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Gary Hingorani, Jianhong Wang, Corey Custer, …
Human Hepatic Stability Screening: a Simplified Higher Throughput Assay and Evaluation of Different Hepatocyte PreparationsGary hingorani , Jianhong wang , Corey custer , Kevin Litwiler and Ron Franklin, Array BioPharma Inc., Boulder, COIn the early stages of drug discovery, hepatic stability screening is an important and widely used method to assess the metabolic stability as well as predict the in vivo hepatic clearance of new chemical entities. Here we present a simplified higher throughput method for rapid stability screening using hepatocytes in a 96-well format for LC-MS determinations. A set of 24 known drugs was chosen that act as substrates for the major human hepatic P450 and UGT isoforms. The predicted human hepatic clearance for these known drugs was determined using cryopreserved, single donor hepatocyte preparations (In Vitro Technologies), and data were compared to literature values for in vivo systemic clearance.
Human Hepatic Stability Screening: a Simplified Higher Throughput Assay and Evaluation of Different Hepatocyte Preparations Gary Hingorani, Jianhong Wang, Corey Custer, Kevin Litwiler and Ron Franklin, Array BioPharma Inc., Boulder, CO In the early stages of drug discovery, hepatic stability screening is an important and widely
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