Clinical experience with saquinavir.

BACKGROUND

Saquinavir, a peptide-based, transition-state analogue of a characteristic HIV proteinase cleavage site, is a potent and highly specific inhibitor of HIV-1 and HIV-2 proteinases.

COMBINATION THERAPY

Combination therapy with saquinavir at 600 mg and zidovudine at 200 mg, both three times a day, has been shown to provide greater and more sustained increases in CD4 cell counts and decreases in HIV-1 RNA plasma levels than treatment with either agent alone in antiretroviral-naive patients with symptomatic HIV infection. In previously antiretroviral-treated patients, triple combination therapy with saquinavir at 600 mg, zidovudine at 200 mg and zalcitabine at 0.75 mg three times a day was associated with greater immunological and virological responses than either saquinavir+zidovudine or zidovudine+zalcitabine, as demonstrated by 48 weeks of follow-up data.

TOLERABILITY

Clinical experience to date has shown that saquinavir is well tolerated, even in patients with advanced disease, alone and in combination with zidovudine or zidovudine+zalcitabine.

ONGOING STUDIES

Phase III studies to support these data and determine the effects of saquinavir on clinical end-points are continuing.