Humanization of SLCO2B1 in rats increases rCYP3A1 protein expression but not the metabolism of erlotinib to OSI-420 [Metabolism, Transport, and Pharmacogenetics]
ASPET
MARCH 6, 2024
A first pharmacological phenotyping with the OATP2B1 substrate-drug atorvastatin revealed reduced hepatic content and increased expression of rCYP3A1 in the humanized animals. Western blot analysis of rat liver lysates and microsomes confirmed higher rCYP3A1 protein expression in untreated SLCO2B1 +/+ compared to Slco2b1 -/ - rats.
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