Titlebook: Cytochrome P450; In Vitro Methods and Zhengyin Yan,Gary W. Caldwell Book 2021 The Editor(s) (if applicable) and The Author(s), under exclus

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Annual Report on China’s Economic Growthy and development of new drugs, metabolic inhibitor drug interactions are important to consider since they can produce adverse effects. A robust LC/MS-based cytochrome P450 (CYP) inhibition assay using human liver microsomes has been fully developed and validated for major human CYPs, which could pr

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Current Chinese Economic Report Seriesor drug–drug interactions (DDIs). DDIs occur when one drug affects the metabolism of a coadministered drug. This changes the exposure and clearance of a coadministered drug. The consequences are a risk of therapeutic efficacy of a drug to severe adverse drug reactions, leading to death. Thus, it is

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Current Chinese Economic Report Seriesl to produce DDIs. Experiments can be designed that recognize such entities by assessing receptor transactivation in cell-based systems and monitoring reporter gene activity. These in vitro assays have several advantages; activation of a specific nuclear receptor (NR) can be determined, there is a h

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Guanhua Wang,Zhuo Fang,Xiaoyuan Xia in vitro liver model that resembles in vivo microenvironment with improved predictive capabilities is highly desirable. Historically, two-dimensional (2D) primary human hepatocyte (PHH) cultures have been used for the in vitro system to test a compound’s ability to induce or suppress cytochrome P45

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https://doi.org/10.1007/978-981-99-7289-0m of a drug molecule is one way that a drug candidate can fail. Since most small molecules are metabolized by the liver, the enzymes in the liver need to be heavily accounted for. The majority of these enzymes are cytochrome P450 (CYP), and therefore screening compounds for activity with CYPs is nec

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Yiming Yuan,Zhenkun Yan,Xuan Litochrome P450 (CYP)-mediated metabolism. Therefore, hepatic clearance is undeniably one of the most critical pharmacokinetic parameters. In the early stages of drug discovery, the in vitro hepatic metabolic stability assay carries great importance as it provides a time- and cost-effective route for