Drug metabolism, pharmacokinetics and toxicokinetics as determinants of drug attrition and the safety of xenobiotics are critically important. This book presents a comprehensive treatise on the current issues and challenges facing drug metabolism and pharmacokinetics. Readers will find a thorough exploration of their predictive role in impacting drug discovery and development and in improving the success rate and safety assessment of pharmaceuticals and industrial or occupational chemicals. Chapters not only focus on the current state of art, with distinct examples, but on future needs and approaches likely to improve our prediction of potential human risk. Discussions of critical properties that are determinants of a compoundOs metabolic and pharmacokinetic fate follow introductory chapters. The Drug Discovery process increasingly incorporates pharmacokinetics and drug metabolism screening and focus has shifted towards in silico, computational and systems biology approaches. Core chapters reflect this and the recent interest and need to assess the role of transporters, along with drug metabolizing enzymes, as potential determinants of pharmacokinetic behaviour, toxicity and drug-drug interactions. Lastly, chapters cover the issues and factors involved in translating pharmacokinetics from in silico to in vivo and from animal models to man, and postulate future directions and opportunities.Leading experts from academia, industry and regulatory bodies across the globe contribute their knowledge to this book, which scientists involved in many aspects of the drug discovery process, as well as regulators and postgraduate students, will find a useful resource.