Remdesivir-d4 is intended for use as an internal standard for the quantification of remdesivir by GC- or LC-MS. Remdesivir is a prodrug form of the antiviral nucleoside analog GS-441524 .1,2 Upon entry into cells, remdesivir is metabolized into a nucleoside monophosphate form, which is further metabolized to an active nucleotide triphosphate that induces RNA chain termination and inhibits viral polymerases.3 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).4 In vivo, remdesivir (25 and 50 mg/kg) reduces lung viral titers and prevents weight loss in a mouse model of SARS-CoV infection.2 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).4 Formulations containing remdesivir have been used in the treatment of COVID-19.
1.Agostini, M.L., Andres, E.L., Sims, A.C., et al.Coronavirus susceptibility to the antiviral remdesivir (GS-5734) is mediated by the viral polymerase and the proofreading exoribonucleasemBio9(2)e00221-00218(2018) 2.Sheahan, T.P., Sims, A.C., Graham, R.L., et al.Broad-spectrum antiviral GS-5734 inhibits both epidemic and zoonotic coronavirusesSci. Transl. Med.9(396)eaal3653(2017) 3.Eastman, R.T., Roth, J.S., Brimacombe, K.R., et al.Remdesivir: A review of its discovery and development leading to emergency use authorization for treatment of COVID-19ACS Cent. Sci.6(5)672-683(2020) 4.Pruijssers, A.J., George, A.S., SchÄfer, A., et al.Remdesivir inhibits SARS-CoV-2 in human lung cells and chimeric SARS-CoV expressing the SARS-CoV-2 RNA polymerase in miceCell Rep.32(3)107940(2020)