This symposium was held in Trento, Italy, from June 14 to 16, 2007, and was co chaired by William G. Kaelin, Enrico Mihich, and Charles L. Sawyers. A session was devoted to the proof of concept derived from successes in target-oriented therapeutics. Molecular targets must be identified in each patients because they are equally present in all patients with the same tumor type. A session was devoted to the identification of markers of drug effectiveness. Two sessions were focused on opportunities for developing new specific molecular target-oriented therapies.