Literature DB >> 32735901

Revisiting HBV resistance to entecavir with a phenotypic approach.

Julien Marlet1, Clément Lier2, Emmanuelle Roch3, Morgan Maugey3, Alain Moreau3, Benjamin Combe3, Sandrine Lefeuvre4, Louis d'Alteroche5, Didier Barbereau5, Xavier Causse6, Frédéric Bastides7, Marie-Nadege Bachelier8, Denys Brand2, Catherine Gaudy-Graffin2.   

Abstract

Treatment adaptation after hepatitis B virus (HBV) treatment failure relies on genotypic resistance testing. However, the results of such tests are not always consistent with treatment response. These discrepancies may be due to differences in resistance levels between isolates with the same genotypic resistance testing profiles. We explored this hypothesis by investigating six cases of entecavir treatment failure with an integrative strategy combining genotypic and phenotypic resistance testing, medical record review and therapeutic drug monitoring. Among isolates with genotypic reduced susceptibility to entecavir, one displayed a higher level of resistance to entecavir (mean fold change in entecavir IC50 of 1 508 ± 531 vs. 318 ± 53, p = 0.008). This isolate harbored a substitution (rt250L) at a position reported to be associated with resistance (rt250V). Reversion to wild-type amino acid at this position partially restored susceptibility to entecavir, confirming that the rt250L mutation was responsible for the high level of resistance to entecavir. This is the first description of entecavir treatment failure associated with selection of the rt250L mutation without other entecavir resistance mutations. One isolate with genotypic resistance to entecavir, harboring the rt173L mutation, displayed a lower level of resistance than the other, harboring the rt202G mutation (mean fold change of 323 ± 124 vs. 6 036 ± 2 100, p = 0.20). These results suggest that isolates harboring the rt250L mutations should be considered resistant to entecavir, whereas isolates harboring the rt173L mutations should be considered to display reduced susceptibility to entecavir. An integrative approach to antiviral drug resistance in HBV would provide a more accurate assessment of entecavir treatment failures and help to improve the accuracy of genotypic testing algorithms.
Copyright © 2020 Elsevier B.V. All rights reserved.

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Keywords:  Antiviral; Entecavir; HBV; Phenotypic; Polymerase; Resistance

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Year:  2020        PMID: 32735901     DOI: 10.1016/j.antiviral.2020.104869

Source DB:  PubMed          Journal:  Antiviral Res        ISSN: 0166-3542            Impact factor:   5.970


  1 in total

1.  Synthesis and Antiviral Evaluation of (1,4-Disubstituted-1,2,3-Triazol)-(E)-2-Methyl-but-2-Enyl Nucleoside Phosphonate Prodrugs.

Authors:  Tuniyazi Abuduaini; Vincent Roy; Julien Marlet; Catherine Gaudy-Graffin; Denys Brand; Cécile Baronti; Franck Touret; Bruno Coutard; Tamara R McBrayer; Raymond F Schinazi; Luigi A Agrofoglio
Journal:  Molecules       Date:  2021-03-09       Impact factor: 4.411

  1 in total

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