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buparlisib + carboplatin + paclitaxel

Development stage: Unknown
Lead developer: Adlai Nortye
Modality: Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration: Oral, Intravenous

Overview

A combination regimen consisting of **buparlisib** (an oral pan-class I phosphatidylinositol-3-kinase [PI3K] inhibitor), **carboplatin** (a platinum-based chemotherapy agent), and **paclitaxel** (a microtubule-stabilizing chemotherapeutic agent). Buparlisib inhibits the PI3K/AKT signaling pathway, sensitizing tumor cells to platinum/taxane-based chemotherapy. Carboplatin induces DNA crosslinking and apoptosis, while paclitaxel disrupts microtubule function, arrests cell division, and causes apoptosis. This combination has been investigated in phase I trials for advanced solid tumors, including ovarian, lung, salivary gland, and nasopharyngeal cancers, especially in patients with PTEN loss, and is notable for its tolerability and preliminary clinical activity[1][3].

Other names: buparlisib + carboplatin + paclitaxelBKM120 + carboplatin + paclitaxel

Targets

PIK3CA (Phosphoinositide 3-kinase alpha)DNAPIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)PIK3CB (Phosphatidylinositol 3-kinase beta subunit)PIK3CD (Phosphatidylinositol 3-kinase delta)TUBB (Tubulin (alpha and beta subunits))

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