Eighteen patients [in the UK?] with symptomatic HIV disease were enrolled into a phase I/II study of a microsphere formulation of the HIV protease inhibitor KNI-272, with doses escalated up to a maximum dose of 60 mg/kg/day. One patient (only) developed 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.
Journal of Antimicrobial Chemotherapy (2001) 47 (3), pp. 353-355.