Safety and Efficacy in HIV‐1‐Infected Patients Treated with Ritonavir‐Boosted Saquinavir Mesylate

Objective.  To evaluate the safety, tolerability, and efficacy of ritonavir‐boosted saquinavir 1000/100 mg twice daily administered as a 500 mg film‐coated tablet in HIV‐1‐infected patients. Methods.  In this open‐label, observational, 24‐week survey conducted in 8 European countries, eligible HIV‐infected participants had been prescribed saquinavir/ritonavir in combination with other nonprotease inhibitor (PI) antiretroviral agents as part of their HIV treatment regimen. The safety (grade 3 or 4 adverse events [AEs]), tolerability (by an investigator‐reported subjective rating system), and efficacy (the percentage of participants with <50 and <400 copies/mL HIV RNA and change from baseline in mean CD4+ cell count) were analyzed for the overall study population and 7 subpopulations. Results.  The enrolled population included 2122 participants with 1908 completing the study; 44 (2.1%) withdrew prematurely because of AEs, including 7 nontreatment‐related deaths. There were 33 grade 3 or 4 AEs in 29 (1.4%) participants; 7 AEs in 7 (0.3%) participants were considered treatment‐related. Tolerability was reported to be “very good” or “good” in 42% and 25% of participants, respectively. From baseline to week 24, the proportion of participants with HIV RNA <50 copies/mL increased from 31.2% to 47.6% and the proportion with <400 copies/mL increased from 42.5% to 61.4%; the mean CD4+ cell count increased by 75 cells/µL. In the subpopulation analysis, the greatest efficacy benefits occurred in participants who were treatment‐naïve and in those not having received prior PI therapy. Conclusions.  Treatment with the saquinavir 500 mg film‐coated tablet resulted in few grade 3 or 4 AEs and was well tolerated and effective in a broad population of patients.