Clonal analysis of the quasispecies of antiviral-resistant HBV genomes in patients with entecavir resistance during rescue treatment and successful treatment of entecavir resistance with tenofovir

Antivir Ther. 2013;18(1):77-85. doi: 10.3851/IMP2294. Epub 2012 Aug 10.

Abstract

Background: Clonal analysis of quasispecies of resistant HBV genomes in patients with entecavir (ETV) resistance receiving lamivudine (3TC) plus adefovir (ADV) rescue therapy has never been performed.

Methods: A sample of 10 patients with ETV resistance who were switched to 3TC+ADV treatment were analysed for changes in viral quasispecies. Serum samples at baseline, and at months 3 and 6 of 3TC+ADV treatment could be clonally analysed in 7 of 10 patients; 3-82 clones per sample (total 1,068 clones, mean 63) were sequenced.

Results: 3TC+ADV therapy led to a modest decline in HBV DNA. Almost all clones had L180M and M204V 3TC resistance mutations before and during combination therapy. All clones had ≥1 of the S202G, T184F, T184A, T184L, T184I and M250V ETV resistance mutations. The percentages of detected clones bearing 3TC (rtL180M and rtM204V) and ETV mutations did not change with rescue 3TC+ADV therapy. In 7 of 8 patients with detectable HBV DNA (median 5.17 log(10) copies/ml) after a median 24 months of ADV therapy, HBV DNA became undetectable with 3TC plus tenofovir after 6 months of treatment.

Conclusions: In patients with ETV resistance tenofovir is effective. Clonal analysis data indicate no selection of specific HBV mutants during rescue 3TC+ADV.

Publication types

  • Clinical Trial, Phase III
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenine / analogs & derivatives*
  • Adenine / pharmacology
  • Adenine / therapeutic use
  • Adult
  • Antiviral Agents / pharmacology*
  • Antiviral Agents / therapeutic use
  • Drug Resistance, Viral / drug effects
  • Drug Resistance, Viral / genetics*
  • Drug Therapy, Combination
  • Female
  • Genome, Viral / drug effects
  • Genome, Viral / genetics
  • Guanine / analogs & derivatives*
  • Guanine / pharmacology
  • Guanine / therapeutic use
  • Hepatitis B virus / classification
  • Hepatitis B virus / drug effects*
  • Hepatitis B virus / genetics*
  • Hepatitis B, Chronic / drug therapy*
  • Hepatitis B, Chronic / virology
  • Humans
  • Lamivudine / therapeutic use
  • Male
  • Middle Aged
  • Mutation
  • Organophosphonates / pharmacology
  • Organophosphonates / therapeutic use*
  • Tenofovir
  • Treatment Outcome
  • Young Adult

Substances

  • Antiviral Agents
  • Organophosphonates
  • Lamivudine
  • entecavir
  • Guanine
  • adefovir
  • Tenofovir
  • Adenine