Biotechnology: Pharmaceutical Aspects

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

Editors: Borchardt, R., Kerns, E., Hageman, M., Thakker, D., Stevens, J. (Eds.)

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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.

Table of contents (18 chapters)

  • Strategic Use of Preclinical Pharmacokinetic Studies and In Vitro Models in Optimizing ADME Properties of Lead Compounds

    Thakker, Dhiren R.

    Pages 1-23

  • Role of Mechanistic Transport Studies in Lead Optimization

    Hochman, Jerome (et al.)

    Pages 25-47

  • Metabolic Activation-Role in Toxicity and Idiosyncratic Reactions

    Walsh, John S.

    Pages 49-80

  • Case History — Use of ADME Studies for Optimization of Drug Candidates

    Gan, Liang-Shang (et al.)

    Pages 81-97

  • Solubility, Solubilization and Dissolution in Drug Delivery During Lead Optimization

    Hageman, Michael J.

    Pages 99-130

Buy this book

eBook $269.00
price for USA (gross)
  • ISBN 978-0-387-44961-6
  • Digitally watermarked, DRM-free
  • Included format: PDF
  • ebooks can be used on all reading devices
  • Immediate eBook download after purchase
Hardcover $339.00
price for USA
  • ISBN 978-0-387-34056-2
  • Free shipping for individuals worldwide
  • Usually dispatched within 3 to 5 business days.
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Bibliographic Information

Bibliographic Information
Book Title
Optimizing the "Drug-Like" Properties of Leads in Drug Discovery
Editors
  • Ronald Borchardt
  • Edward Kerns
  • Michael Hageman
  • Dhrien Thakker
  • James Stevens
Series Title
Biotechnology: Pharmaceutical Aspects
Series Volume
IV
Copyright
2006
Publisher
Springer-Verlag New York
Copyright Holder
Springer-Verlag New York
eBook ISBN
978-0-387-44961-6
DOI
10.1007/978-0-387-44961-6
Hardcover ISBN
978-0-387-34056-2
Edition Number
1
Number of Pages
X, 512
Topics