ArticleAntimicrobial agents and chemotherapy2026
Identification of key metabolic enzymes involved in the activation of obeldesivir and remdesivir to the active triphosphate metabolite.
Article in Antimicrobial agents and chemotherapy, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
Obeldesivir (GS-5245, ODV), an orally administered 5'-isobutyryl ester prodrug of GS-441524, has demonstrated anti-SARS-CoV-2 activity in preclinical and clinical settings. ODV is hydrolyzed in plasma to provide high systemic exposures of GS-441524, enabling the efficient intracellular formation of the bioactive 5'-triphosphate GS-443902, an ATP analog inhibiting the SARS-CoV-2 RNA-dependent RNA polymerases. Remdesivir (RDV), the first US FDA-approved antiviral treatment for COVID-19, is also activated to GS-443902. In this paper, we systematically profiled the human enzymes potentially involved in ODV and RDV activation using multiple approaches: (i) biochemical studies on the catalytic efficiency (
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