Efficacy, safety and pharmacokinetics of once-daily saquinavir soft-gelatin capsule/ritonavir in antiretroviral-naive, HIV-infected patient

Julio S.G. Montaner, Malte Schutz, Robert Schwartz, Dushyantha T. Jayaweera, Alfred F. Burnside, Sharon Walmsley, Michael S. Saag

Research output: Contribution to journalArticle

23 Scopus citations

Abstract

Context: Once-daily HIV treatment regimens are being used in clinical practice with the objective of improving patient acceptance and adherence. Objective: To evaluate the efficacy and safety of saquinavir -soft-gelatin capsule (SGC)/ritonavir combination (1600 mg/100 mg) vs efavirenz (600 mg) both once daily and combined with 2 nucleoside analogs twice daily. Setting: Twenty-six centers in the United States, Canada, and Puerto Rico. Patients: A total of 171 antiretroviral naive HIV-infected individuals were enrolled in a 48-week, phase 3, open-label, randomized study. Main Outcome Measure: Proportion of patients with HIV-RNA levels < 50 copies/mL. The pharmacokinetic profile of saquinavir-SGC was analyzed in a subset of randomly selected patients. Results: In the primary intent-to-treat population at week 48, 51% (38/75) and 71% (55/77) of patients in the saquinavir SGC/ritonavir and efavirenz groups, respectively, achieved HIV-RNA suppression < 50 copies/ mL (P = .5392, 95% 1-confidence interval [Cl] = -33.5%). In the on-treatment (OT) population, 73% (38/52) and 93% (54/58) of patients in the saquinavir-SGC/ritonavir and efavirenz groups, respectively, had effective viral suppression < 50 copies/mL (P = .501 95% 1-sided Cl = -33.4%). Mean CD4+ cell counts increased by 239 and 204 cells/ microliters (mcL), in the saquinavir SGC/ritonavir and efavirenz groups, respectively, in the OT analysis (P = .058). Both regimens were reasonably well tolerated, although more gastrointestinal adverse events were reported with saquinavir-SGC/ritonavir. Pharmacokinet profiles in 6 patients showed an observed median Cmin at 24 hours of 429 ng/ mL (range, 68-1750 ng/mL). Conclusions: Once-daily efavirenz was statistically superior to once-daily saquinavir-SGC/ritonavir. Gastrointestinal adverse effects were commonly associated with treatment failure in the saquinavir-SGC/ ritonavir arm of the study.

Original languageEnglish (US)
Article number36
JournalMedGenMed Medscape General Medicine
Volume8
Issue number2
StatePublished - May 29 2006
Externally publishedYes

Keywords

  • Efavirenz
  • Efficacy
  • Once-daily
  • Pharmacokinetics
  • Saquinavir soft-gelatin capsule/ritonavir

ASJC Scopus subject areas

  • Medicine(all)

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