ArticleACS medicinal chemistry letters2022
Phosphoramidate Prodrugs Continue to Deliver, The Journey of Remdesivir (GS-5734) from RSV to SARS-CoV-2.
Article in ACS medicinal chemistry letters, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
What it found
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
21 citing papers in PubMed.
- Towards broader-spectrum direct-acting antivirals against RNA viruses.Nature reviews. Microbiology · 2026Review
- Medicinal Chemistry Perspectives on Drug Repurposing: Innovative Approaches and Therapeutic Breakthrough.Therapeutic innovation & regulatory science · 2026Review
- Catching our breath: development of interventions and therapies for respiratory syncytial virus.Microbiology and molecular biology reviews : MMBR · 2026Review
- Phosphoramidate Derivatives of Betulin, New Molecules with Promising Biological Activity: Synthesis and Characterization.Molecules (Basel, Switzerland) · 2026Article
- Fluorogenic Imaging Enables the Identification of Phosphoramidate Antibody-Drug Conjugate Linkers.Bioconjugate chemistry · 2026Article
- Review
- Photoinduced, Copper-Catalyzed Enantioconvergent Azidation of Alkyl Halides.Journal of the American Chemical Society · 2025Article
- Advances and Challenges in Antiviral Development for Respiratory Viruses.Pathogens (Basel, Switzerland) · 2024Review
- Clinical pharmacodynamics of obeldesivir versus remdesivir.Antimicrobial agents and chemotherapy · 2024Article
- The activation cascade of the broad-spectrum antiviral bemnifosbuvir characterized at atomic resolution.PLoS biology · 2024Article
- Differential Bioactivation Profiles of Different GS-441524 Prodrugs in Cell and Mouse Models: ProTide Prodrugs with High Cell Permeability and Susceptibility to Cathepsin A Are More Efficient in Delivering Antiviral Active Metabolites to the Lung.Journal of medicinal chemistry · 2024Article
- The landscape of small-molecule prodrugs.Nature reviews. Drug discovery · 2024Review
- SARS-CoV-2 resistance to monoclonal antibodies and small-molecule drugs.Cell chemical biology · 2024Review
- Anti-COVID-19, Anti-Inflammatory, and Anti-Osteoarthritis Activities of Sesamin fromBioengineering (Basel, Switzerland) · 2023Article
- Cell-Dependent Activation of ProTide Prodrugs and Its Implications in Antiviral Studies.ACS pharmacology & translational science · 2023Article
- The Many Faces of Histidine Triad Nucleotide Binding Protein 1 (HINT1).ACS pharmacology & translational science · 2023Review
- Structure-Based Drug Design of RdRp Inhibitors against SARS-CoV-2.Topics in current chemistry (Cham) · 2023Review
- An Isomer of Galidesivir That Potently Inhibits Influenza Viruses and Members of theACS medicinal chemistry letters · 2023Article
- Can changing the prodrug moiety in remdesivir be a life-saving strategy in COVID-19 infection?The Indian journal of medical research · 2023Article
- RETRACTED: Synthesis and Evaluation of Anti-HIV Activity of Mono- and Di-Substituted Phosphonamidate Conjugates of Tenofovir.Molecules (Basel, Switzerland) · 2022Article
Corrections and comments
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Authors and funding
1 author.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Remdesivir (GS-5734) is a monophenol, 2-ethylbutylalanine phosphoramidate prodrug of a 1'-cyano-4-aza-7,9-dideazaadenosine C-nucleoside (GS-441524) that is FDA approved for the treatment of hospitalized patients with COVID-19. The prodrug, initially invented for respiratory syncytial virus, was later found to have activity toward emerging RNA viruses, including Ebola and coronaviruses. Remdesivir is among the first examples of a phosphoramidate prodrug aimed at delivering a nucleoside monophosphate into lung cells to efficiently generate the nucleoside triphosphate inhibitor of viral RNA polymerases. With remdesivir as the central case study, the present work describes the antiviral potency and in vitro metabolism evidence for lung cell activation of phosphoramidates, together with their in vivo pharmacokinetics, lung distribution, and antiviral efficacy toward respiratory viruses. The lung delivery of nucleoside monophosphate analogs using prodrugs warrants further investigation toward the development of novel respiratory antivirals.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.