Pharmacokinetics and metabolism in drug design

Abstract

An understanding of pharmacokinetics is necessary to ensure that drugs that are active in vitro will also be active in the human body. The optimization of the pharmacokinetic properties of lead compounds is therefore of central importance to drug development. In this new edition of a bestseller, all the contents have been updated and new material has been added, especially in the areas of toxicity testing and high throughput analysis. The authors, all of them employed at Pfizer in the discovery and development of new active substances, discuss the significant parameters and processes important for the absorption, distribution and retention of drug compounds in the body, plus the potential problems created by their transformation into toxic byproducts. They cover everything from the fundamental principles right up to the impact of pharmacokinetic parameters on the discovery of new drugs.