Статус Emergency use authorization (EUA) FDA.
Программа расширенного доступа в странах Евросоюза.
ЕМА выдало статус Conditional marketing authorisation.
Remdesivir is a monophosphoramidate prodrug of remdesivirtriphosphate (RDV-TP), an adenosine analog that acts as an inhibitor of RNA-dependent RNA polymerases (RdRps). Remdesivir-TP competes with adenosine-triphosphate for incorporation into nascent viral RNA chains. Once incorporated into the viral RNA at position i, RDV-TP terminates RNA synthesis at position i+3. Because RDV-TP does not cause immediate chain termination (i.e., 3 additional nucleotides are incorporated after RDV-TP), the drug appears to evade proofreading by viral exoribonuclease (an enzyme thought to excise nucleotide analog inhibitors).
Remdesivir has been administered to several hundred patients with confirmed, severe SARS-CoV-2 infections in the United States, Europe, and Japan through Expanded Access or Compassionate Use programs.
In preclinical trials, remdesivir has demonstrated significant activity against coronavirus and a high genetic barrier to resistance.
- In vitro data found remdesivir exerts potent antiviral activity against a clinical isolate of SARS-CoV-2; [half-maximal effective concentration (EC50) = 0.77 mcgM, half-cytotoxic concentration (CC50) greater than 100 mcgM, selective index (SI) greater than 129.87].
- Data suggest remdesivir (GS-5735) inhibits activity of 2002 SARS-CoV, MERS-CoV, and bat CoV strains that have the ability to replicate in human epithelial cells and mediate entry via human CoV receptors.
- Remdesivir has shown prophylactic and therapeutic efficacy against 2002 SARS-CoV in a mouse model.
- Resistance mutations have not been identified.
Several clinical trials evaluating the efficacy of remdesivir in patients infected with SARS-CoV-2 are currently being conducted. Data from some trials are expected by April 2020.
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