Abstract
Background: The prediction of human pharmacokinetics from data generated in relevant in vitro screens, and/or from pharmacokinetics determined in preclinical species, is of rapidly increasing interest throughout drug discovery, development and beyond. Objective: To provide a brief overview of the methods available for pharmacokinetic prediction and describe some of the advantages to be obtained from its application. Methods: Because of the relative degree of realism in the models, and the corresponding richness of the data available for model development, the technique of physiologically based pharmacokinetic (PBPK) modelling offers the best means of performing clinically relevant pharmacokinetic prediction. A small number of selected examples from the literature that illustrate significant applications of PBPK modelling are described. Results/conclusion: The development of reliable clinical pharmacokinetic prediction is critically dependent on, and will follow on from, further improvements in the quantitative determination of relevant processes at the biomolecular level. When combined with efficacy and toxicity data to predict in vivo pharmacological and toxic responses, the PBPK model will prove to be an indispensable tool in drug discovery and development.