trials for patients with advanced solid tumors to determine safety, tolerability, and recommended dosing[1][2]. Preliminary results indicate manageable toxicity and some antitumor activity.

Other names
BKM120 + carboplatinbuparlisib + carboplatin
02

Targets

DNAPIK3CB (Phosphatidylinositol 3-kinase beta subunit)PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)TUBB (Tubulin (alpha and beta subunits))PIK3CA (Phosphoinositide 3-kinase alpha)PIK3CD (Phosphatidylinositol 3-kinase delta)

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