Short-term administration of the CCR5 antagonist vicriviroc to patients with HIV and HCV coinfection is safe and tolerable

J Acquir Immune Defic Syndr. 2010 Jan;53(1):78-85. doi: 10.1097/QAI.0b013e3181bb28dc.

Abstract

Objective: CCR5 antagonists block HIV cell entry through competitive binding to the CCR5 receptor present on the surface of CD4(+) cells. The CCR5 receptor is also present on CD8(+) cells involved in clearing hepatitis C virus (HCV). The goal of the present study was to examine the short-term safety of a CCR5 antagonist, vicriviroc, in patients with HIV/HCV coinfection.

Methods: A randomized, double-blind trial was conducted in 28 HIV/HCV-coinfected subjects with compensated liver disease and plasma HIV RNA below 400 copies/mL. All subjects were receiving a ritonavir-enhanced protease inhibitor regimen, to which vicriviroc (5, 10, or 15 mg/day) or placebo was added for 28 days. Clinical and laboratory evaluations were performed 21 days beyond the treatment period.

Results: Treatment with vicriviroc resulted in no clinically meaningful changes in HCV or HIV viral load or any immune parameters. Adverse events were equally distributed among placebo and vicriviroc groups. Transaminase elevations of grade 1 or more were reported as AEs in 1 subject receiving 10-mg vicriviroc and 1 placebo subject. Vicriviroc plasma concentrations were similar to those observed in healthy subjects.

Conclusions: Short-term treatment with vicriviroc as part of a ritonavir-containing protease inhibitor-based regimen was safe and well tolerated in HIV/HCV-coinfected subjects. HIV/HCV coinfection also did not affect vicriviroc pharmacokinetics.

Publication types

  • Multicenter Study
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Antigens, CD / metabolism
  • Antigens, CD19 / metabolism
  • Apyrase / metabolism
  • C-Reactive Protein / analysis
  • CCR5 Receptor Antagonists*
  • CD4 Antigens / metabolism
  • CD4 Lymphocyte Count
  • CD8 Antigens / metabolism
  • Double-Blind Method
  • Female
  • HIV Infections / complications
  • HIV Infections / drug therapy*
  • HIV-1 / drug effects
  • Hepacivirus / drug effects
  • Hepatitis C / complications
  • Hepatitis C / drug therapy*
  • Humans
  • Immunoglobulins / blood
  • Liver / drug effects*
  • Liver / metabolism
  • Liver / virology
  • Lymphocyte Subsets / drug effects*
  • Lymphocyte Subsets / metabolism
  • Male
  • Middle Aged
  • Piperazines / administration & dosage*
  • Piperazines / adverse effects
  • Piperazines / pharmacokinetics
  • Pyrimidines / administration & dosage*
  • Pyrimidines / adverse effects
  • Pyrimidines / pharmacokinetics
  • Viral Load
  • alpha-Fetoproteins / analysis

Substances

  • Antigens, CD
  • Antigens, CD19
  • CCR5 Receptor Antagonists
  • CD4 Antigens
  • CD8 Antigens
  • Immunoglobulins
  • Piperazines
  • Pyrimidines
  • alpha-Fetoproteins
  • C-Reactive Protein
  • Apyrase
  • CD39 antigen
  • vicriviroc