Pharmacokinetics and short-term efficacy of a double-boosted protease inhibitor regimen in treatment-naive HIV-1-infected adults

Jasper van der Lugt, Reshma Saskia Autar, Sasiwimol Ubolyam, Evian Fernandez Garcia, Jongkol Sankote, Anchalee Avihingson, Theshinee Chuenyam, David A. Cooper, Joep Lange, Praphan Phanuphak, Ferdinand Wit, Kiat Ruxrungtham, David Burger, Anchalee Avihingsanon

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Objectives: To study the pharmacokinetics and short-term efficacy of low and standard dose lopinavir/ritonavir and saquinavir combinations in Thai, human immunodeficiency virus (HIV)-infected, treatment-naive patients. Methods: In this open-label, 24-week, prospective study, 48 treatment-naive patients were randomized to lopinavir/ritonavir 400/100 mg + saquinavir 1000 mg twice daily (arm A), lopinavir/ritonavir 400/100 mg + saquinavir 600 mg twice daily (arm B), lopinavir/ritonavir 266/66 mg + saquinavir 1000 mg twice daily (arm C), or lopinavir/ritonavir 266/ 66 mg + saquinavir 600 mg twice daily (arm D). A 12 h. pharmacokinetic profile in all patients was performed. Plasma concentrations of saquinavir and lopinavir were determined using an HPLC technique. HIV-1 RNA was measured over 24 weeks. Results: Forty-three subjects were included in the pharmacokinetic analysis. The total exposure differed significantly for the different arms. Median values for lopinavir area under the curve at 0-12 h were 128.2, 119.2, 66.1 and 68.5 mg·h/L for arms A - D, respectively. For saquinavir, the median values were 36.9, 19.2, 25.3 and 12.4 mg·h/L for arms A - D, respectively. The proportion of patients having a viral load below 50 copies/mL at week 24 was 39% for arm A, 63% for arm B, 55.0% for arm C, and 69% for arm D. Conclusions: The pharmacokinetic parameters for the different treatment arms were adequate. However, the proportion of subjects with an undectable viral load at week 24 was lower than anticipated.

Original languageEnglish
Pages (from-to)1145-1153
Number of pages9
JournalJournal of antimicrobial chemotherapy
Issue number5
Publication statusPublished - 1 May 2008


  • Dose reduction
  • Efficacy
  • Lopinavir
  • Saquinavir
  • Viral dynamics

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