In vitro techniques for studying drug metabolism

J Pharmacokinet Biopharm. 1996 Oct;24(5):521-33. doi: 10.1007/BF02353478.


A considerable amount of information has been obtained about human enzymes involved in drug metabolism. Cytochrome P450 is presented as a paradigm in order to illustrate the experimental techniques now available. In vitro assays can be done with tissue slices, microsomes, or even short-term cell cultures. In addition, recombinant enzymes can be produced in a variety of different vector systems. Information about catalytic selectivity regarding new drugs can be obtained, as well as important information about potential drug-drug interactions and bioavailability. Such studies play a role in the drug development process as well as metabolism and safety assessment.

MeSH terms

  • Animals
  • Antibodies / metabolism
  • Cells, Cultured / metabolism
  • Cytochrome P-450 Enzyme Inhibitors
  • Cytochrome P-450 Enzyme System / metabolism*
  • Drug Design
  • Enzyme Induction / physiology
  • Enzyme Inhibitors / metabolism*
  • Enzymes / metabolism*
  • Gene Expression
  • Humans
  • In Vitro Techniques
  • Microsomes, Liver / metabolism
  • Pharmaceutical Preparations / metabolism*
  • Polymorphism, Genetic


  • Antibodies
  • Cytochrome P-450 Enzyme Inhibitors
  • Enzyme Inhibitors
  • Enzymes
  • Pharmaceutical Preparations
  • Cytochrome P-450 Enzyme System