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

Scand J Infect Dis. 2013 May;45(5):407-10. doi: 10.3109/00365548.2012.751507. Epub 2013 Mar 11.

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.

MeSH terms

  • Adult
  • Aged
  • Antiretroviral Therapy, Highly Active / adverse effects
  • Darunavir
  • Female
  • HIV Infections / blood*
  • HIV Infections / drug therapy*
  • HIV Infections / metabolism
  • HIV Protease Inhibitors / administration & dosage*
  • HIV Protease Inhibitors / adverse effects
  • HIV Protease Inhibitors / blood*
  • HIV Protease Inhibitors / pharmacokinetics
  • Humans
  • Male
  • Middle Aged
  • Retrospective Studies
  • Ritonavir / administration & dosage
  • Sulfonamides / administration & dosage*
  • Sulfonamides / adverse effects
  • Sulfonamides / blood*
  • Sulfonamides / pharmacokinetics
  • Viral Load

Substances

  • HIV Protease Inhibitors
  • Sulfonamides
  • Ritonavir
  • Darunavir