Efficacy, safety, and pharmacokinetics of once-daily boosted darunavir in pretreated HIV-infected patients

Abstract

Objective and methods: The efficacy and safety of switching to a combined regimen containing darunavir/ritonavir (DRV/r) was investigated in a retrospective study. Results: Sixty-six experienced patients receiving once-daily DRV/r (900/100 mg) in various regimens were included (median age 51 y; male 82%; Centers for Disease Control and Prevention (CDC) stages B or C 70%). The number of patients with plasma HIV RNA < 50 copies/ml increased from 71% (45/63) at baseline (before switch) to 84% (52/62) at visit 1 (weeks 3–11), and to 92% (60/65) at visit 2 (weeks 12–24). CD4 cells increased from 498 ± 201 cells/mm³ at baseline to 567 ± 232 cells/mm³ by visit 2. Good digestive and metabolic tolerance was observed. The median steady-state DRV plasma concentration, measured 24 ± 4 h after the last drug intake, was 1427 ng/ml. All DRV plasma concentrations were above the protein-binding corrected median effective concentration (EC₅₀) for the wild-type virus (55 ng/ml). Conclusions: Once-daily DRV/r (900/100 mg) was efficacious in pretreated patients, with safe responses.

Keywords::

• HIV infection
• highly active antiretroviral treatment
• treatment switch
• boosted darunavir

Acknowledgements

The authors would like to thank Dr F. Sordet, Janssen Laboratories for helpful contributions to our discussions and Newmed Publishing Services for technical editing of the final manuscript without charge.

Declaration of interest:

Neither the study nor its follow-up and analysis were funded. All follow- up and analysis was conducted by the Institut de Médecine et d’Epidémiologie Appliquée in Paris.