Pharmaceutical giants have doubled their investments in drug development in the past decade only to see new drug approvals remain constant. This book investigates and highlights a set of proactive strategies aimed at generating sustainable competitive advantage based on value-generating business practices. We focus on three sources of pharmaceutical innovation: new management methods in the drug development pipeline, new technologies as enablers for cutting-edge R&D, and new forms of cooperation and internationalization, such as open innovation in the early phases of R&D. Our findings are illustrated by cases from Europe, the US, and Asia.