Thoroughly revised and updated, Optimization in Drug Discovery: In Vitro Methods, Second Edition presents a wide spectrum of in vitro assays including formulation, plasma binding, absorption and permeability, cytochrome P450 (CYP) and UDP-glucuronosyltransferases (UGT) metabolism, CYP inhibition and induction, drug transporters, drug-drug interactions via assessment of reactive metabolites, genotoxicity, and chemical and photo-mutagenicity assays. Written for the Methods in Pharmacology and Toxicology series, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible protocols, and tips on troubleshooting and avoiding known pitfalls. Expert authors have developed and utilized these in vitro assays to achieve drug-like characteristics in addition to efficacy properties and good safety profiles of drug candidates.
Comprehensive and up-to-date, Optimization in Drug Discovery: In Vitro Methods, Second Edition aims to guide researchers down the difficult path to successful drug discovery and development.
This fresh edition features new assay variations and the latest protocols for optimizing drug discovery. With expert tips and troubleshooting advice, and revised throughout for this second edition, it covers cutting-edge techniques such as cytochrome P450.
1. Small Molecule Formulation Screening Strategies in Drug Discovery
??????????? Gary W. Caldwell, Becki Hasting, John Masucci, and Zhengyin Yan
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2. Assessment of Drug Plasma Protein Binding in Drug Discovery
??????????? Dennis Kalamaridis and Nayan Patel
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3. Drug Partition in Red Blood Cells
??????????? Dennis Kalamaridis and Karen DiLoreto
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4. Permeabilitlsh