Optimizing the “Drug-Like” Properties of Leads in Drug Discovery

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

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

Table of contents

  1. Front Matter
    Pages i-x
  2. Jerome Hochman, Qin Mei, Masayo Yamazaki, Cuyue Tang, Thomayant Prueksaritanont, Mark Bock et al.
    Pages 25-47
  3. Liang-Shang Gan, Frank W. Lee, Nelamangala Nagaraja, Ping Li, Jason Labutti, Wei Yin et al.
    Pages 81-97
  4. William N. Charman, Susan A. Charman, Christopher J. H. Porter
    Pages 131-150
  5. Philip S. Burton, Italo Poggesi, Massimiliano Germani, Jay T. Goodwin
    Pages 195-219
  6. Valentino J. Stella
    Pages 221-242
  7. David E. Watson, Timothy P. Ryan, James L. Stevens
    Pages 255-270
  8. Alastair Cribb
    Pages 271-299
  9. Constantine Kreatsoulas, Stephen K. Durham, Laura L. Custer, Greg M. Pearl
    Pages 301-322
  10. Stuart Friedrich, Evelyn Lobo, Karen Zimmerman, Anthony Borel, Carlos O. Garner
    Pages 323-353
  11. Thomas J. Raub, Barry S. Lutzke, Paula K. Andrus, Geri A. Sawada, Brian A. Staton
    Pages 355-410
  12. Geoffrey S Ginsburg, Julie Lekstrom-Himes, William Trepicchio
    Pages 411-421
  13. Hartmut Glaeser, Richard B. Kim
    Pages 423-459
  14. Back Matter
    Pages 461-511

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.


Borchardt Discovery Drug Leads Like Optimizing Properties lead

Editors and affiliations

  • Ronald T. Borchardt
    • 1
  • Edward H. Kerns
    • 2
  • Michael J. Hageman
    • 3
  • Dhiren R. Thakker
    • 4
  • James L. Stevens
    • 5
  1. 1.University of KansasLawrenceUSA
  2. 2.Wyeth ResearchMonmouth JunctionUSA
  3. 3.Pfizer, Inc.KalamazooUSA
  4. 4.University of North CarolinaChapel HillUSA
  5. 5.Eli Lilly Research LaboratoryGreenfieldUSA

Bibliographic information