Pharmacokinetic and pharmacodynamic evaluation of telaprevir for the treatment of hepatitis C

Expert Opin Drug Metab Toxicol. 2015 Jul;11(7):1157-65. doi: 10.1517/17425255.2015.1049532. Epub 2015 May 25.

Abstract

Introduction: Telaprevir is one of the first direct-acting antiviral drugs approved for the treatment of the hepatitis C virus (HCV) genotype 1. Following its approval in 2011, new data regarding the pharmacokinetics and pharmacodynamics were reported, leading to important clinical applications.

Areas covered: This article reviews the pharmacokinetic and pharmacodynamic properties of telaprevir for the treatment of the HCV. The areas covered include data regarding the drug's absorption, distribution, metabolism and excretion, in addition to the antiviral activity strategy such as the clinical dose selection and treatment duration.

Expert opinion: Telaprevir presents several pharmacological properties that could limit its administration such a high-fat, high-calorie meal; the need to be administrated with pegylated IFN plus ribavirin; and the drug-drug interaction profile. As a consequence and considering the new therapeutic arsenal against the HCV, the use of telaprevir as part of HCV therapy will be limited.

Keywords: direct-acting agent; drug exposure; hepatitis C; pharmacodynamics; pharmacokinetics; telaprevir.

Publication types

  • Review

MeSH terms

  • Animals
  • Antiviral Agents / pharmacokinetics
  • Antiviral Agents / pharmacology
  • Antiviral Agents / therapeutic use*
  • Drug Interactions
  • Drug Therapy, Combination
  • Food-Drug Interactions
  • Genotype
  • Hepacivirus / drug effects
  • Hepacivirus / genetics
  • Hepatitis C / drug therapy*
  • Hepatitis C / virology
  • Humans
  • Oligopeptides / pharmacokinetics
  • Oligopeptides / pharmacology
  • Oligopeptides / therapeutic use*

Substances

  • Antiviral Agents
  • Oligopeptides
  • telaprevir