This graduate elective course presents principles and applications of contemporary empirical and mechanism-based mathematical modeling approaches to characterize the pharmacokinetic properties of small and macromolecule drugs within the context of drug discovery and development. Case studies will be used to demonstrate how to identify, interpret, and in some cases predict drug- and system-specific properties that control the time-course and extent of drug exposure in relevant biological fluids (e.g., plasma) and sites of action.