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Humanization of SLCO2B1 in rats increases rCYP3A1 protein expression but not the metabolism of erlotinib to OSI-420 [Metabolism, Transport, and Pharmacogenetics]

ASPET

Western blot analysis of rat liver lysates and microsomes confirmed higher rCYP3A1 protein expression in untreated SLCO2B1 +/+ compared to Slco2b1 -/ - rats. The contrary was observed, when microsomes isolated from treatment naive animals were assessed for the OSI-420 formation after erlotinib exposure.