Remdesivir has received significant attention for its potential application in the treatment of COVID-19, caused by SARS-CoV-2. Remdesivir has already been tested for Ebola virus disease treatment and found to have activity against SARS and MERS coronaviruses. The remdesivir core contains GS-441524, which interferes with RNA-dependent RNA polymerases alone. In non-human primates, following IV administration, remdesivir is rapidly distributed into PBMCs and converted within 2 h to the active nucleoside triphosphate form, while GS-441524 is detectable in plasma for up to 24 h. Nevertheless, remdesivir pharmacokinetics and pharmacodynamics in humans are still unexplored, highlighting the need for a precise analytical method for remdesivir and GS-441524 quantification.

Development and validation of a UHPLC-MS/MS method for quantification of the prodrug remdesivir and its metabolite GS-441524: a tool for clinical pharmacokinetics of SARS-CoV-2/COVID-19 and Ebola virus disease

Avataneo, Valeria
First
;
de Nicolò, Amedeo;Cusato, Jessica;Antonucci, Miriam;Manca, Alessandra;Palermiti, Alice;di Perri, Giovanni;D'Avolio, Antonio
Last
2020-01-01

Abstract

Remdesivir has received significant attention for its potential application in the treatment of COVID-19, caused by SARS-CoV-2. Remdesivir has already been tested for Ebola virus disease treatment and found to have activity against SARS and MERS coronaviruses. The remdesivir core contains GS-441524, which interferes with RNA-dependent RNA polymerases alone. In non-human primates, following IV administration, remdesivir is rapidly distributed into PBMCs and converted within 2 h to the active nucleoside triphosphate form, while GS-441524 is detectable in plasma for up to 24 h. Nevertheless, remdesivir pharmacokinetics and pharmacodynamics in humans are still unexplored, highlighting the need for a precise analytical method for remdesivir and GS-441524 quantification.
2020
75
7
1772
1777
Avataneo, Valeria; de Nicolò, Amedeo; Cusato, Jessica; Antonucci, Miriam; Manca, Alessandra; Palermiti, Alice; Waitt, Catriona; Walimbwa, Stephen; Lamorde, Mohammed; di Perri, Giovanni; D'Avolio, Antonio
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2318/1759603
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