Saquinavir is the first proteinase inhibitor approved in combination w
ith nucleoside analogues for the treatment of advanced HIV infection i
n selected patients. Approval was based only on changes in surrogate m
arkers in patients receiving it in combination with zidovudine or zalc
itabine; no information is available about its use with other nucleosi
des or its effects on HIV disease progression or survival. It is a pot
ent inhibitor of HIV in vitro, is active against zidovudine-resistant
strains, and is effective in acutely and chronically infected cells. S
aquinavir is well tolerated and must be administered with food. Althou
gh more effective and potent proteinase inhibitors are available, saqu
inavir provides a unique addition to the current formulary of antiretr
oviral agents, and might have clinical benefits for selected HIV-posit
ive patients.