A phase I/II study of the safety and activity of a microsphere formulationof KNI-272 in patients with HIV-1 infection

Eighteen patients with symptomatic HIV disease were enrolled into a phase I /II study of a microsphere formulation of the HIV protease inhibitor KNI-27 2, with doses escalated up to a maximum dose of 60 mg/kg/day. One patient d eveloped reversible elevation in hepatic transaminase. The plasma half-life of the drug was very short, varying between 0.25 and 1.1 h. No consistent effect on plasma HIV RNA levels or CD4(+) lymphocyte counts was seen.