Population pharmacokinetics and exposure-response of albinterferon alfa-2b

J Clin Pharmacol. 2012 Apr;52(4):475-86. doi: 10.1177/0091270011399576. Epub 2011 May 6.

Abstract

Albinterferon alfa-2b (albIFN) has been studied for treatment of chronic hepatitis C virus (HCV). A population pharmacokinetics model was developed using nonlinear mixed-effects modeling. Efficacy/safety exposure-response relationships were assessed for subcutaneous albIFN doses (900-1800 µg once every 2 or 4 weeks) administered for either 24 weeks (HCV genotypes 2/3) or 48 weeks (genotype 1), plus daily oral ribavirin. Sustained virologic response (SVR) exposure-response was modeled using logistic regression. Adverse event incidence was tabulated versus exposure quartiles. First-order absorption rate constant (0.0148 h(-1)), apparent clearance (38.9 mL/h), and apparent volume of distribution (11.6 L) had interindividual variances (coefficient of variation) of 21%, 34%, and 24%, respectively. Residual variance estimates were 27% (coefficient of variation) and 1.51 ng/mL (standard deviation). For the only explanatory covariate-body weight-exposure decreased as weight increased. Important SVR predictors included baseline HCV RNA, fibrosis score, and black race (genotype 1); SVR was minimally related to exposure. Most adverse events had similar incidence rates across exposure quartiles. Some adverse events had a higher incidence in the upper exposure quartile without evidence of exposure-response across the lower quartiles. Given the lack of consistent efficacy/safety exposure-response relationships, further investigation is necessary to optimize albIFN dosing.

Publication types

  • Clinical Trial, Phase II
  • Clinical Trial, Phase III
  • Randomized Controlled Trial

MeSH terms

  • Adolescent
  • Adult
  • Aged
  • Albumins / administration & dosage*
  • Albumins / adverse effects
  • Albumins / pharmacokinetics
  • Antiviral Agents / administration & dosage*
  • Antiviral Agents / adverse effects
  • Antiviral Agents / pharmacokinetics
  • Dose-Response Relationship, Drug
  • Drug Therapy, Combination
  • Female
  • Genotype
  • Hepacivirus / genetics
  • Hepacivirus / isolation & purification
  • Hepatitis C, Chronic / drug therapy*
  • Hepatitis C, Chronic / virology
  • Humans
  • Injections, Subcutaneous
  • Interferon-alpha / administration & dosage*
  • Interferon-alpha / adverse effects
  • Interferon-alpha / pharmacokinetics
  • Logistic Models
  • Male
  • Middle Aged
  • Models, Biological*
  • Ribavirin / administration & dosage
  • Ribavirin / therapeutic use
  • Tissue Distribution
  • Young Adult

Substances

  • Albumins
  • Antiviral Agents
  • Interferon-alpha
  • Ribavirin
  • albinterferon alfa-2b