Abstract: The invention provides an encapsulated unit dosage form for picoplatin that is adapted for oral administration of the picoplatin containing a substantially dry powder with about 20 to 55 wt % picoplatin in the physical form of a picoplatin particulate wherein an average picoplatin particle diameter is less than about 10 microns. The picoplatin particles are dispersed within the powder of the formulation which includes a substantially water-soluble, water-dispersible, or water-absorbing carbohydrate and an effective amount of up to about 5 wt % of a lubricant.

Abstract: The invention provides a method of treatment of cancer, wherein a individual doses of picoplatin, each of less than about 200 mg picoplatin content, the individual doses having high oral bioavailability, are administered to a patient in need thereof. The oral bioavailability can be greater than about 50%, or greater than about 75%, or greater than about 90%, depending upon the particular dosage form and dosing regimen used. The invention provides a quasi-metronomic dosing schedule including drug dosing intervals and drug intermission intervals, optionally including fasting periods prior to and following administration of each individual dose of picoplatin.