Drug design/development ADME studies

ADME studies provide information on absorption, distribution, metabolism, and excretion for the compound of interest in animals and humans. In drug development, these studies are performed with either C-14- or tritium-labeled material to provide detailed quantitative information on the circulating metabolites, the extent of metabolism and routes of excretion for drug and its metabolites. Readers are encouraged to refer Chapter 18 of this book for more detailed discussion on ADME study design and data presentation. 

Nonclinical ADME studies are used to link the animal pharmacology and toxicology studies to humans. Data obtained from the animal metabolism and excretory pathways of a drug may be useful to design a clinical mass balance study. Once in the development stage, ADME data in animals and humans with radiolabeled materials will reveal the major circulating metabolite(s) and... 

This chapter will review some of the important methods for carrying out in vivo absorption and bioavailability studies, as well as attempt to provide an overview of how the information may be used in the drug discovery process. The chapter is aimed at medicinal chemists and thus will focus on the use of animals in discovery phase absorption, distribution, metabolism, and excretion/pharmacokinetic (ADME/PK) studies, rather than the design of studies that are for regulatory submission, or part of a development safety package. 

---