Role of ADME/PK in Drug Discovery, Safety Assessment, and Clinical Development

The term ADME/PK (Absorption, Distribution, Metabolism, Excretion and Pharmacokinetics) refers to the complete set of properties of a drug molecule describing its entry into the body, residence time within the body, distribution to organs, metabolic transformations involved in its clearance, and routes of elimination of drug-related materials from the body. These phenomena are as important as pharmacological effect and potency in designing a "drug-like" molecule. Therefore, medicinal chemists go through a process of optimization to arrive at a compound with the best overall balance of these properties suitable for clinical development. This chapter describes the detailed meaning of these properties, their fundamental importance to clinical utility, and how the medicinal chemist can follow a rational pathway to optimize them.