The proportion of drugs marketed as individual stereoisomers has rocketed over the last decade, a fact that reinforces the importance of the link between chirality and drug design and development. In this chapter, the reasons for this newfound focus in the marketing of chiral drugs will be discussed. First, in this chapter a brief overview of the fundamental principles of stereochemistry will be given. We will then focus on the underlying reasons why individual stereoisomers may have different pharmacological activities. The major challenges in bringing chiral drugs to market are in the production of single stereoisomers on a large scale and in finding methods to assess their purity. Therefore, the final sections of this chapter concentrate on these two important aspects.

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