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LJM716 + alpelisib + trastuzumab

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

Overview

A combination therapy consisting of LJM716 (anti-HER3 monoclonal antibody), alpelisib (BYL719, PI3K inhibitor), and trastuzumab (anti-HER2 monoclonal antibody). This triple combination targets multiple aspects of HER family signaling pathways in HER2-overexpressing cancers. LJM716 binds to HER3 and traps it in an inactive conformation, preventing heterodimer formation with other HER family receptors. Alpelisib is a PI3K inhibitor that targets downstream signaling. Trastuzumab binds to the extracellular domain of HER2, blocking receptor signaling and inducing antibody-dependent cell-mediated cytotoxicity.

Brand names: PiqrayHerceptin
Other names: BYL719 + LJM716 + trastuzumab

Targets

ERBB3 (Erb-b2 receptor tyrosine kinase 3)PIK3CA (Phosphoinositide 3-kinase alpha)ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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