Phase 2 study of cobicistat versus ritonavir each with once-daily atazanavir and fixed-dose emtricitabine/tenofovir df in the initial treatment of HIV infection

AIDS. 2011 Sep 24;25(15):1881-6. doi: 10.1097/QAD.0b013e32834b4d48.

Abstract

Objective: To assess efficacy and safety of cobicistat versus ritonavir as pharmacoenhancers for atazanavir when administered with emtricitabine/tenofovir df as initial treatment for HIV-1 infection.

Design: Randomized, partially placebo-controlled, double-blind, multicenter study.

Participants: Antiretroviral treatment-naive adults, screening HIV-1 RNA of at least 5000 copies/ml and CD4 cell count more than 50 cells/μl.

Intervention: Randomized 2 : 1 (stratified by HIV RNA ≤ or >100,000 copies/ml) to receive placebo-blinded once-daily cobicistat 150 mg or ritonavir 100 mg with open-label atazanavir and fixed-dose emtricitabine/tenofovir df.

Main outcome measures: Efficacy and safety at weeks 24 and 48.

Results: Eighty-four percent of ATV/co participants and 86% of ATV/r participants suppressed HIV-1 RNA (<50 copies/ ml) at week 24, and 82 and 86% at week 48, respectively, and mean CD4 cell count increased 203 and 199 cells/μl at week 24 and 208 and 177 cells/μl at week 48, respectively. Study treatment discontinuation due to adverse events occurred in 4% ATV/co and in 3% ATV/r participants through 48 weeks. Treatment-related adverse events occurred in 36% ATV/co and 48% ATV/r participants; hyperbilirubinemia occurred in 96 and 100%, and ocular icterus or jaundice occurred in 14 and 17%, respectively. Mean estimated glomerular filtration rate (Cockcroft-Gault, ml/min) decrease occurred in both treatment groups and was evident at week 2 (ATV/co -9, ATV/r -4), reached a nadir by week 24 (-15, -14, respectively), and did not progress further through week 48 (-13, -14).

Conclusion: Using cobicistat and ritonavir as pharmacoenhancers for atazanavir and administered with emtricitabine/tenofovir df achieved comparable rates of virologic suppression and CD4 cell count increase with satisfactory safety profiles.

Publication types

  • Clinical Trial, Phase II
  • Multicenter Study
  • Randomized Controlled Trial

MeSH terms

  • Adenine / administration & dosage
  • Adenine / analogs & derivatives*
  • Antiretroviral Therapy, Highly Active*
  • Atazanavir Sulfate
  • CD4 Lymphocyte Count
  • Carbamates / administration & dosage*
  • Cobicistat
  • Deoxycytidine / administration & dosage
  • Deoxycytidine / analogs & derivatives*
  • Double-Blind Method
  • Drug Administration Schedule
  • Emtricitabine
  • Female
  • HIV Infections / drug therapy*
  • HIV-1*
  • Humans
  • Male
  • Oligopeptides / administration & dosage*
  • Organophosphonates / administration & dosage*
  • Pyridines / administration & dosage*
  • RNA, Viral
  • Ritonavir / administration & dosage*
  • Tenofovir
  • Thiazoles / administration & dosage*
  • Treatment Outcome

Substances

  • Carbamates
  • Oligopeptides
  • Organophosphonates
  • Pyridines
  • RNA, Viral
  • Thiazoles
  • Deoxycytidine
  • Atazanavir Sulfate
  • Tenofovir
  • Emtricitabine
  • Adenine
  • Cobicistat
  • Ritonavir