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  • © 2014

Optimization in Drug Discovery

In Vitro Methods

  • 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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Table of contents (34 protocols)

  1. Front Matter

    Pages i-xvii
  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. In Vitro CYP/FMO Reaction Phenotyping

    • Carlo Sensenhauser
    Pages 137-169
  9. Characterization of Constitutive Androstane Receptor (CAR) Activation

    • Caitlin Lynch, Haishan Li, Hongbing Wang
    Pages 195-205
  10. 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
  11. In Vitro CYP Induction Using Human Hepatocytes

    • Monica Singer, Carlo Sensenhauser, Shannon Dallas
    Pages 237-253
  12. Identification of Time-Dependent CYP Inhibitors Using Human Liver Microsomes (HLM)

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

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.

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

Buy it now

Buying options

eBook USD 119.00
Price excludes VAT (USA)
  • Available as EPUB and PDF
  • Read on any device
  • Instant download
  • Own it forever
Softcover Book USD 159.00
Price excludes VAT (USA)
  • Compact, lightweight edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info
Hardcover Book USD 219.99
Price excludes VAT (USA)
  • Durable hardcover edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info

Tax calculation will be finalised at checkout

Other ways to access