How does TAK-285 differ from lapatinib in terms of P-glycoprotein (Pgp) substrate activity?

Label:chem

Topic
P-glycoprotein (Pgp) is a major efflux transporter that limits the penetration of many drugs into the central nervous system (CNS). Lapatinib, a known HER2/EGFR inhibitor, is a substrate for Pgp, which restricts its efficacy in treating brain metastases.
Answer
Unlike lapatinib, TAK-285 is not a substrate for Pgp. This property allows TAK-285 to bypass the Pgp-mediated efflux mechanism, enabling it to penetrate the blood-brain barrier (BBB) and achieve higher concentrations in the CNS, making it more effective in treating brain metastases.
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