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Scientific and technological advances of the last 10 years have led to new approaches to the discovery of genetic drug susceptibility loci, the development of high\u2010tech analytical strategies for drug susceptibility profiling, and a flood of new gene discoveries in the area of receptors and receptor polymorphisms. Extension and refinement of our knowledge of human genetic diversity is essential to the use of drugs in more of an individualized manner and to the discovery of better therapies, but knowledge of the functional consequences of this diversity, the next great challenge in pharmacogenetics, provides the best chance to profit from this diversity. Environ. Mol. 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