Glossary and tutorial of xenobiotic metabolism terms used during small molecule drug discovery and development (IUPAC Technical Report)

Author:

Erhardt Paul1,Bachmann Kenneth2,Birkett Donald3,Boberg Michael4,Bodor Nicholas5,Gibson Gordon6,Hawkins David7,Hawksworth Gabrielle8,Hinson Jack9,Koehler Daniel10,Kress Brian11,Luniwal Amarjit12,Masumoto Hiroshi13,Novak Raymond14,Portoghese Phillip15,Sarver Jeffrey10,Serafini M. Teresa16,Trabbic Christopher17,Vermeulen Nico18,Wrighton Steven19

Affiliation:

1. Center for Drug Design and Development , University of Toledo , Toledo , Ohio , USA

2. Ceuticare, Inc. , Sylvania , Ohio , USA, (TGM and ST)

3. Department of Clinical Pharmacology , Flinders University , Adelaide , Australia (now Emeritus), (TGM)

4. Metabolism and Isotope Chemistry , Bayer , AG , Germany (now undetermined), (TGM)

5. Center for Drug Discovery , University of Florida , Belle Glade , FL , USA (now Emeritus Grad Res Prof/CEO Bodor Labs), (TGM)

6. School of Biomedical and Life Sciences, University of Surrey , Surrey , UK (now deceased), (TGM)

7. Huntingdon Life Sciences , Huntingdon , UK (now retired), (TGM)

8. Department of Medicine and Therapeutics , University Aberdeen , Aberdeen , UK (now deceased), (TGM)

9. Division of Toxicology , University Arkansas for Medical Sciences , Little Rock , Arkansas , USA (now Emeritus Dist Prof), (TGM)

10. Department of Pharmacology , University of Toledo , Toledo , Ohio , USA, (ST)

11. Department of Medicinal and Biological Chemistry , University of Toledo , Toledo , Ohio , USA, (ST)

12. NAmSA, Inc. , Northwood , Ohio , USA, (ST)

13. Drug Metabolism , Daiichi Pharm. Corp., Ltd. , Chuo , Tokyo , Japan (now retired), (TGM)

14. Institute of Environmental Health Science, Wayne State University , Detroit , Michigan , USA (now undetermined), (TGM)

15. Department of Medicinal Chemistry , University of Minnesota , Minneapolis , Minnesota , USA (now same), (TGM)

16. Department of Pharmacokinetics and Drug Metabolism , Laboratories Dr. Esteve, S.A. , Barcelona , Spain (now Head Early ADME), (TGM)

17. MPI Research, Inc. , Mattawan , Michigan , USA, (ST)

18. Department of Pharmacochemistry , Vrije University , Amsterdam , Netherlands (now Emeritus Section Molecular Toxicology), (TGM)

19. Eli Lilly, Inc. , Indianapolis , Indiana , USA (now retired), (TGM)

Abstract

Abstract This project originated more than 15 years ago with the intent to produce a glossary of drug metabolism terms having definitions especially applicable for use by practicing medicinal chemists. A first-draft version underwent extensive beta-testing that, fortuitously, engaged international audiences in a wide range of disciplines involved in drug discovery and development. It became clear that the inclusion of information to enhance discussions among this mix of participants would be even more valuable. The present version retains a chemical structure theme while expanding tutorial comments that aim to bridge the various perspectives that may arise during interdisciplinary communications about a given term. This glossary is intended to be educational for early stage researchers, as well as useful for investigators at various levels who participate on today’s highly multidisciplinary, collaborative small molecule drug discovery teams.

Publisher

Walter de Gruyter GmbH

Subject

General Chemical Engineering,General Chemistry

Reference287 articles.

1. P. Erhardt. Pure Appl. Chem., 74, 703 (2002).

2. Drug Metabolism: Databases and High Throughput Testing During Drug Design and Development, P. Erhardt with chapter contributions from more than 30 international expert contributors (Ed.), IUPAC/Blackwell, Geneva (1999).

3. P. Erhardt. in Pharmacology: Principles and Practice, M. Hacker, W. Messer and K. Bachmann (Eds.), pp. 475–560, Elsevier, Oxford (2009).

4. A. Avdeef. Absorption and Drug Development, Wiley, Hoboken (2003).

5. F. Lipmann. J. Biol. Chem., 160, 173 (1945).

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