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The use of a high-throughput luminescent method to assess CYP3A enzyme induction in cultured rat hepatocytes
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In Vitro Cellular & Developmental Biology
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May 1, 2008
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Copyright informationCopyright Society for In Vitro Biology May/Jun 2008. Provided by ProQuest LLC. (Hide copyright information)
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Abstract Assessment of a new chemical entity for cytochrome P450 (CYP) enzyme induction at an early stage in discovery is crucial to prevent potential drug-drug interactions. CYP3A, the most abundant CYP isoform in the liver, metabolizes approximately 50% of drugs currently on the market and is also a highly inducible enzyme. The use of both rat and human hepatocyte culture for the prediction of in vivo CYP3A induction has become refined and validated and is considered a standard in vitro model. The current evaluation of CYP3A enzyme induction involves the use of substrates requiring subsequent analysis of metabolites by high-performance liquid chromatography/ mass spectrometry, which adds ...
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