Novel hepatitis B virus reverse transcriptase mutations in patients with sustained viremia despite long-term tenofovir treatment

J Clin Virol. 2022 Jun:150-151:105159. doi: 10.1016/j.jcv.2022.105159. Epub 2022 Apr 12.

Abstract

Background: Chronic hepatitis B virus (HBV) treatment consists of nucleos(t)ide analogues to suppress viral replication. The HBV inhibitor tenofovir has a high barrier to resistance, however, evidence of virus-escape is emerging. This study investigates HBV evolution in patients undergoing tenofovir treatment with the primary aim to assess the emergence of putative resistance mutations.

Methods: HBV DNA was extracted from blood samples of two patients with HBeAg-positive chronic HBV infection and persistent viremia despite tenofovir treatment, and subsequently amplified by PCR before full-length HBV genomes were assembled by deep sequencing. The mutation linkage within the viral population was evaluated by clonal analysis of amplicons.

Results: Sequence analysis of HBV, derived from 11 samples collected 2010-2020 from one patient, identified 12 non-synonymous single-nucleotide polymorphisms (SNPs) emerging during a tenofovir treatment interruption from 2014 to 2017. Two of the SNPs were in the reverse transcriptase (RT; H35Q and D263E). The two RT mutations were linked and persisted despite restarting tenofovir treatment in 2017. For the second patient, we analyzed HBV derived from six samples collected 2014-2020 following 10 years of tenofovir treatment, and identified five non-synonymous SNPs, that confer resistance towards entecavir and/or lamivudine. Two RT mutations (H35N and P237T) emerged during subsequent 5-year entecavir treatment. H35N was maintained during final tenofovir treatment.

Conclusions: Our findings indicate that changes at the conserved residue 35 (H35N/Q) in the HBV RT may be associated with tenofovir resistance. These variants have not previously been described, and further studies are warranted to assess resistance in vitro and in vivo.

Keywords: DANHEP; Hepatitis B virus infection; Hepatitis B virus sequencing; Tenofovir disoproxil fumarate; Tenofovir resistance.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenine / adverse effects
  • Antiviral Agents / pharmacology
  • Antiviral Agents / therapeutic use
  • DNA, Viral / genetics
  • Drug Resistance, Viral / genetics
  • Hepatitis B virus / genetics
  • Hepatitis B, Chronic* / drug therapy
  • Humans
  • Mutation
  • Organophosphonates* / therapeutic use
  • RNA-Directed DNA Polymerase / genetics
  • Tenofovir / pharmacology
  • Tenofovir / therapeutic use
  • Viremia / drug therapy

Substances

  • Antiviral Agents
  • DNA, Viral
  • Organophosphonates
  • Tenofovir
  • RNA-Directed DNA Polymerase
  • Adenine