In September 2005 an International Meeting on “Targeted Therapies in Cancer: Myth or Reality” was held in Milan. This successful Meeting was intended to represent a forum for scientists and clinicians working in cancer drug discovery and therapy to share their reflections and experiences on how the paradigm shift from empiricism to molecular targeted therapies is contributing to the translation of basic knowledge into new therapies for cancer patients. This book collects the contributions given by scientists and clinicians, from Academia and Industry, who participated to this Meeting. We hope that this book contributes to improve our approach to cancer drug discovery and, ultimately, to find new, more efficacious and better tolerated drugs for cancer patients. It provides an overview of diverse approaches ranging from drug discovery to cellular therapy. Although this change in paradigm has been useful, its entry into the clinical arena was associates with unforeseen problems including the emergence of resistance, unexpected side effects and failures. Time is therefore ripe for a critical cultural reflection on the state of the art, prospects and limitations. Ultimately, is targeted therapy in cancer a myth or a reality?