ArticleScience translational medicine2024
The oral nucleoside prodrug GS-5245 is efficacious against SARS-CoV-2 and other endemic, epidemic, and enzootic coronaviruses.
Article in Science translational medicine, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed.
- Identification of key metabolic enzymes involved in the activation of obeldesivir and remdesivir to the active triphosphate metabolite.Antimicrobial agents and chemotherapy · 2026Article
- The 5'-Isobutyryl Ester Prodrug of 4'-Thiouridine Inhibits SARS-CoV‑2 Replication in Culture and in a Syrian Hamster Infection Model.ACS omega · 2026Article
- Pharmacokinetics, Safety, and Tolerability of Obeldesivir in Healthy Japanese and White Participants.European journal of drug metabolism and pharmacokinetics · 2026Article
- Addressing the zoonotic threat of merbecoviruses.Nature microbiology · 2026Review
- Stereoselective synthesis of 1'-α-cyano carbocyclic pyrimidine nucleoside analogsOrganic & biomolecular chemistry · 2026Article
- Extending the Targets for Coronavirus Antivirals Beyond That of Approved Drugs: Insights From Preclinical Research.Microbial biotechnology · 2026Review
- Prodrug strategies in developing antiviral nucleoside analogs.RSC medicinal chemistry · 2026Review
- 1'-Cyanocytidine-5'-isobutyryl is a potent SARS-CoV-2 inhibitor in culture and infected Syrian hamsters.Science advances · 2025Article
- Article
- Phylogeny-driven design of broadly protective sarbecovirus receptor-binding domain nanoparticle vaccines.bioRxiv : the preprint server for biology · 2025Article
- Broad-Spectrum Antiviral Activity of the Orally Bioavailable Antiviral ATV014 Against Multiple Coronaviruses.MedComm · 2025Article
- Emerging Strategies and Progress in the Medical Management of Marburg Virus Disease.Pathogens (Basel, Switzerland) · 2025Review
- Remdesivir and Obeldesivir Retain Potent Antiviral Activity Against SARS-CoV-2 Omicron Variants.Viruses · 2025Article
- An oral non-covalent non-peptidic inhibitor of SARS-CoV-2 Mpro ameliorates viral replication and pathogenesis in vivo.Cell reports · 2024Article
- Oral pharmacokinetics and efficacy of oral phospholipid remdesivir nucleoside prodrugs against SARS-CoV-2 in mice.Antimicrobial agents and chemotherapy · 2024Article
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Abstract
Despite the wide availability of several safe and effective vaccines that prevent severe COVID-19, the persistent emergence of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) variants of concern (VOCs) that can evade vaccine-elicited immunity remains a global health concern. In addition, the emergence of SARS-CoV-2 VOCs that can evade therapeutic monoclonal antibodies underscores the need for additional, variant-resistant treatment strategies. Here, we characterize the antiviral activity of GS-5245, obeldesivir (ODV), an oral prodrug of the parent nucleoside GS-441524, which targets the highly conserved viral RNA-dependent RNA polymerase (RdRp). We show that GS-5245 is broadly potent in vitro against alphacoronavirus HCoV-NL63, SARS-CoV, SARS-CoV-related bat-CoV RsSHC014, Middle East respiratory syndrome coronavirus (MERS-CoV), SARS-CoV-2 WA/1, and the highly transmissible SARS-CoV-2 BA.1 Omicron variant. Moreover, in mouse models of SARS-CoV, SARS-CoV-2 (WA/1 and Omicron B1.1.529), MERS-CoV, and bat-CoV RsSHC014 pathogenesis, we observed a dose-dependent reduction in viral replication, body weight loss, acute lung injury, and pulmonary function with GS-5245 therapy. Last, we demonstrate that a combination of GS-5245 and main protease (M
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