Integration of Pharmaceutical Discovery and Development

Case Histories

  • Ronald T. Borchardt
  • Roger M. Freidinger
  • Tomi K. Sawyer
  • Philip L. Smith

Part of the Pharmaceutical Biotechnology book series (PBIO, volume 11)

Table of contents

  1. Front Matter
    Pages i-xxix
  2. Ralph Hirschmann
    Pages 1-5
  3. Saul H. Rosenberg, Hollis D. Kleinert
    Pages 7-28
  4. David J. Carini, David D. Christ, John V. Duncia, Michael E. Pierce
    Pages 29-56
  5. Robert T. Shuman, Paul D. Gesellchen
    Pages 57-80
  6. Annette M. Doherty, Andrew C. G. Uprichard
    Pages 81-112
  7. John D. Elliott, Eliot H. Ohlstein, Catherine E. Peishoff, Harma M. Ellens, M. Amparo Lago
    Pages 113-129
  8. Fortuna Haviv, Eugene N. Bush, Judith Knittle, Jonathan Greer
    Pages 131-149
  9. Kenneth W. Funk, Jonathan Greer, Akwete L. Adjei
    Pages 151-182
  10. Peter Marbach, Wilfried Bauer, David Bodmer, Ulrich Briner, Christian Bruns, Ioana Lancranjan et al.
    Pages 183-209
  11. Guy E. Padbury, Gail L. Zipp, Francis J. Schwende, Zhiyang Zhao, Kenneth A. Koeplinger, Kong Teck Chong et al.
    Pages 211-232
  12. George V. De Lucca, Prabhakar K. Jadhav, Robert E. Waltermire, Bruce J. Aungst, Susan Erickson-Viitanen, Patrick Y. S. Lam
    Pages 257-284
  13. Wade J. Adams, Paul A. Aristoff, Richard K. Jensen, Walter Morozowich, Donna L. Romero, William C. Schinzer et al.
    Pages 285-312
  14. Richard L. Jarvest, David Sutton, R. Anthony Vere Hodge
    Pages 313-344
  15. Pradip K. Bhatnagar, William F. Huffman, Andrew G. King, Louis M. Pelus, William M. Potts, Philip L. Smith et al.
    Pages 367-391
  16. Stephen V. Frye, H. Neal Bramson, David J. Hermann, Frank W. Lee, Achintya K. Sinhababu, Gaochao Tian
    Pages 393-422
  17. Kimberly K. Adkison, Kathy A. Halm, Joel E. Shaffer, David Drewry, Achintya K. Sinhababu, Judd Berman
    Pages 423-443
  18. Steven G. Blanchard, Robert C. Andrews, Peter J. Brown, Liang-Shang L. Gan, Frank W. Lee, Achintya K. Sinhababu et al.
    Pages 445-463
  19. Franco Lombardo, Steven M. Winter, Larry Tremaine, John A. Lowe III
    Pages 465-479
  20. Bharat K. Trivedi, Joanna P. Hinton
    Pages 481-505
  21. Elizabeth E. Sugg, Lawrence Birkemo, Liang-Shang L. Gan, Timothy K. Tippin
    Pages 507-524
  22. Arthur A. Patchett, Roy G. Smith, Matthew J. Wyvratt
    Pages 525-554
  23. Gerald S. Ponticello, Michael F. Sugrue, Bernard Plazonnet, Geneviève Durand-Cavagna
    Pages 555-574
  24. Mac E. Hadley, Victor J. Hruby, James Blanchard, Robert T. Dorr, Norman Levine, Brenda V. Dawson et al.
    Pages 575-595
  25. Back Matter
    Pages 597-609

About this book


In the late 1980s, it became painfully evident to the pharmaceutical industry that the old paradigm of drug discovery, which involved highly segmented drug - sign and development activities, would not produce an acceptable success rate in the future. Therefore, in the early 1990s a paradigm shift occurred in which drug design and development activities became more highly integrated. This new str- egy required medicinal chemists to design drug candidates with structural f- tures that optimized pharmacological (e. g. , high affinity and specificity for the target receptor), pharmaceutical (e. g. , solubility and chemical stability), bioph- maceutical (e. g. , cell membrane permeability), and metabolic/pharmacokinetic (e. g. , metabolic stability, clearance, and protein binding) properties. Successful implementation of this strategy requires a multidisciplinary team effort, incl- ing scientists from drug design (e. g. , medicinal chemists, cell biologists, en- mologists, pharmacologists) and drug development (e. g. , analytical chemists, pharmaceutical scientists, physiologists, and molecular biologists representing the disciplines of pharmaceutics, biopharmaceutics, and pharmacokinetics/drug metabolism). With this new, highly integrated approach to drug design now widely utilized by the pharmaceutical industry, the editors of this book have provided the sci- tific community with case histories to illustrate the nature of the interdisciplinary interactions necessary to successfully implement this new approach to drug d- covery. In the first chapter, Ralph Hirschmann provides a historical perspective of why this paradigm shift in drug discovery has occurred.


Nucleoside chemistry development metabolism pharmaceutical receptor

Editors and affiliations

  • Ronald T. Borchardt
    • 1
  • Roger M. Freidinger
    • 2
  • Tomi K. Sawyer
    • 3
  • Philip L. Smith
    • 4
  1. 1.The University of KansasLawrence
  2. 2.Merck Research LaboratoriesWest Point
  3. 3.ARIAD Pharmaceuticals, Inc.Cambridge
  4. 4.Smith Kline BeechamCollegeville

Bibliographic information

  • DOI
  • Copyright Information Kluwer Academic Publishers 1998
  • Publisher Name Springer, Boston, MA
  • eBook Packages Springer Book Archive
  • Print ISBN 978-0-306-45743-2
  • Online ISBN 978-0-306-47384-5
  • Series Print ISSN 1078-0467
  • Buy this book on publisher's site