Long-term efficacy and emergence of multidrug resistance in patients with lamivudine-refractory chronic hepatitis B treated by combination therapy with adefovir plus lamivudine

J Gastroenterol. 2014 Jun;49(6):1094-104. doi: 10.1007/s00535-013-0864-4. Epub 2013 Aug 9.

Abstract

Background: Few studies have investigated the emergence of multidrug resistance to adefovir dipivoxil (ADV) plus lamivudine (LAM) combination therapy for patients with LAM-refractory chronic hepatitis B (CHB). In this retrospective study, we investigated the long-term clinical course of these patients with or without multidrug resistance mutations.

Methods: We analyzed 406 Japanese patients with LAM-refractory CHB treated with combination therapy with follow-up for a median of 5.4 (0.5-9.5) years. Multidrug resistance of hepatitis B virus (HBV) DNA was analyzed using direct sequencing or cloning methods at baseline and viral breakthrough or insufficient decline during combination therapy.

Results: Ratio of patients with undetectable serum HBV DNA levels (<2.6 log copies/mL) during combination therapy was 63, 72, 75, 79, 82, 80 and 85 % at years 1 through 7, respectively. Substitutions associated with multidrug resistance were identified in 11 patients (2.7 %) at baseline, and in 12 patients (3 %) during therapy. HBV DNA levels of patients with rtA181S mutation at baseline and emergence of rtA181T + rtN236T double mutation or a wide variety of mutations during combination therapy could not be suppressed. Moreover, using ultra-deep sequencing, rtA181T/V mutations were detected at baseline in 7 of 10 patients with emergent multidrug resistance during combination therapy, although 6 of these 7 patients had very low frequency (<1 %) variants.

Conclusion: Long-term ADV plus LAM combination therapy is effective in LAM-refractory patients. However, HBV DNA levels of the patients with multidrug resistance at baseline or during combination therapy sometimes could not achieve complete suppression or were re-elevated after a decrease.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenine / administration & dosage
  • Adenine / analogs & derivatives*
  • Adenine / therapeutic use
  • Adult
  • Aged
  • Asian People
  • DNA, Viral / blood*
  • Drug Resistance, Multiple / genetics*
  • Drug Resistance, Viral / genetics*
  • Drug Therapy, Combination
  • Female
  • Follow-Up Studies
  • Hepatitis B virus / genetics*
  • Hepatitis B, Chronic / drug therapy*
  • Humans
  • Lamivudine / administration & dosage
  • Lamivudine / therapeutic use*
  • Male
  • Middle Aged
  • Mutation
  • Organophosphonates / administration & dosage
  • Organophosphonates / therapeutic use*
  • Reverse Transcriptase Inhibitors / administration & dosage
  • Reverse Transcriptase Inhibitors / therapeutic use*
  • Sequence Analysis, DNA
  • Treatment Outcome

Substances

  • DNA, Viral
  • Organophosphonates
  • Reverse Transcriptase Inhibitors
  • Lamivudine
  • adefovir
  • Adenine