Drug intelligence / Profile preview

buparlisib + trastuzumab + paclitaxel

Development stage
Phase 2
Lead developer
Novartis
Modality
Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules, Antibody-Based Therapeutics
Administration
Oral, Intravenous
01

Overview

A **three-drug combination therapy** of buparlisib (an oral pan-class I PI3K inhibitor), trastuzumab (a monoclonal antibody against human epidermal growth factor receptor 2 or HER2), and paclitaxel (a taxane-class microtubule inhibitor chemotherapy), primarily investigated as a neoadjuvant or advanced/metastatic treatment for breast cancer, particularly HER2-positive subtypes. The regimen aims to inhibit cancer cell growth and survival via blockade of PI3K pathway signaling (buparlisib), HER2 receptor targeting (trastuzumab), and microtubule stabilization leading to mitotic arrest (paclitaxel). Early phase studies show feasibility of administration, but efficacy over standard combinations is not established in phase II/III trials[1][4][7].

Other names
BKM120 + paclitaxel + trastuzumabbuparlisib + paclitaxel + trastuzumab
02

Targets

PIK3CA (Phosphoinositide 3-kinase alpha)PIK3CB (Phosphatidylinositol 3-kinase beta subunit)PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)PIK3CD (Phosphatidylinositol 3-kinase delta)ERBB2 (Erb-b2 receptor tyrosine kinase 2)TUBB (Tubulin (alpha and beta subunits))

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