Biomolecules & Therapeutics

The Korean Society of Applied Pharmacology (한국응용약물학회)
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Inhibition of Cytochrome P450 Enzymes by Drugs-Molecular Basis and Practical Applications

  • Guengerich, F. Peter (Department of Biochemistry, Vanderbilt University School of Medicine)
  • Received : 2021.06.22
  • Accepted : 2021.07.22
  • Published : 2022.01.01
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Abstract

Drug-drug interactions are a major cause of hospitalization and deaths related to drug use. A large fraction of these is due to inhibition of enzymes involved in drug metabolism and transport, particularly cytochrome P450 (P450) enzymes. Understanding basic mechanisms of enzyme inhibition is important, particularly in terms of reversibility and the use of the appropriate parameters. In addition to drug-drug interactions, issues have involved interactions of drugs with foods and natural products related to P450 enzymes. Predicting drug-drug interactions is a major effort in drug development in the pharmaceutical industry and regulatory agencies. With appropriate in vitro experiments, it is possible to stratify clinical drug-drug interaction studies. A better understanding of drug interactions and training of physicians and pharmacists has developed. Finally, some P450s have been the targets of drugs in some cancers and other disease states.

Keywords

Acknowledgement

Thanks are extended to K. Trisler for assistance in preparation of the manuscript. P450 research in the author's laboratory is supported by National Institutes of Health grant R01 GM118122. The content is solely the responsibility of the author and does not necessarily represent the official view of the National Institutes of Health.

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