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瑞德西韦通过共价修饰有效抑制羧酸酯酶-2：表明存在强烈的药物相互作用。

Remdesivir potently inhibits carboxylesterase-2 through covalent modifications: signifying strong drug-drug interactions.

作者信息

Shen Yue, Eades William, Yan Bingfang

机构信息

Division of Pharmaceutical Sciences, James L. Winkle College of Pharmacy, University of Cincinnati, Cincinnati, OH, USA.

出版信息

Fundam Clin Pharmacol. 2021 Apr;35(2):432-434. doi: 10.1111/fcp.12643. Epub 2021 Jan 6.

DOI:10.1111/fcp.12643
PMID:33369768
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8284663/
Abstract

Remdesivir was recently approved to treat COVID-19. While this antiviral agent delivers clinical benefits, several safety concerns in many cases have been raised. This study reports that remdesivir at nanomolar concentrations inhibits carboxylesterase-2 (CES2) through covalent modifications. CES2 is a major drug-metabolizing enzyme. The combination of high potency with irreversible inhibition concludes that cautions must be exercised when remdesivir is used along with drugs hydrolyzed by CES2.

摘要

瑞德西韦最近被批准用于治疗新冠肺炎。虽然这种抗病毒药物带来了临床益处，但在许多情况下也引发了一些安全问题。本研究报告称，纳摩尔浓度的瑞德西韦通过共价修饰抑制羧酸酯酶-2（CES2）。CES2是一种主要的药物代谢酶。高效力与不可逆抑制的结合表明，当瑞德西韦与由CES2水解的药物联合使用时必须谨慎。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f7be/8284663/1f0d35e2a6b2/nihms-1721926-f0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f7be/8284663/1f0d35e2a6b2/nihms-1721926-f0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f7be/8284663/1f0d35e2a6b2/nihms-1721926-f0001.jpg

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