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Principles of Drug Metabolism

Drug Discovery

  1. Bernard Testa

Published Online: 15 APR 2010

DOI: 10.1002/0471266949.bmc033.pub2

Burger's Medicinal Chemistry and Drug Discovery

Burger's Medicinal Chemistry and Drug Discovery

How to Cite

Testa, B. 2010. Principles of Drug Metabolism. Burger's Medicinal Chemistry and Drug Discovery. 403–454.

Author Information

  1. University Hospital Centre, Department of Pharmacy, Lausanne, Switzerland

Publication History

  1. Published Online: 15 APR 2010


The focus of this chapter is essentially on drug metabolism reactions and their enzymes. Connected information of significance to medicinal chemists is also given attention. Introductory principles of drug metabolism are presented in the introduction. Oxidoreductases are discussed in the next section together with a systematic and extensive treatment of the chemical groups they target and the functionalization reactions they catalyze. Attention is paid to the cytochromes P450, their multiplicity, specificities and relative importance. Hydrolases are also treated. The next section is dedicated to the transferases and the conjugation reactions they catalyze, for example, glucuronidation and glutathione conjugation. The last section, which is particularly close to the interests of medicinal chemists, discusses pharmacological and toxicological consequences of metabolism, structure-metabolism relationships and the prediction of metabolism, and briefly outlines the biological factors that influence biotransformation.


  • biotransformation;
  • conjugation reactions;
  • cytochromes P450;
  • enzymes;
  • functionalization reactions;
  • hydrolases;
  • interindividual factors;
  • intraindividual factors;
  • oxidoreductases;
  • pharmacological consequences;
  • prediction of metabolism;
  • toxicological consequences;
  • toxophoric groups;
  • transferases;
  • structure–metabolism relationships