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buparlisib + carboplatin + paclitaxel
- Development stage
- Phase 1
- Lead developer
- Adlai Nortye
- Modality
- Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Oral, Intravenous
01
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
02
Targets
DNAPIK3CA (Phosphoinositide 3-kinase alpha)PIK3CB (Phosphatidylinositol 3-kinase beta subunit)PIK3CD (Phosphatidylinositol 3-kinase delta)PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)TUBB (Tubulin (alpha and beta subunits))
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