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Clinical Trial
. 2006 May 10;8(2):36.
doi: 10.1186/1758-2652-8-2-36.

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

Julio S G Montaner  1 , Malte Schutz, Robert Schwartz, Dushyantha T Jayaweera, Alfred F Burnside, Sharon Walmsley, Michael S Saag
Affiliations
Clinical Trial

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

Julio S G Montaner et al. MedGenMed. .

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-sided confidence interval [CI] = -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 = .5015, 95% 1-sided CI = -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. Pharmacokinetic 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.

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Figures

Figure 1
Figure 1
Study design and completion status. ITT=intent to treat
Figure 2
Figure 2
Percentage of patients treated with either saquinavir-soft gelatin capsule/ritonavir or efavirenz both once-daily in combination with 2 nucleoside reverse transcriptase inhibitors, with undetectable HIV-RNA levels (< 50 copies/mL), as detected by the Ultra-Sensitive assay. ITT=intent to treat; OT=on treatment
Figure 3
Figure 3
Mean levels of triglycerides and total cholesterol in the safety population of patients treated with either saquinavir-soft gelatin capsule/ritonavir or efavirenz both once daily in combination with 2 nucleoside reverse transcriptase inhibitors.
Figure 4
Figure 4
Intensive pharmacokinetic profile of 6 patients at week 4. EC50 = concentration for 50% maximal effect
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