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Remdesivir potently inhibits carboxylesterase-2 through covalent modifications: signifying strong drug-drug interactions.
Shen, Yue; Eades, William; Yan, Bingfang.
  • Shen Y; Division of Pharmaceutical Sciences, James L. Winkle College of Pharmacy, University of Cincinnati, Cincinnati, OH, USA.
  • Eades W; Division of Pharmaceutical Sciences, James L. Winkle College of Pharmacy, University of Cincinnati, Cincinnati, OH, USA.
  • Yan B; Division of Pharmaceutical Sciences, James L. Winkle College of Pharmacy, University of Cincinnati, Cincinnati, OH, USA.
Fundam Clin Pharmacol ; 35(2): 432-434, 2021 Apr.
Article in English | MEDLINE | ID: covidwho-998909
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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Full text: Available Collection: International databases Database: MEDLINE Main subject: Antiviral Agents / Adenosine Monophosphate / Carboxylesterase / Alanine / Enzyme Inhibitors Type of study: Prognostic study Limits: Humans Language: English Journal: Fundam Clin Pharmacol Journal subject: Pharmacology Year: 2021 Document Type: Article Affiliation country: Fcp.12643

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Full text: Available Collection: International databases Database: MEDLINE Main subject: Antiviral Agents / Adenosine Monophosphate / Carboxylesterase / Alanine / Enzyme Inhibitors Type of study: Prognostic study Limits: Humans Language: English Journal: Fundam Clin Pharmacol Journal subject: Pharmacology Year: 2021 Document Type: Article Affiliation country: Fcp.12643