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Optimizing the "Drug-Like" Properties of Leads in Drug Discovery

  • Book
  • © 2006

Overview

Editors:
  1. Ronald T. Borchardt

    1. University of Kansas, Lawrence, USA

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  2. Edward H. Kerns

    1. Wyeth Research, Monmouth Junction, USA

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  3. Michael J. Hageman

    1. Pfizer, Inc., Kalamazoo, USA

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  4. Dhiren R. Thakker

    1. University of North Carolina, Chapel Hill, USA

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  5. James L. Stevens

    1. Eli Lilly Research Laboratory, Greenfield, USA

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  • Outlines strategies and methodologies designed to guide pharmaceutical and biotechnology companies through the drug discovery and development process
  • Emphasis on advancing higher quality drug candidates into preclinical and clinical development, resulting in more efficacious and safer drugs

Part of the book series: Biotechnology: Pharmaceutical Aspects (PHARMASP, volume IV)

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Table of contents (18 chapters)

  1. Front Matter

    Pages i-x
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  2. Strategic Use of Preclinical Pharmacokinetic Studies and In Vitro Models in Optimizing ADME Properties of Lead Compounds

    • Dhiren R. Thakker
    Pages 1-23

  3. Role of Mechanistic Transport Studies in Lead Optimization

    • Jerome Hochman, Qin Mei, Masayo Yamazaki, Cuyue Tang, Thomayant Prueksaritanont, Mark Bock et al.
    Pages 25-47

  4. Metabolic Activation-Role in Toxicity and Idiosyncratic Reactions

    • John S. Walsh
    Pages 49-80

  5. Case History — Use of ADME Studies for Optimization of Drug Candidates

    • Liang-Shang Gan, Frank W. Lee, Nelamangala Nagaraja, Ping Li, Jason Labutti, Wei Yin et al.
    Pages 81-97

  6. Solubility, Solubilization and Dissolution in Drug Delivery During Lead Optimization

    • Michael J. Hageman
    Pages 99-130

  7. Lipid-based Systems, Drug Exposure and Lead Optimization

    • William N. Charman, Susan A. Charman, Christopher J. H. Porter
    Pages 131-150

  8. Biopharmaceutics Modeling and the Role of Dose and Formulation on Oral Exposure

    • Brian R. Rohrs
    Pages 151-166

  9. Application of Physicochemical Data to Support Lead Optimization by Discovery Teams

    • Li Di, Edward H. Kerns
    Pages 167-193

  10. Computational Models Supporting Lead Optimization in Drug Discovery

    • Philip S. Burton, Italo Poggesi, Massimiliano Germani, Jay T. Goodwin
    Pages 195-219

  11. Prodrug Strategies for Improving Drug-Like Properties

    • Valentino J. Stella
    Pages 221-242

  12. The Application of Multivariate Data Analysis to Compound Property Optimization

    • John W. Ellingboe
    Pages 243-254

  13. Case History: Toxicology Biomarker Development Using Toxicogenomics

    • David E. Watson, Timothy P. Ryan, James L. Stevens
    Pages 255-270

  14. Predicting Idiosyncratic Drug Reactions

    • Alastair Cribb
    Pages 271-299

  15. Elementary Predictive Toxicology for Advanced Applications

    • Constantine Kreatsoulas, Stephen K. Durham, Laura L. Custer, Greg M. Pearl
    Pages 301-322

  16. The Application of PK/PD Modeling and Simulations During Lead Optimization

    • Stuart Friedrich, Evelyn Lobo, Karen Zimmerman, Anthony Borel, Carlos O. Garner
    Pages 323-353

  17. Early Preclinical Evaluation of Brain Exposure in Support of Hit Identification and Lead Optimization

    • Thomas J. Raub, Barry S. Lutzke, Paula K. Andrus, Geri A. Sawada, Brian A. Staton
    Pages 355-410

  18. Optimizing Biomarker Development for Clinical Studies at the Lead Optimization Stage of Drug Development

    • Geoffrey S Ginsburg, Julie Lekstrom-Himes, William Trepicchio
    Pages 411-421

  19. The Relevance of Transporters in Determining Drug Disposition

    • Hartmut Glaeser, Richard B. Kim
    Pages 423-459

  20. Back Matter

    Pages 461-511
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Keywords

About this book

Drug discovery and development is a very complex, costly, and ti- consuming process. Because of the uncertainties associated with predicting the pharmacological effects and the toxicity characteristics of new chemical entities in man, their clinical development is quite prone to failure. In recent years, phar- ceutical companies have come under increasing pressure to introduce new blockbuster drugs into the marketplace more rapidly. Companies have responded to these pressures by introducing new technologies and new strategies to expedite drug discovery and development. Drug discovery and development have traditionally been divided into three separate processes (i. e. , discovery research, preclinical development, and clinical development) that ideally should be integrated both organizationally and functionally. Instead, separate and distinct discovery research, preclinical development, and clinical development divisions were created within many companies during the 1980s and 1990s, Because of their isolation, scientists in the discovery research divisions often were advancing drug candidates into preclinical development that had marginal drug-like properties. For the purpose of this presentation, “drug-like” properties refer to the molecule’s physicochemical, absorption-distribution-metabolism-excretion (ADME), and toxicological properties. Lacking optimal drug-like properties often caused these drug candidates to fail in preclinical or clinical development.

Editors and Affiliations

  • University of Kansas, Lawrence, USA

    Ronald T. Borchardt

  • Wyeth Research, Monmouth Junction, USA

    Edward H. Kerns

  • Pfizer, Inc., Kalamazoo, USA

    Michael J. Hageman

  • University of North Carolina, Chapel Hill, USA

    Dhiren R. Thakker

  • Eli Lilly Research Laboratory, Greenfield, USA

    James L. Stevens

Bibliographic Information

  • Book Title: Optimizing the "Drug-Like" Properties of Leads in Drug Discovery

  • Editors: Ronald T. Borchardt, Edward H. Kerns, Michael J. Hageman, Dhiren R. Thakker, James L. Stevens

  • Series Title: Biotechnology: Pharmaceutical Aspects

  • DOI: https://doi.org/10.1007/978-0-387-44961-6

  • Publisher: Springer New York, NY

  • eBook Packages: Biomedical and Life Sciences, Biomedical and Life Sciences (R0)

  • Copyright Information: Springer-Verlag New York 2006

  • Hardcover ISBN: 978-0-387-34056-2Published: 03 August 2006

  • Softcover ISBN: 978-1-4939-5047-8Published: 25 October 2016

  • eBook ISBN: 978-0-387-44961-6Published: 31 December 2007

  • Edition Number: 1

  • Number of Pages: X, 512

  • Topics: Pharmacology/Toxicology

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