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Remdesivir and related

Remdesivir is a prodrug form of the antiviral nucleotide analog GS-443902.Upon entry into cells, remdesivir is metabolized into the intermediate metabolite GS-441524, which is then further metabolized to the active nucleotide triphosphate GS-443902 that induces RNA chain termination and inhibits viral polymerases.Remdesivir reduces viral titers in primary human airway epithelial (HAE) cells infected with Middle East respiratory syndrome coronavirus (MERS-CoV) or severe acute respiratory syndrome CoV (SARS-CoV; EC50s = 0.074 and 0.069 µM, respectively). It reduces infectious virus production in SARS-CoV-2-infected HAE cells (EC50 = 10 nM). In vivo, remdesivir (25 and 50 mg/kg) reduces lung viral titers and prevents weight loss in a mouse model of SARS-CoV infection.Remdesivir (25 mg/kg) also reduces lung viral titers and lung hemorrhage and improves pulmonary function in mice infected with a chimeric SARS-CoV encoding the SARS-CoV-2 RNA-dependent RNA polymerase (RdRp).Formulations containing remdesivir have been used in the treatment of COVID-19.