During the last decade the use of ω‐transaminases has been identified as a very powerful method for the preparation of optically pure amines from the corresponding ketones. Their immense potential for the preparation of chiral amines, together with their ease of use in combination with existing biocatalytic methods, have made these biocatalysts a competitor to any chemical methodology for (asymmetric) amination. An increasing number of examples, especially from industry, shows that this biocatalytic technology outmaneuvers existing chemical processes by its simple and flexible nature. In the last few years numerous publications and patents on synthetic routes, mainly to pharmaceuticals, involving ω‐transaminases have been published. The review gives an overview of the application of ω‐transaminases in organic synthesis with a focus on active pharmaceutical ingredients (APIs) and the developments during the last few years. ω‐Transaminase‐catalyzed preparation of chiral amines has emerged as one of the most successful fields in biocatalysis over the past ten years. This review covers the development of the catalytic systems and points out the most important applications, especially with regard to industrial and commercial use of the technology.