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

Drug metabolism letters Pub Date : 2021-01-01 DOI:10.2174/1872312814666200811110024

Sarvesh Sabarathinam, Thangavel M Vijayakumar

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引用次数: 6

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.

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筛选CYP3A4敏感底物(探针药物)的简短探索。

背景:肝脏CYP450酶在外源性药物代谢中具有重要作用。探针药物策略广泛用于评估药物/草药-药物相互作用/食物-药物相互作用的药效学和药代动力学。探针药物通过其靶向性揭示了药物在肝脏中代谢的确切途径。CYP3A4同工酶代谢大部分药物(65%)。方法:从admetSAR (version2)在线数据库中观察靶向探针药物的特征。结果:咪达唑仑因其独特的性质被广泛用作探针药物。咪达唑仑证实了药物动力学介导的药物相互作用的准确和一致的预测，即使在纳克浓度下，有或没有有效的CYP3A抑制剂。值得注意的是，咪达唑仑在大多数体内研究中被用作CYP3A4底物。结论:咪达唑仑与其他探针药物相比，具有较短的半衰期和生物利用度，在所有临床研究中均表现出较好的疗效。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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Drug metabolism letters Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science

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期刊介绍： Drug Metabolism Letters publishes letters and research articles on major advances in all areas of drug metabolism and disposition. The emphasis is on publishing quality papers very rapidly by taking full advantage of the Internet technology both for the submission and review of manuscripts. The journal covers the following areas: In vitro systems including CYP-450; enzyme induction and inhibition; drug-drug interactions and enzyme kinetics; pharmacokinetics, toxicokinetics, species scaling and extrapolations; P-glycoprotein and transport carriers; target organ toxicity and interindividual variability; drug metabolism and disposition studies; extrahepatic metabolism; phase I and phase II metabolism; recent developments for the identification of drug metabolites.