Comparison of anti-SARS-CoV-2 activity and intracellular metabolism of remdesivir and its parent nucleoside

Comparison of anti-SARS-CoV-2 activity and intracellular metabolism of remdesivir and its parent nucleoside

Remdesivir, a monophosphate prodrug of nucleoside analog GS-441524, is widely used for the treatment of moderate to severe COVID-19. It has been suggested to use GS-441524 instead of remdesivir in the clinic and in new inhalation formulations. Thus, we compared the anti-SARS-CoV-2 activity of remdes...

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Bibliographic Details
Main Authors: Sijia Tao, Keivan Zandi, Leda Bassit, Yee Tsuey Ong, Kiran Verma, Peng Liu, Jessica A. Downs-Bowen, Tamara McBrayer, Julia C. LeCher, James J. Kohler, Philip R. Tedbury, Baek Kim, Franck Amblard, Stefan G. Sarafianos, Raymond F. Schinazi
Format: Article
Language:English
Published: Elsevier 2021-01-01
Series:Current Research in Pharmacology and Drug Discovery
Subjects:
COVID-19
Antiviral agents
Coronavirus
Anti-SARS-CoV-2
Remdesivir
GS-441524
Online Access:http://www.sciencedirect.com/science/article/pii/S2590257121000328
Description
Summary:Remdesivir, a monophosphate prodrug of nucleoside analog GS-441524, is widely used for the treatment of moderate to severe COVID-19. It has been suggested to use GS-441524 instead of remdesivir in the clinic and in new inhalation formulations. Thus, we compared the anti-SARS-CoV-2 activity of remdesivir and GS-441524 in Vero E6, Vero CCL-81, Calu-3, Caco-2 ​cells, and anti-HCoV-OC43 activity in Huh-7 ​cells. We also compared the cellular pharmacology of these two compounds in Vero E6, Vero CCL-81, Calu-3, Caco-2, Huh-7, 293T, BHK-21, 3T3 and human airway epithelial (HAE) cells. Overall, remdesivir exhibited greater potency and superior intracellular metabolism than GS-441524 except in Vero E6 and Vero CCL-81 ​cells.
ISSN:2590-2571

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