Drug intelligence / Profile preview

alpelisib + tucatinib

Development stage: Unknown
Lead developer: Criterium
Modality: Small Molecules
Administration: Oral

Overview

Alpelisib + tucatinib is a combination therapy targeting both PI3K and HER2 pathways in cancer cells. Alpelisib is a PI3K inhibitor specifically targeting the alpha catalytic subunit of PI3K, while tucatinib is a tyrosine kinase inhibitor that selectively targets HER2. This combination is being investigated primarily for HER2-positive metastatic breast cancer with PIK3CA mutations, which are present in approximately 30% of HER2-positive tumors and linked to drug resistance and decreased survival. The combination aims to overcome resistance mechanisms to HER2-targeted therapies by simultaneously inhibiting the PI3K pathway.

Brand names: TukysaPiqray

Targets

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

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