Can remdesivir and its parent nucleoside GS-441524 be potential oral drugs? An
10.1016/j.apsb.2021.03.028
- Author:
Jiashu XIE
1
;
Zhengqiang WANG
1
Author Information
1. Center for Drug Design, College of Pharmacy, University of Minnesota, Minneapolis, MN 55455, USA.
- Publication Type:Journal Article
- Keywords:
ADK, adenosine kinase;
Antiviral;
COVID-19;
CYP, cytochrome P450;
Cobi, cobicistat;
DMPK, drug metabolism and pharmacokinetics;
Drug metabolism;
EMS, enhanced mass scan;
EPI, enhanced product ion;
FIPV, feline infectious peritonitis coronavirus;
GS-441524;
HINTs, histidine triad nucleotide binding proteins;
HLMs, human liver microsomes;
IDA, information dependent acquisition;
MLMs, mouse liver microsomes;
MRM, multiple reaction monitoring;
Nucleoside;
Oral bioavailability;
RDV, remdesivir;
RdRp, RNA-dependent RNA-polymerases;
Remdesivir;
SARS-CoV-2;
SOF, sofosbuvir;
TAF, tenofovir alafenamide
- From:
Acta Pharmaceutica Sinica B
2021;11(6):1607-1616
- CountryChina
- Language:English
-
Abstract:
Remdesivir (RDV) is the only US Food and Drug Administration (FDA)-approved drug for treating COVID-19. However, RDV can only be given by intravenous route, and there is a pressing medical need for oral antivirals. Significant evidence suggests that the role of the parent nucleoside GS-441524 in the clinical outcomes of RDV could be largely underestimated. We performed an