Disclosed is a method for predicting the optimal amounts of radiopharmaceutical and/or chemotherapy agents to administer to a patient, by determining the level of saturation of the therapeutic agents in the patients cells. The method comprises measuring cellular incorporation of the candidate therapeutic agents in a target cell population on a cell-by-cell basis. The method is able to identify an optimal cocktail of therapeutic agents for treatment of a disease. A method of high-throughput drug discovery incorporating this method, and a 2-stage targeting method of treating a disease using this method are also disclosed.