Introduction

The objectives for the DMDG course on Pharmacokinetics in Drug Discovery are to develop an understanding and appreciation of the importance and contribution of drug metabolism and pharmacokinetics to drug design by first intent. The course highlights the importance of physicochemical properties in drug design and covers the fundamental aspects of pharmacokinetics and pharmacodynamics, safety study design and toxicokinetics, the importance of ADME and the relevance of metabolite pharmacokinetics.

Approaches to the prediction of human pharmacokinetics and therapeutic dose are introduced. Concepts associated with the assessment of pharmacokinetics in association with pharmacodynamic endpoints in First Time in Human and Proof of Mechanism and Concept clinical trials are also discussed.

The overarching theme is one of data integration and the utility of pharmacokinetic evaluation to assess and contextualise risk vs benefit at key stages of drug discovery and development. To illustrate the utility of DMPK science in the pharmaceutical industry in relation to compound progression the delegates also have the opportunity to conduct a series of workshops and integrate data from numerous sources to overcome real life problems and decisions in preclinical drug discovery and development.

The course takes the format of a series of lectures detailing theory and practice where the content is reinforced by the conduct of tutorials in small break out groups to create a forum for discussion and further learning. Students will be expected to play an active role in data calculation, interpretation and discussion.