Maraviroc once-daily nucleoside analog-sparing regimen in treatment-naive patients: randomized, open-label pilot study

J Acquir Immune Defic Syndr. 2013 Feb 1;62(2):164-70. doi: 10.1097/QAI.0b013e31827b51b5.

Abstract

Objective: This study was performed to evaluate a once-daily dual-therapy regimen, maraviroc (MVC) + atazanavir/ritonavir (ATV/r), in treatment-naive patients.

Design: A phase 2b, randomized, open-label pilot study.

Methods: In Study A4001078 (NCT00827112), treatment-naive patients with CCR5-tropic HIV-1 (HIV-1 RNA ≥1000 copies/mL; CD4 cell count ≥100 cells/mm) were randomized to receive either MVC 150 mg once daily (n = 60) or tenofovir/emtricitabine (TDF/FTC) 300/200 mg once daily (n = 61) + ATV/r 300/100 mg once daily. Primary endpoint was proportion of patients with HIV-1 RNA <50 copies per milliliter at week 48.

Results: At week 48, 44 (74.6%) and 51 (83.6%) patients in the MVC and TDF/FTC treatment groups, respectively, had plasma HIV-1 RNA <50 copies per milliliter. Median change from baseline in CD4 cell count at week 48 was +173 and +187 cells per cubic millimeter with MVC and TDF/FTC, respectively. Seven patients discontinued from each arm; there were no deaths. The incidence of serious adverse events (AEs) was similar in each group; however, there were more grade 3/4 AEs in the MVC group (18 vs 11), mostly due to hyperbilirubinemia. Three patients in each arm were evaluable for virological analysis at discontinuation or failure (HIV-1 RNA >500 copies/mL); no genotypic resistance, change in tropism, or loss of susceptibility relevant to treatment was observed.

Conclusions: The virological activity and immunological benefit of once-daily MVC + ATV/r were confirmed. Indirect hyperbilirubinemia and associated signs were the most commonly reported AEs in both study treatment groups and were not associated with significant transaminase increases. No drug resistance occurred.

Publication types

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

MeSH terms

  • Adenine / analogs & derivatives
  • Adenine / therapeutic use
  • Adolescent
  • Adult
  • Aged
  • Anti-HIV Agents / therapeutic use
  • Atazanavir Sulfate
  • CCR5 Receptor Antagonists
  • CD4 Lymphocyte Count
  • Cyclohexanes / adverse effects
  • Cyclohexanes / pharmacokinetics
  • Cyclohexanes / therapeutic use*
  • Deoxycytidine / analogs & derivatives
  • Deoxycytidine / therapeutic use
  • Drug Therapy, Combination / adverse effects
  • Emtricitabine
  • Female
  • HIV Fusion Inhibitors / adverse effects
  • HIV Fusion Inhibitors / pharmacokinetics
  • HIV Fusion Inhibitors / therapeutic use*
  • HIV Infections / drug therapy*
  • HIV Infections / immunology
  • HIV-1*
  • Humans
  • Male
  • Maraviroc
  • Middle Aged
  • Oligopeptides / therapeutic use
  • Organophosphonates / therapeutic use
  • Pilot Projects
  • Pyridines / therapeutic use
  • RNA, Viral / blood*
  • Ritonavir / therapeutic use
  • Tenofovir
  • Triazoles / adverse effects
  • Triazoles / pharmacokinetics
  • Triazoles / therapeutic use*
  • Viral Load
  • Young Adult

Substances

  • Anti-HIV Agents
  • CCR5 Receptor Antagonists
  • Cyclohexanes
  • HIV Fusion Inhibitors
  • Oligopeptides
  • Organophosphonates
  • Pyridines
  • RNA, Viral
  • Triazoles
  • Deoxycytidine
  • Atazanavir Sulfate
  • Tenofovir
  • Emtricitabine
  • Adenine
  • Maraviroc
  • Ritonavir