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Stem cells have a high self-renewal capability and can give rise to any cell in the body making them a very attractive target for researchers in regenerative medicine, as well as drug discovery and development. Preclinical screening of drug metabolism is a fundamental component of drug development and is used to aid in predicting drug bioavailability, drug–drug interactions, and toxicity. The main tissues responsible for drug metabolism are the liver, intestine, and kidney. Tissue specific cells generated from pluripotent stem cells for all three of these organs have vast potential to aid in drug metabolism screens. In this chapter we provide an overview of the current state of stem cell technologies regarding their use in drug metabolism screening, with an emphasis on stem cell derived hepatocytes.

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