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New data shows better lipid safety profile of boosted saquinavir vs. boosted indinavir

SAN DIEGO, CA., Sept. 27 -- Roche announced results of two studies examining the lipid safety profile of twice-daily boosted saquinavir (1000 mg saquinavir with 100 mg ritonavir) for HIV.

Data from the first head-to-head study of boosted protease inhibitors (the MaxCmin1 trial) revealed that boosted saquinavir (Fortovase) led to significantly lower increases in fasting total cholesterol, LDL cholesterol and triglyceride levels than boosted indinavir (Crixivan) at 48 weeks, while a separate study found no significant rises in triglycerides or cholesterol after 20 days of treatment with boosted saquinavir alone.

The studies were presented at the 42nd Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC), and at the 4th International Workshop on Adverse Drug Reactions and Lipodystrophy in HIV, respectively.

"Given the long-term nature of antiretroviral treatment, evaluating the lipid safety profiles of protease inhibitor-based regimens provides valuable information to HIV-treating physicians," said Dr. Cal Cohen, Director of Research, Community Research Initiative of New England, Boston. "It is clear from these studies that boosting twice-daily saquinavir (1000 mg) with a mini-dose of ritonavir (100 mg) allows patients to avoid the negative lipid impact of higher doses of ritonavir while maintaining maximum therapeutic benefit with saquinavir."

Patients from 14 countries in North America, South America and Europe participated in the MaxCmin1 study. The primary objective of the study, which enrolled 317 patients, was to evaluate differences in virological failure between 1000 mg saquinavir (n=148) and 800 mg indinavir (n=158), each co-administered with a small 100 mg dose of ritonavir, at 48 weeks (Eleven patients who were randomized did not initiate therapy).

At baseline, no difference between the study arms were observed in demographic, clinical or laboratory variables, nor in the use of any antiretroviral drug prior to inclusions or at baseline.

A separate study found no significant rises in triglycerides or total cholesterol after 20 days of treatment with twice-daily boosted saquinavir in the absence of other antiretroviral agents. In this single-center, open-label, cross-over, pharmacokinetic study, 24 healthy male volunteers were randomized to receive 10 days of treatment with either 1000 mg of saquinavir soft gel capsules (Fortovase) or hard gel capsules (Invirase) with 100 mg ritonavir twice daily, and then switched to the alternate formulation of saquinavir. Fasting levels of triglycerides and cholesterol and other laboratory parameters were measured at screening and at days one, 10 and 20 of the trial, as well as during three to seven days of follow-up.

At twenty days, mean total cholesterol levels fell by 1.0 mg/dl and triglycerides rose by 1.2 mg/dl. None of these changes were considered statistically significant. There was no statistically significant change in any laboratory parameter and there were no Grade 3 or 4 laboratory toxicities during the trial. The incidence of diarrhea was significantly lower with boosted Invirase (four of 24) than with boosted Fortovase (15 of 24 subjects). There was no significant correlation between saquinavir drug levels and the incidence of either diarrhea or abdominal symptoms.

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Posted: September 2002