. The objective of this proposal is to formulate a protease inhibitor, KNI-272, to improve bioavailability following oral administration. This will be accomplished using patented technology to convert this nearly water-insoluble drug into spherical, amorphous, uniformly-sized submicron particles suspended in a biocompatible aqueous medium. This technology has been used to produce formulations for anti-cancer and antimicrobial therapy with improved oral bioavailability. The proposed formulation of KNI-272 will be subjected to preliminary bioavailability evaluations in mice to demonstrate feasibility. Phase II objectives will focus on preclinical efficacy and toxicity studies following oral administration and explore possible benefits of intravenous administration. In Phase III, clinical trials will be carried out.
