ITC Recommendations for Transporter Kinetic Parameter Estimation and Translational Modeling of Transport-Mediated PK and DDIs in Humans

This white paper provides a critical analysis of methods for estimating transporter kinetics and recommendations on proper parameter calculation in various experimental systems. Rational interpretation of transporter‐knockout animal findings and application of static and dynamic physiologically based modeling approaches for prediction of human transporter‐mediated pharmacokinetics and drug–drug interactions (DDIs) are presented. The objective is to provide appropriate guidance for the use of in vitro, in vivo, and modeling tools in translational transporter science. Clinical Pharmacology & Therapeutics (2013); 94 1, 64–79. doi:10.1038/clpt.2013.45