This book includes general principles of drug targeting, targeting in the cardiovascular system, tumor targeting, brain targeting, miscellaneous targeting and novel approaches for targeting (new horizons). It is designed in a course-like fashion: from more general and simple to more specific and complex material. This framework will help even unfamiliar readers to learn new topics and navigate in the text. Although the book is aimed primarily at industrial and academic pharmacologists and drug discovery researchers, its design will make the book useful for advanced level graduate students. The book focuses on ligand-mediated drug targeting strategies, with additional chapters on general aspects of drug delivery that are of paramount importance in drug targeting (biological barriers, stealth technologies). Included are topics on targeting of genetic materials important in the biomedical context of the ligand-mediated targeting.