Description
A panel of researchers and experts from leading universities and major pharmaceutical companies from all over the world systematically describe cutting-edge experimental protocols for the early in vitro evaluation of new chemical entities (NCE). These readily reproducible assays measure such critical parameters as physicochemical properties, adsorption, plasma binding, metabolism, drug interactions, and toxicity. By uncovering early in the discovery stage the defects that can eliminate candidate drugs from preclinical and clinical development, these techniques can save millions of dollars in time and effort. pKa, Solubility and Lipophilicity: Assessing Physicochemical Properties of Lead Compounds Yushen Guo and Hong Shen Use of Caco-2 Cell Monolayers to Study Drug Absorption and Metabolism Ming Hu, Jie Ling, Huimin Lin, and Jun Chen Absorption Screening Using the PAMPA Approach Jeffrey A. Ruell and Alex Avdeef In Situ Single-Pass Perfused Rat Intestinal Model for Absorption and Metabolism Eun Ju Jeong, Yan Liu, Huimin Lin, and Ming Hu In Vitro Permeation Study With Bovine Brain Microvessel Endothelial Cells Seong-Hee Park, Sung-Hack Lee, Yaming Su, and Patrick J. Sinko An Enzymatic Microplate Assay for Testing P-Glycoprotein Substrates and Inhibitors S. Orlowski, J. Nugier, and Eric Ezan Evaluation of Drug-Transporter Interactions Using In Vitro Cell Models Yaming Su and Patrick J. Sinko Plasma Protein-Binding Methods in Drug Discovery Lucinda H. Cohen Isothermal Titration Calorimetry Characterization of Drug-Binding Energetics to Blood Proteins Gary W. Caldwell and Zhengyin Yan Metabolic Stability Assessed by Liver Microsomes and Hepatocytes David C. Ackley, Kevin T. Rockich, and Timothy R. Baker In Vitro Drug Metabolite Profiling Using Hepatic S9 and Human Liver Microsomes Wu-Nan Wu and Linda A. McKown In Vitro Identification of UDP-glucuronosyltransferases Involved in Drug Metabolism Michael H. Court In Vitro CYP Induction in Human Hepatocytes Daniel R. Mudra and Andrew Parkinson High-Throughput Screening of Human Cytochrome P450 Inhibitors Using Fluorometric Substrates: Methodology for 25 Enzyme/Substrate Pairs David M. Stresser Evaluation of Cytochrome P450 Inhibition in Human Liver Microsomes Zhengyin Yan and Gary W. Caldwell Identification of CYP Mechanism-Based Inhibitors Amin A. Nomeir, Jairam Palamanda, and Leonard Favreau Detection of DNA Adducts by 32P-Postlabeling Analysis Naomi Suzuki, Padmaja M. Prabhu, and Shinya Shibutani Covalent DNA Adduct Formation Mediated by Cytochrome P450 Marie Stiborov Application of In Vitro Comet Assay for Genotoxicity Testing Bojana Zegura and Metka Filipic Assessing DNA Damage Using a Reporter Gene System Xuming Jia and Wei Xiao Improvement of the Ames Test Using Human Liver S9 Preparation Atsushi Hakura, Satoshi Suzuki, and Tetsuo Satoh Screening for Chemical Mutagens Using the Mouse Lymphoma Assay Tao Chen and Martha M. Moore A High-Throughput Binding Assay for HERG Keith Finlayson and John Sharkey In Vitro Drug Metabolism: Thiol Conjugation Wei Tang and Randy R. Miller In Vitro Screening Assay of the Reactivity of Acyl Glucuronides Sbastien Bolze Index
