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alpelisib + paclitaxel
- Development stage
- Unknown
- Lead developer
- Novartis
- Modality
- Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
- Administration
- Oral, Intravenous
01
Overview
Alpelisib (BYL719) is an oral small molecule inhibitor that selectively targets the phosphoinositide 3-kinase catalytic subunit alpha (PI3Kα), encoded by the PIK3CA gene. Paclitaxel is a microtubule-stabilizing chemotherapeutic agent. The combination of alpelisib and paclitaxel (including its albumin-bound formulation nab-paclitaxel) has been investigated for synergistic antitumor activity in advanced solid tumors—particularly breast cancer and gastric cancer with PIK3CA mutations or PTEN loss. Alpelisib inhibits PI3Kα signaling to block tumor cell proliferation and survival pathways; when combined with paclitaxel’s cytotoxic effects on dividing cells via microtubule stabilization, this regimen aims to enhance efficacy over either agent alone. Clinical studies have shown encouraging response rates and manageable safety profiles for this combination in patients with advanced or metastatic HER2-negative breast cancer and other solid tumors[1][2][5][10].
- Brand names
- Piqray
- Other names
- BYL719 + paclitaxelalpelisib + paclitaxelBYL719 plus paclitaxelBYL-719 plus paclitaxelBYL 719 plus paclitaxelalpelisib plus paclitaxelBYL719 + nab-paclitaxelalpelisib + nab-paclitaxel
02
Targets
PIK3CA (Phosphoinositide 3-kinase alpha)TUBB (Tubulin (alpha and beta subunits))
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