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This is an advanced textbook about drug design that fills the gap between existing texts in medicinal chemistry, pharmacology and biochemistry. The book fills the need for pharmacy and physiology instruction found in chemistry students seeking jobs in the pharmaceutical industry. It also illustrates scientific challenges in understanding the molecular basis of diseases, and shows technological solutions available to medicinal chemists when tackling diseases. The text is organized around stages of the drug design pipeline rather than a disease or molecular target. For each stage, the author explains key problems, discusses the general path toward solutions, presents key enabling technologies, and finishes with an example that highlights the merits and limitations of the approaches used. Worked-out case studies integrate individual concepts at the end of the book. The book is accompanied by a collection of electronic resources, including PowerPoint lecture slides, on-line tutorials, a test-bank with answers, templates for guiding student projects, and ready-to-use 3D molecular structures of the drugs discussed in the book.