Metabolic Activation of the Acrylamide Michael Acceptor Warhead in Futibatinib to an Epoxide Intermediate Engenders Covalent Inactivation of CYP3A
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DOI: 10.1124/dmd.122.000895
Abstract: Futibatinib (FUT) is a potent inhibitor of fibroblast growth factor receptor (FGFR) 1–4 that is currently under clinical investigation for intrahepatic cholangiocarcinoma. Unlike its predecessors, FUT possesses an acrylamide warhead, which enables it to bind… read more here.
Keywords: cyp3a; inactivation cyp3a; epoxide; covalent inactivation ... See more keywords