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Phosphoramidate Prodrugs Continue to Deliver: The Journey of Remdesivir (GS-5734) from the Liver to Peripheral Blood Mononuclear Cells.

Abstract
Remdesivir (GS-5734) is a monophenol, 2-ethylbutylalanine phosphoramidate prodrug of GS-441524 that is FDA-approved for the treatment of patients hospitalized for COVID-19. Despite showing strong, broad-spectrum antiviral activity in preclinical models, the clinical efficacy of remdesivir is mixed. This work highlights the pharmacodynamic discordance of remdesivir between humans and non-human primates, thereby demonstrating that non-human primate disease models overestimate the therapeutic efficacy of phosphoramidate prodrugs.
AuthorsVictoria C Yan
JournalACS medicinal chemistry letters (ACS Med Chem Lett) Vol. 13 Issue 4 Pg. 520-523 (Apr 14 2022) ISSN: 1948-5875 [Print] United States
PMID35450350 (Publication Type: Journal Article)
Copyright© 2022 American Chemical Society.

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