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The use of mathematical modeling to characterize the disposition and effects of xenobiotics in humans Most people are exposed to countless foreign chemicals (xenobiotics) throughout their lifetimes. Some of these chemicals provide important therapeutic effects while others may lead to serious adverse health consequences. Traditional methods for the determination of the disposition and effects of these chemicals involve the acquisition of data through time- and resource-intensive studies involving large numbers of animals. Promisingly, advances in mathematical modeling are beginning to allow researchers to make important predictions in this area using only a limited set of experimental data. In this presentation, I will introduce a few relevant concepts in pharmacology and toxicology, present an overview of some of the mathematical modeling approaches in these fields, and showcase several studies we have conducted in which computational approaches have led to insights and quantitation of important endpoints related to chemical disposition and efficacy or toxicity.