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 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.


RESULTS
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.
Phase III studies to support these data and determine the effects of saquinavir on clinical end-points are continuing.
Vella
S
S
Laboratory of Virology, Istituto Superiore di Sanità, Rome, Italy.
D000998:Antiviral Agents / Q000627:therapeutic use*; D002986:Clinical Trials as Topic; D004359:Drug Therapy, Combination; D015658:HIV Infections / Q000188:drug therapy*; D017320:HIV Protease Inhibitors / Q000627:therapeutic use*; D006801:Humans; D007546:Isoquinolines / Q000627:therapeutic use*; D011804:Quinolines / Q000627:therapeutic use*; D018894:Reverse Transcriptase Inhibitors / Q000627:therapeutic use; D019258:Saquinavir; D015215:Zidovudine / Q000627:therapeutic use
D000998:Antiviral Agents; D017320:HIV Protease Inhibitors; D007546:Isoquinolines; D011804:Quinolines; D018894:Reverse Transcriptase Inhibitors; D015215:Zidovudine; D019258:Saquinavir