The mechanism of resistance to favipiravir in influenza
File(s)
Author(s)
Type
Journal Article
Abstract
Favipiravir is a broad-spectrum antiviral that has shown promise in treatment of influenza virus infections. While emergence of resistance has been observed for many antiinfluenza drugs, to date, clinical trials and laboratory studies of favipiravir have not yielded resistant viruses. Here we show evolution of resistance to favipiravir in the pandemic H1N1 influenza A virus in a laboratory setting. We found that two mutations were required for robust resistance to favipiravir. We demonstrate that a K229R mutation in motif F of the PB1 subunit of the influenza virus RNA-dependent RNA polymerase (RdRP) confers resistance to favipiravir in vitro and in cell culture. This mutation has a cost to viral fitness, but fitness can be restored by a P653L mutation in the PA subunit of the polymerase. K229R also conferred favipiravir resistance to RNA polymerases of other influenza A virus strains, and its location within a highly conserved structural feature of the RdRP suggests that other RNA viruses might also acquire resistance through mutations in motif F. The mutations identified here could be used to screen influenza virus-infected patients treated with favipiravir for the emergence of resistance.
Date Issued
2018-11-06
Date Acceptance
2018-10-02
Citation
Proceedings of the National Academy of Sciences of the United States of America, 2018, 115 (45), pp.11613-11618
ISSN
0027-8424
Publisher
National Academy of Sciences
Start Page
11613
End Page
11618
Journal / Book Title
Proceedings of the National Academy of Sciences of the United States of America
Volume
115
Issue
45
Copyright Statement
© 2018 the Author(s). Published by PNAS. This open access article is distributed under Creative Commons Attribution-NonCommercial-NoDerivatives License 4.0 (CC BY-NC-ND - https://creativecommons.org/licenses/by-nc-nd/4.0/).
Identifier
http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcApp=PARTNER_APP&SrcAuth=LinksAMR&KeyUT=WOS:000449459000079&DestLinkType=FullRecord&DestApp=ALL_WOS&UsrCustomerID=1ba7043ffcc86c417c072aa74d649202
Subjects
Science & Technology
Multidisciplinary Sciences
Science & Technology - Other Topics
antiviral
resistance
polymerase
influenza
virus
VIRAL-RNA POLYMERASE
T-705 FAVIPIRAVIR
A VIRUSES
IN-VITRO
LETHAL MUTAGENESIS
OSELTAMIVIR
RIBAVIRIN
SUSCEPTIBILITY
EVOLUTION
COMBINATIONS
Publication Status
Published
Date Publish Online
2018-10-23