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Remdesivir potently inhibits carboxylesterase‐2 through covalent modifications: signifying strong drug‐drug interactions
Author(s) -
Shen Yue,
Eades William,
Yan Bingfang
Publication year - 2021
Publication title -
fundamental and clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.655
H-Index - 73
eISSN - 1472-8206
pISSN - 0767-3981
DOI - 10.1111/fcp.12643
Subject(s) - carboxylesterase , drug , pharmacology , potency , chemistry , covalent bond , organophosphate , enzyme , medicine , biochemistry , in vitro , biology , organic chemistry , pesticide , agronomy
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.