molecules of the month


oral antiviral prodrug of remdesivir

effective in a ferret SARS-CoV-2 model

from remdesivir nucleoside (GS-441524)

Nature Communications

Gilead Sciences Inc.

Chemical structure of molecule GS-621763 Gilead SARS-CoV-2 drug
1 min read

2.      The Gilead SARS-CoV-2 drug, GS-621763, is an oral prodrug of the parent nucleoside of remdesivir (GS-441524) which demonstrated therapeutic and prophylactic efficacy in a ferret model of SARS-CoV-2 infection, significantly reducing viral load to near-undetectable levels with twice-daily administration. Remdesivir is already FDA approved as an IV medication, and this orally available counterpart would greatly improve its utility in combating Covid especially in outpatient settings.  GS-621763 is pre-systemically hydrolyzed to provide high systemic exposures of GS-441524, which is converted in lungs to the triphosphate metabolite; identical to the metabolite generated by remdesivir. The potential human daily oral dose of this molecule is estimated to be roughly 250 mg. This is another proof-of-concept that suggests that oral pills and combinations of…

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