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

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

Volume: 14 Issue: 1

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

Affiliation:

• Department of Pharmacy Practice, SRM College of Pharmacy, SRM Institute of Science and Technology, SRM Nagar, Kattankulathur, 603203, Kanchipuram, Chennai, TN,India

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

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.

Cite this article as:

Sabarathinam Sarvesh and Vijayakumar M. Thangavel *, A Short Exploration of Selected Sensitive CYP3A4 Substrates (Probe Drug), Drug Metabolism Letters 2021; 14 (1) . https://dx.doi.org/10.2174/1872312814666200811110024