Drug intelligence / Profile preview

alpelisib + pertuzumab + trastuzumab

Development stage: Unknown
Lead developer: Novartis
Modality: Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration: Oral, Intravenous

Overview

A combination therapy consisting of alpelisib (an α-specific PI3K inhibitor), pertuzumab (a HER2-targeted monoclonal antibody), and trastuzumab (a HER2-targeted monoclonal antibody). This combination targets multiple pathways in HER2-positive breast cancer, particularly in tumors harboring PIK3CA mutations. The rationale is based on evidence that PIK3CA mutations confer resistance to HER2-targeted therapy, but single-agent PI3K blockade might be compromised by feedback inhibition which can be overcome by concurrent HER2 and HER3 blockade.

Targets

PIK3CA (Phosphoinositide 3-kinase alpha)ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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