title: Pharmacokinetics and short-term efficacy of a double-boosted protease inhibitor regimen in treatment-naive HIV-1-infected adults.
abstract: OBJECTIVE
  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.
authors.affiliation: HIV Netherlands Australia Thailand Research Collaboration, Thai Red Cross AIDS Research Center Bangkok, 104 Ratchadamri Road, Pathumwan, Bangkok 10330, Thailand. jasper.v@hivnat.org
authors.forename: Jasper
authors.initials: J
authors.lastname: van der Lugt
authors.forename: Reshma Saskia
authors.initials: RS
authors.lastname: Autar
authors.forename: Sasiwimol
authors.initials: S
authors.lastname: Ubolyam
authors.forename: Evian Fernandez
authors.initials: EF
authors.lastname: Garcia
authors.forename: Jongkol
authors.initials: J
authors.lastname: Sankote
authors.forename: Anchalee
authors.initials: A
authors.lastname: Avihingsanon
authors.forename: Anchalee
authors.initials: A
authors.lastname: Avihingson
authors.forename: Theshinee
authors.initials: T
authors.lastname: Chuenyam
authors.forename: David A
authors.initials: DA
authors.lastname: Cooper
authors.forename: Joep
authors.initials: J
authors.lastname: Lange
authors.forename: Praphan
authors.initials: P
authors.lastname: Phanuphak
authors.forename: Ferdinand
authors.initials: F
authors.lastname: Wit
authors.forename: Kiat
authors.initials: K
authors.lastname: Ruxrungtham
authors.forename: David
authors.initials: D
authors.lastname: Burger
mesh_terms: D000328:Adult; D019380:Anti-HIV Agents / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use*; D019540:Area Under Curve; D004305:Dose-Response Relationship, Drug; D005260:Female; D015658:HIV Infections / Q000188:drug therapy*; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D008297:Male; D011480:Protease Inhibitors / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use*
chemical_list: D019380:Anti-HIV Agents; D011480:Protease Inhibitors