Synonyms: compound 4b [PMID: 28124907] | GS-5734 | GS5734 | Veklury®
remdesivir is an approved drug (FDA & EMA (2020))
Compound class:
Synthetic organic
Comment: Remdesivir (GS-5734) is a nucleotide analogue drug that was developed by Gilead Sciences for antiviral potential, in particular for anti-Ebola and anti-Marburg virus activity [7]. It acts is an inhibitor of the viral RNA-dependent RNA polymerase (RdRP) that functions as a chain terminator during viral RNA synthesis. Remdesivir is a prodrug whose major active metabolite is GS-441524. Its 1'-CN group and C-linked nucleobase ensure optimal anti-Ebola potency and selectivity against host polymerase enzymes. Remdesivir has broad-spectrum activity against several viral families such as filoviruses, paramyxoviruses, and coronaviruses, and including the SARS and MERS coronaviruses (CoVs), endemic circulating human CoVs, and against SARS-CoV-2 [1-2,6]. The first patient to test positive for SARS-CoV-2 in the US was treated with i.v. remdesivir (using compassionate use of an investigational therapy prescribing) and his clinical condition improved significantly within the next 24h without observation of adverse effects [4].
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Bioactivity Comments |
Remdesivir (GS-5734) inhibits SARS-CoV and MERS-CoV replication in multiple in vitro systems, including primary human airway epithelial cell cultures, and activity in animal models is suggestive of prophylactic potential following early therapeutic administration [6]. It exhibits antiviral activity against Ebola virus in human macrophages (EC50 86 nM) [7]. |
Selectivity at other protein targets | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Targets where the ligand is described in the comment field | |
Target | Comment |
CoV RNA-dependent RNA polymerase | The conservation of RdRP catalytic domain between different RNA viruses endows inhibitors that were designed against other viral pathogens with activity against the SARS coronaviruses. Viral RdRP is the molecular target of nucleotide-based broad-spectrum antiviral compounds like remdesivir, tenofovir and ribavirin [2,8-9]. |