This review surveys the enantiomer separation of drugs by electrokinetic chromatography (EKC). EKC is one option of capillary electrophoretic (CE) techniques, which permits the separation of electrically neutral drugs. In enantiomer separation by EKC, ionic pseudo-stationary phases such as chiral micelles and proteins, which can migrate with its electrophoretic mobility and can interact with the solutes, are employed as chiral selectors. Addition of electrically neutral chiral selectors such as cyclodextrins and precolumn conversion of solutes into diastereomers are also successful in EKC. A brief theory of separation and modes of EKC enantiomer separation are described with some typical applications.