What is the role of TAK-285 in inhibiting HER2 and EGFR kinases?

Label:chem

Topic
TAK-285 is a novel, investigational dual EGFR/HER2 kinase inhibitor designed to target human epidermal growth factor receptor 2 (HER2) and epidermal growth factor receptor (EGFR). These receptors are often overexpressed in various cancers, including breast and lung cancers, and are associated with poor prognosis.
Answer
TAK-285 demonstrates high specificity for inhibiting HER2 and EGFR kinases, with IC50 values of 17 nmol/L for HER2 and 23 nmol/L for EGFR. It shows strong inhibitory activity against HER family kinases and is not a substrate for P-glycoprotein (Pgp) efflux, allowing it to penetrate the central nervous system (CNS) effectively.
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