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Optimization in Drug Discovery

In Vitro Methods

  • Book
  • © 2014
  • Latest edition

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Editors:
  1. Gary W. Caldwell

    1. CREATe Core Science Technologies, Janssen Research & Development, LLC, Spring House, USA

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    You can also search for this editor in PubMed   Google Scholar

  2. Zhengyin Yan

    1. CREATe Core Science Technologies, Janssen Research & Development, LLC, Spring House, USA

    View editor publications

    You can also search for this editor in PubMed   Google Scholar

  • Provides updated variations on assays as well as numerous new protocols for drug discovery optimization
  • Features readily reproducible methods and protocols that are lab-tested and successful
  • Includes expert tips and key implementation advice

Part of the book series: Methods in Pharmacology and Toxicology (MIPT)

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About this book

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.

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Table of contents (34 protocols)

  1. Front Matter

    Pages i-xvii
    Download chapter PDF

  2. Small Molecule Formulation Screening Strategies in Drug Discovery

    • Gary W. Caldwell, Becki Hasting, John A. Masucci, Zhengyin Yan
    Pages 1-20

  3. Assessment of Drug Plasma Protein Binding in Drug Discovery

    • Dennis Kalamaridis, Nayan Patel
    Pages 21-37

  4. Drug Partition in Red Blood Cells

    • Dennis Kalamaridis, Karen DiLoreto
    Pages 39-47

  5. Permeability Assessment Using 5-day Cultured Caco-2 Cell Monolayers

    • Gary W. Caldwell, Chrissa Ferguson, Robyn Buerger, Lovonia Kulp, Zhengyin Yan
    Pages 49-76

  6. In Situ Single Pass Perfused Rat Intestinal Model

    • Maria Markowska, L. Mark Kao
    Pages 77-86

  7. Metabolic Stability Assessed by Liver Microsomes and Hepatocytes

    • Kevin J. Coe, Tatiana Koudriakova
    Pages 87-99

  8. Metabolic Assessment in Alamethicin-Activated Liver Microsomes: Co-activating CYPs and UGTs

    • Gary W. Caldwell, Zhengyin Yan
    Pages 101-115

  9. Phenotyping UDP-Glucuronosyltransferases (UGTs) Involved in Human Drug Metabolism: An Update

    • Michael H. Court
    Pages 117-136

  10. In Vitro CYP/FMO Reaction Phenotyping

    • Carlo Sensenhauser
    Pages 137-169

  11. Human Pregnane X Receptor (hPXR) Activation Assay in Stable Cell Lines

    • Judy L. Raucy
    Pages 171-193

  12. Characterization of Constitutive Androstane Receptor (CAR) Activation

    • Caitlin Lynch, Haishan Li, Hongbing Wang
    Pages 195-205

  13. DNA Binding (Gel Retardation Assay) Analysis for Identification of Aryl Hydrocarbon (Ah) Receptor Agonists and Antagonists

    • Anatoly A. Soshilov, Michael S. Denison
    Pages 207-219

  14. Cell-Based Assays for Identification of Aryl Hydrocarbon Receptor (AhR) Activators

    • Guochun He, Jing Zhao, Jennifer C. Brennan, Alessandra A. Affatato, Bin Zhao, Robert H. Rice et al.
    Pages 221-235

  15. In Vitro CYP Induction Using Human Hepatocytes

    • Monica Singer, Carlo Sensenhauser, Shannon Dallas
    Pages 237-253

  16. Assessment of CYP3A4 Time-Dependent Inhibition in Plated and Suspended Human Hepatocytes

    • J. George Zhang, David M. Stresser
    Pages 255-268

  17. Evaluation of Time-Dependent CYP3A4 Inhibition Using Human Hepatocytes

    • Yuan Chen, Adrian J. Fretland
    Pages 269-279

  18. Rapidly Distinguishing Reversible and Time-Dependent CYP450 Inhibition Using Human Liver Microsomes, Co-incubation, and Continuous Fluorometric Kinetic Analyses

    • Gary W. Caldwell, Zhengyin Yan
    Pages 281-303

  19. Identification of Time-Dependent CYP Inhibitors Using Human Liver Microsomes (HLM)

    • Kevin J. Coe, Judith Skaptason, Tatiana Koudriakova
    Pages 305-314

  20. CYP Time-Dependent Inhibition (TDI) Using an IC50 Shift Assay with Stable Isotopic Labeled Substrate Probes to Facilitate Liquid Chromatography/Mass Spectrometry Analyses

    • Gary W. Caldwell, Zhengyin Yan
    Pages 315-336
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Editors and Affiliations

  • CREATe Core Science Technologies, Janssen Research & Development, LLC, Spring House, USA

    Gary W. Caldwell, Zhengyin Yan

Bibliographic Information

  • Book Title: Optimization in Drug Discovery

  • Book Subtitle: In Vitro Methods

  • Editors: Gary W. Caldwell, Zhengyin Yan

  • Series Title: Methods in Pharmacology and Toxicology

  • DOI: https://doi.org/10.1007/978-1-62703-742-6

  • Publisher: Humana Totowa, NJ

  • eBook Packages: Springer Protocols

  • Copyright Information: Springer Science+Business Media New York 2014

  • Hardcover ISBN: 978-1-62703-741-9Published: 09 November 2013

  • Softcover ISBN: 978-1-4939-6070-5Published: 23 August 2016

  • eBook ISBN: 978-1-62703-742-6Published: 08 November 2013

  • Series ISSN: 1557-2153

  • Series E-ISSN: 1940-6053

  • Edition Number: 2

  • Number of Pages: XVII, 597

  • Number of Illustrations: 64 b/w illustrations, 49 illustrations in colour

  • Topics: Pharmacology/Toxicology

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