The present invention provides the use of Icaritin for the preparation of a composition for treating cancer, wherein the composition is orally administered to a patient at least one cycle, each cycle comprising a continuous 28-day dosing schedule, in which Icaritin is administered at least once daily, at a dosage of 400-1800 mg daily. The patients treated with Icaritin according to the present method receive better treatment, with reduced adverse effects.
