Selected article for: "active form and drug resistance"
Author: McCreary, Erin K; Pogue, Jason M
Title: Coronavirus Disease 2019 Treatment: A Review of Early and Emerging Options
  • Document date: 2020_3_23
    • ID: j0i9ozsz_4
    Snippet: Gilead Sciences, Inc. in response to the Ebola outbreak in West Africa from 2014 to 2016. In its active triphosphate nucleoside form, remdesivir binds to ribonucleic acid (RNA)-dependent RNA polymerase and acts as an RNA-chain terminator. It displays potent in vitro activity against SARS-CoV-2 with an EC 50 at 48 hours of 0.77 µM in Vero E6 cells [3] . Similar activity has been demonstrated against other zoonotic coronaviruses with EC 50 values .....
    Document: Gilead Sciences, Inc. in response to the Ebola outbreak in West Africa from 2014 to 2016. In its active triphosphate nucleoside form, remdesivir binds to ribonucleic acid (RNA)-dependent RNA polymerase and acts as an RNA-chain terminator. It displays potent in vitro activity against SARS-CoV-2 with an EC 50 at 48 hours of 0.77 µM in Vero E6 cells [3] . Similar activity has been demonstrated against other zoonotic coronaviruses with EC 50 values of 0.07 µM demonstrated for both SARS-CoV-1 and MERS-CoV [3] [4] [5] [6] . Remdesivir is highly selective for viral polymerases and is therefore expected to have a low propensity to cause human toxicity. Accordingly, Sheahan et al [6] demonstrated a wide therapeutic index for remdesivir in a human airway epithelial cell model. The drug also displays a high genetic barrier to resistance in coronaviruses and has a long intracellular half-life that allows for once-daily dosing [7, 8] . The dose under investigation for treatment of COVID-19 is 200 mg intravenously (IV) on day 1 followed by 100 mg IV daily for up to 10 days, infused over 30-60 minutes ( Table 1) .

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