Pharmacokinetics, efficacy, and safety of darunavir/ritonavir 800/100 mg once-daily in treatment-naïve and -experienced patients

HIV Clin Trials. 2008 Nov-Dec;9(6):418-27. doi: 10.1310/hct0906-418.

Abstract

Darunavir is a new protease inhibitor (PI) with in vitro activity against wild-type and PI-resistant HIV; it is used with the pharmacokinetic booster ritonavir. The currently approved dose of darunavir/ritonavir is 600/100 mg twice-daily, licensed for treatment-experienced patients. However, during the clinical development of darunavir, a range of once-daily and twice-daily doses of darunavir/ritonavir were evaluated. The relatively long terminal elimination plasma half-life of darunavir (15 hours) supports once-daily dosing. In treatment-naïve patients, the ARTEMIS trial has shown high rates of HIV RNA suppression for darunavir-ritonavir at the 800/100 mg once-daily dose (84% with HIV RNA <50 copies/mL at Week 48) versus a control arm of lopinavir/ritonavir (78% with HIV RNA <50 copies/mL). In a population pharmacokinetic substudy, darunavir 24-hour minimum plasma concentration levels remained above the predefined EC(50) of 55 ng/mL for all 335 patients evaluated in the ARTEMIS trial. Once-daily darunavir/ritonavir has also been evaluated in treatment-experienced patients in the TMC114-C207 proof-of-principle trial and the POWER 1 and 2 trials. For the overall POWER trial population, with significant baseline resistance to PIs, the rates of HIV RNA suppression <50 copies/mL at Week 24 for darunavir/ritonavir 800/100 mg once-daily [DOSAGE ERROR CORRECTED] were lower than for the 600/100 mg twice-daily dosage (31% vs. 47%, respectively). However, for patients with no genotypic darunavir resistance-associated mutations at baseline, rates of HIV RNA suppression were 62% and 67% for the 800/100 mg once-daily and 600/100 mg twice-daily doses. The current evidence from clinical trials of darunavir/ritonavir supports the efficacy of the 800/100 mg once-daily dose for treatment-naïve patients and further evaluation for treatment-experienced patients with no genotypic resistance to darunavir.

Publication types

  • Review

MeSH terms

  • Anti-HIV Agents* / administration & dosage
  • Anti-HIV Agents* / therapeutic use
  • CD4 Lymphocyte Count
  • Darunavir
  • Drug Therapy, Combination
  • HIV Infections / drug therapy*
  • HIV Infections / immunology
  • HIV Infections / virology
  • HIV Protease Inhibitors* / administration & dosage
  • HIV Protease Inhibitors* / adverse effects
  • HIV Protease Inhibitors* / pharmacokinetics
  • HIV Protease Inhibitors* / therapeutic use
  • HIV-1 / drug effects*
  • HIV-1 / genetics
  • HIV-1 / physiology
  • Humans
  • RNA, Viral / blood
  • Ritonavir* / administration & dosage
  • Ritonavir* / adverse effects
  • Ritonavir* / pharmacokinetics
  • Ritonavir* / therapeutic use
  • Sulfonamides* / administration & dosage
  • Sulfonamides* / adverse effects
  • Sulfonamides* / pharmacokinetics
  • Sulfonamides* / therapeutic use
  • Treatment Outcome
  • Viral Load

Substances

  • Anti-HIV Agents
  • HIV Protease Inhibitors
  • RNA, Viral
  • Sulfonamides
  • Ritonavir
  • Darunavir