ORAL FORMULATION OF KINASE INHIBITORS

摘要

The invention is directed to formulations of bioactive compounds of limited water solubility, inhibitors of focal adhesion kinase (FAK) of the 2,4-diaminopyridine class, adapted for oral administration to patients. The formulations are self-emulsifying in the gastrointestinal tract of the patients, providing enhanced absorption and bioavailability of the bioactive compounds as dispersions or emulsions in an oil base. For example, esters of PEG-ylated glycerol can be used as the oil, in conjunction with surfactants such as lecithin and TEPG succinate and solubilizers such as PEG 400 to provide useful oral formulations for administration to patients having a malcondition wherein inhibition of FAK is medically indicated, such as cancer or arthritis.