Development of an In Vitro Platform for Screening UGT Inhibitors Using Human Liver Microsomes

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October 12,2024

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UGT-mediated conjugation with glucuronic acid （'glucuronidation'), derived from the cofactor UDP-glucuronic acid (UDPGA), is a major clearance pathway in phase II metabolism. In particular, after cytochromeP450 (CYP) mediated biotransformation, glucuronidation is the most important metabolic pathway for small molecule drugs1. With the release of the new ICH M12 guidelines, the screening of UGT inhibitors is becoming increasingly important in drug development. Therefore, the objective of this study is to meet the need for the implementation of accurate and cost-effective high-throughput in vitro methods.

Development of an In Vitro Platform for Screening UGT Inhibitors Using Human Liver Microsomes

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