Remdesivir potently inhibits carboxylesterase‐2 through covalent modifications: signifying strong drug‐drug interactions
Yue Shen, William C. Eades, Bingfang Yan · Fundamental and Clinical Pharmacology · 2020
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.