Interrelationship between Pharmacokinetics and Metabolism

Abstract

In drug development, approximately 40% of all new chemical entities (NCEs) fail to become clinically successful drugs due to undesirable pharmacokinetic properties. A knowledge of the capacity for the metabolism of an NCE and an understanding of the human metabolism pathways and the enzymes involved have now become key components in the selection of compounds for clinical development. This article examines the relationship between metabolism and the resulting pharmacokinetic profile of a drug, and reviews the major factors that may have an impact on a drug's metabolism and may have a detrimental effect on its pharmacokinetics and clinical use.