A Short Exploration of Selected Sensitive CYP3A4 Substrates (Probe Drug)

Author(s): Sarvesh Sabarathinam, Thangavel M. Vijayakumar*

Journal Name: Drug Metabolism Letters

Volume 14 , Issue 1 , 2021

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Graphical Abstract:


Background: CYP450 enzymes in the liver have a significant role in the metabolism of xenobiotics. Probe drug strategy is broadly used to evaluate the pharmacodynamic and pharmacokinetic drug/ herb-drug interactions/ food-drug interactions. Probe drugs reveal the exact pathway of drug metabolism in the liver by their targeted tractability property. The CYP3A4 isoenzyme metabolizes the majority of the drugs (65%).

Methods: The characteristics of targeted probe drugs were observed from the admetSAR (version2) online database.

Results: Midazolam is widely used as a probe drug because of its peculiar character. Midazolam affirms the accurate and consistent prediction of pharmacokinetic mediated drug interactions even in nanogram concentrations with or without a potent CYP3A inhibitor. Remarkably, midazolam is used as a CYP3A4 substrate in the majority of in vivo studies.

Conclusion: It is concluded that midazolam shows a good response in all clinical studies because of its lesser half-life and bioavailability when compared with other probe drugs.

Keywords: Probe drug, CYP3A4, midazolam, drug interactions, substrates, inhibitor, CAM.

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Article Details

Year: 2021
Published on: 11 August, 2020
Page: [2 - 4]
Pages: 3
DOI: 10.2174/1872312814666200811110024
Price: $65

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