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Fundam Clin Pharmacol · Apr 2021
Remdesivir potently inhibits carboxylesterase-2 through covalent modifications: signifying strong drug-drug interactions.
- Yue Shen, William Eades, and Bingfang Yan.
- Division of Pharmaceutical Sciences, James L. Winkle College of Pharmacy, University of Cincinnati, Cincinnati, OH, USA.
- Fundam Clin Pharmacol. 2021 Apr 1; 35 (2): 432-434.
AbstractRemdesivir 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.© 2020 Société Française de Pharmacologie et de Thérapeutique.
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