Emergence of drug resistance-associated variants and changes in serum lipid profiles in sofosbuvir plus ledipasvir-treated chronic hepatitis C patients

J Med Virol. 2017 Nov;89(11):1963-1972. doi: 10.1002/jmv.24885. Epub 2017 Jul 25.

Abstract

Combination of sofosbuvir plus ledipasvir therapy has been expected to enhance sustained virological response (SVR) rates in hepatitis C virus (HCV) genotype 1 chronic infected patients. We analyzed the emergence of drug resistance-associated variants (RAVs) in treatment failure and changes in lipid profiles in sofosbuvir/ledipasvir-treated patients. A total of 176 patients with chronic HCV genotype 1 infection without decompensated liver cirrhosis were treated with sofosbuvir/ledipasvir for 12 weeks. NS5A and NS5B RAVs were determined by either Invader assay or direct sequencing. Serum lipid-related markers were measured at the start of treatment and at week 4 in patients who received sofosbuvir/ledipasvir and ombitasvir/paritaprevir/ritonavir therapies. SVR was achieved in 94.9% (167 out of 176) of patients. SVR12 rate was 97.1% for patietns with low frequncy (<25%) of baseline NS5A RAVs, but 82.8% for patients with high frequency (>75%) of NS5A RAVs. In multivariate regression analysis, higher albumin (odds ratio [OR] = 0.020 for presence; P = 0.007), and NS5A-L31/Y93 RAVs with a population frequency <75% (OR = 29.860 for presence; P = 0.023) were identified as significant independent predictors for SVR12. NS5A-Y93H substitutions were detected in all nine treatment failures at HCV relapse, and three out of six patients with NS5A inhibitor-naïve patients achieved additional NS5A RAVs. Serum low-density lipoprotein cholesterol and apolipoprotein B levels were significantly elevated at week 4 in sofosbuvir/ledipasvir-treated patients. These elevations were greater than in ombitasvir/paritaprevir/ritonavir-treated patients. In conclusion, NS5A multi-RAVs are likely to develop in patients who fail to respond to sofosbuvir/ledipasvir therapy. Inhibition of HCV replication with sofosbuvir might affect lipid metabolism.

Keywords: chronic hepatitis C; lipid profiles; resistance-associated variant; sofosbuvir plus ledipasvir.

MeSH terms

  • Adult
  • Aged
  • Aged, 80 and over
  • Anilides / therapeutic use
  • Antiviral Agents / therapeutic use*
  • Benzimidazoles / therapeutic use*
  • Carbamates / therapeutic use
  • Cyclopropanes
  • Drug Resistance, Multiple, Viral / genetics*
  • Drug Therapy, Combination
  • Female
  • Fluorenes / therapeutic use*
  • Genetic Variation
  • Hepacivirus / drug effects*
  • Hepacivirus / genetics
  • Hepatitis C, Chronic / drug therapy*
  • Hepatitis C, Chronic / virology
  • Humans
  • Lactams, Macrocyclic
  • Lipids / blood*
  • Macrocyclic Compounds / therapeutic use
  • Male
  • Middle Aged
  • Mutation
  • Proline / analogs & derivatives
  • Ritonavir / therapeutic use
  • Sofosbuvir
  • Sulfonamides
  • Sustained Virologic Response
  • Treatment Failure
  • Uridine Monophosphate / analogs & derivatives*
  • Uridine Monophosphate / therapeutic use
  • Valine
  • Young Adult

Substances

  • Anilides
  • Antiviral Agents
  • Benzimidazoles
  • Carbamates
  • Cyclopropanes
  • Fluorenes
  • Lactams, Macrocyclic
  • Lipids
  • Macrocyclic Compounds
  • Sulfonamides
  • ledipasvir, sofosbuvir drug combination
  • ombitasvir
  • Proline
  • Uridine Monophosphate
  • Valine
  • Ritonavir
  • paritaprevir
  • Sofosbuvir