Most pharmaceutically active compounds possess a chirality that greatly influences their pharmacological properties. Since all pharmaceutical products nowadays are produced in chirally pure form, this places huge demands on the technology used for drug synthesis, purification, analysis and testing. Here, the two editors from academia and a major pharmaceutical company have assembled an experienced, international team to provide first-hand practical advice and report previously unpublished data. Divided into the three main sections of synthesis, analysis and drug development, this handbook covers all stages of the drug development process, including large-scale synthesis and purification of chirally pure pharmaceuticals. In the first section, the isolation of chiral drugs from natural sources, their production in enzymatic processes and the resolution of racemic mixtures in preparative chromatography are outlined in separate chapters. For the section on qualitative and quantitative analysis, enantioselective chromatographic methods are presented as well as optical methods and CE-MS, while the final section deals with the pharmacology, pharmacokinetics and metabolic aspects of chiral drugs, devoting whole chapters to stereoselective drug binding and modeling chiral drug-receptor interactions. With its unique industry-relevant aspects, this is a must for medicinal and pharmaceutical chemists.