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Drug Metabolism Letters

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ISSN (Print): 1872-3128
ISSN (Online): 1874-0758

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Opinion Article

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

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

Volume 14, Issue 1, 2021

Published on: 11 August, 2020

Page: [2 - 4] Pages: 3

DOI: 10.2174/1872312814666200811110024

Price: $65

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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