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Remdesivir: Quo vadis?()

Remdesivir (GS-5734, Veklury®) has remained the only antiviral drug formally approved by the US FDA for the treatment of Covid-19 (SARS-CoV-2 infection). Its key structural features are the fact that it is a C-nucleoside (adenosine) analogue, contains a 1′-cyano function, and could be considered as...

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Autor principal: De Clercq, Erik
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier Inc. 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8524699/
https://www.ncbi.nlm.nih.gov/pubmed/34678228
http://dx.doi.org/10.1016/j.bcp.2021.114800
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author De Clercq, Erik
author_facet De Clercq, Erik
author_sort De Clercq, Erik
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description Remdesivir (GS-5734, Veklury®) has remained the only antiviral drug formally approved by the US FDA for the treatment of Covid-19 (SARS-CoV-2 infection). Its key structural features are the fact that it is a C-nucleoside (adenosine) analogue, contains a 1′-cyano function, and could be considered as a ProTide based on the presence of a phosphoramidate group. Its antiviral spectrum and activity in animal models have been well established and so has been its molecular mode of action as a delayed chain terminator of the viral RdRp (RNA-dependent RNA polymerase). Its clinical efficacy has been evaluated, but needs to be optimized with regard to timing, dosage and duration of treatment, and route of administration. Safety, toxicity and pharmacokinetics need to be further addressed, and so are its potential combinations with other drugs such as corticosteroids (i.e. dexamethasone) and ribavirin.
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spelling pubmed-85246992021-10-20 Remdesivir: Quo vadis?() De Clercq, Erik Biochem Pharmacol Review Remdesivir (GS-5734, Veklury®) has remained the only antiviral drug formally approved by the US FDA for the treatment of Covid-19 (SARS-CoV-2 infection). Its key structural features are the fact that it is a C-nucleoside (adenosine) analogue, contains a 1′-cyano function, and could be considered as a ProTide based on the presence of a phosphoramidate group. Its antiviral spectrum and activity in animal models have been well established and so has been its molecular mode of action as a delayed chain terminator of the viral RdRp (RNA-dependent RNA polymerase). Its clinical efficacy has been evaluated, but needs to be optimized with regard to timing, dosage and duration of treatment, and route of administration. Safety, toxicity and pharmacokinetics need to be further addressed, and so are its potential combinations with other drugs such as corticosteroids (i.e. dexamethasone) and ribavirin. Elsevier Inc. 2021-11 2021-10-19 /pmc/articles/PMC8524699/ /pubmed/34678228 http://dx.doi.org/10.1016/j.bcp.2021.114800 Text en © 2021 Elsevier Inc. All rights reserved. Since January 2020 Elsevier has created a COVID-19 resource centre with free information in English and Mandarin on the novel coronavirus COVID-19. The COVID-19 resource centre is hosted on Elsevier Connect, the company's public news and information website. Elsevier hereby grants permission to make all its COVID-19-related research that is available on the COVID-19 resource centre - including this research content - immediately available in PubMed Central and other publicly funded repositories, such as the WHO COVID database with rights for unrestricted research re-use and analyses in any form or by any means with acknowledgement of the original source. These permissions are granted for free by Elsevier for as long as the COVID-19 resource centre remains active.
spellingShingle Review
De Clercq, Erik
Remdesivir: Quo vadis?()
title Remdesivir: Quo vadis?()
title_full Remdesivir: Quo vadis?()
title_fullStr Remdesivir: Quo vadis?()
title_full_unstemmed Remdesivir: Quo vadis?()
title_short Remdesivir: Quo vadis?()
title_sort remdesivir: quo vadis?()
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8524699/
https://www.ncbi.nlm.nih.gov/pubmed/34678228
http://dx.doi.org/10.1016/j.bcp.2021.114800
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