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

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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.

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Shen, Y., Eades, W., & Yan, B. (2021). Remdesivir potently inhibits carboxylesterase-2 through covalent modifications: signifying strong drug-drug interactions. Fundamental and Clinical Pharmacology, 35(2), 432–434. https://doi.org/10.1111/fcp.12643

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