Long term persistence of NS5A inhibitor-resistant hepatitis C virus in patients who failed daclatasvir and asunaprevir therapy

J Med Virol. 2015 Nov;87(11):1913-20. doi: 10.1002/jmv.24255. Epub 2015 Jun 16.

Abstract

Although interferon-free antiviral treatment is expected to improve treatment of hepatitis C, it is unclear to what extent pre-existing drug-resistant amino acid substitutions influence response to therapy. The impact of pre-existing drug-resistant substitutions on virological response to daclatasvir and asunaprevir combination therapy was studied in genotype 1b hepatitis C virus (HCV)-infected patients. Thirty-one patients were treated with daclatasvir and asunaprevir for 24 weeks. Twenty-six patients achieved sustained virological response (SVR), three patients experienced viral breakthrough, and two patients relapsed. Direct sequencing analysis of HCV showed the existence of daclatasvir-resistant NS5A-L31M or -Y93H/F variants in nine out of 30 patients (30%) prior to treatment, while asunaprevir-resistant NS3-D168 mutations were not detected in any patient. All 21 patients with wild-type NS5A-L31 and -Y93 achieved SVR, whereas only four out of nine patients (44%) with L31M or Y93F/H substitutions achieved SVR (P = 0.001). Ultra-deep sequencing analysis showed that treatment failure was associated with the emergence of both NS5A-L31/Y93 and NS3-D168 variants. NS5A-L31/Y93 variants remained at high frequency through post-treatment weeks 103 through 170, while NS3-D168 variants were replaced by wild-type in all patients. In conclusion, pre-existence of NS5A inhibitor-resistant substitutions compromised the response to daclatasvir and asunaprevir combination therapy, and treatment failure was associated with the emergence of both NS5A-L31/Y93 and NS3-D168 variants. While asunaprevir-resistant variants that emerged during therapy returned to wild-type, daclatasvir-resistant variants tended to persist in the absence of the drug.

Keywords: antiviral resistance; asunaprevir; combination therapy; daclatasvir; deep sequencing.

Publication types

  • Clinical Trial, Phase II
  • Clinical Trial, Phase III

MeSH terms

  • Aged
  • Amino Acid Substitution
  • Antiviral Agents / therapeutic use*
  • Carbamates
  • Drug Resistance, Viral
  • Female
  • Genotype*
  • Hepacivirus / classification
  • Hepacivirus / isolation & purification*
  • Hepatitis C, Chronic / drug therapy*
  • Hepatitis C, Chronic / virology*
  • Humans
  • Imidazoles / therapeutic use*
  • Isoquinolines / therapeutic use*
  • Male
  • Middle Aged
  • Pyrrolidines
  • Sulfonamides / therapeutic use*
  • Treatment Failure
  • Valine / analogs & derivatives
  • Viral Nonstructural Proteins / genetics

Substances

  • Antiviral Agents
  • Carbamates
  • Imidazoles
  • Isoquinolines
  • Pyrrolidines
  • Sulfonamides
  • Viral Nonstructural Proteins
  • NS-5 protein, hepatitis C virus
  • Valine
  • daclatasvir
  • asunaprevir