Abstract
This chapter focuses on the concepts relating to the discovery and the development of new drugs for cancer therapy. The purpose is to discuss the practices involved in the discovery and the development for clinical application of molecular-targeted therapeutics, new effective and safe anticancer agents that target critical cancer pathways. The concept of molecular-targeted therapeutic approach, which has now become the paradigm governing the present-day drug discovery process, and the related concepts of molecular targets, target identification and selection, as well as target validation in terms of the processes to explore the biological and therapeutic significance of the target are all discussed. The chapter also briefly outlines strategies that have resulted in some of the well-known new therapeutic agents that are currently approved or near approval for clinical use. In these cases, specific drug candidates are used to exemplify the translation from concepts to the finished products.
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