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Zhou S, Chan E, Li X, et al. Clinical outcomes and management of mechanism-based inhibition of cytochrome P450 3A4. Ther Clin Risk Manag. 2005;1(1):3-13doi: 10.2147/tcrm.1.1.3.53600.
Zhou, S., Chan, E., Li, X., & Huang, M. (2005). Clinical outcomes and management of mechanism-based inhibition of cytochrome P450 3A4. Therapeutics and clinical risk management, 1(1), 3-13. https://doi.org/10.2147/tcrm.1.1.3.53600
Zhou, Shufeng, et al. "Clinical outcomes and management of mechanism-based inhibition of cytochrome P450 3A4." Therapeutics and clinical risk management vol. 1,1 (2005): 3-13. doi: https://doi.org/10.2147/tcrm.1.1.3.53600
Zhou S, Chan E, Li X, Huang M. Clinical outcomes and management of mechanism-based inhibition of cytochrome P450 3A4. Ther Clin Risk Manag. 2005 Mar;1(1):3-13. doi: 10.2147/tcrm.1.1.3.53600. PMID: 18360537; PMCID: PMC1661603.
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Ther Clin Risk Manag. 2005 Mar;1(1):3-13. doi: 10.2147/tcrm.1.1.3.53600.

Clinical outcomes and management of mechanism-based inhibition of cytochrome P450 3A4.

Therapeutics and clinical risk management

Shufeng Zhou, Eli Chan, Xiaotian Li, Min Huang

PMID: 18360537 PMCID: PMC1661603 DOI: 10.2147/tcrm.1.1.3.53600

Abstract

Mechanism-based inhibition of cytochrome P450 (CYP) 3A4 is characterized by NADPH-, time-, and concentration-dependent enzyme inactivation, occurring when some drugs are converted by CYPs to reactive metabolites. Such inhibition of CYP3A4 can be due to the chemical modification of the heme, the protein, or both as a result of covalent binding of modified heme to the protein. The inactivation of CYP3A4 by drugs has important clinical significance as it metabolizes approximately 60% of therapeutic drugs, and its inhibition frequently causes unfavorable drug-drug interactions and toxicity. The clinical outcomes due to CYP3A4 inactivation depend on many factors associated with the enzyme, drugs, and patients. Clinical professionals should adopt proper approaches when using drugs that are mechanism-based CYP3A4 inhibitors. These include early identification of drugs behaving as CYP3A4 inactivators, rational use of such drugs (eg, safe drug combination regimen, dose adjustment, or discontinuation of therapy when toxic drug interactions occur), therapeutic drug monitoring, and predicting the risks for potential drug-drug interactions. A good understanding of CYP3A4 inactivation and proper clinical management are needed by clinical professionals when these drugs are used.

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