Biomolecules & Therapeutics
Inhibition of Cytochrome P450 Enzymes by Drugs—Molecular Basis and Practical Applications
F. Peter Guengerich*
Department of Biochemistry, Vanderbilt University School of Medicine, Nashville, TN 37232-0146, USA
Tel: +1-615-322-2261, Fax: +1-615-343-0704
Received: June 22, 2021; Accepted: July 22, 2021; Published online: September 3, 2021.
© The Korean Society of Applied Pharmacology. All rights reserved.

This is an Open Access article distributed under the terms of the Creative Commons Attribution Non-Commercial License ( which permits unrestricted non-commercial use, distribution, and reproduction in any medium, provided the original work is properly cited.
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: Cytochrome P450, CYP, Drug-drug interactions, P450 inhibition, Enzyme inhibition

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