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Accurate prediction of human drug safety continues to be a major challenge for drug development. In this chapter, the scientific concepts, current applications, and promising new advances in the application of human-based in vitro systems to the assessment of human adverse drug effects are reviewed. Emphasis is placed on two human-based experimental systems, namely, human hepatocytes and the novel technology Integrated Discrete Multiple Organ Co-Culture (IdMOC). Applications of these systems in the evaluation of two major adverse-drug effects: drug–drug interactions and drug toxicity, are reviewed.

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