Case study 3. Application of basic enzyme kinetics to metabolism studies: real-life examples.

ABSTRACT

An appreciation of the principles of enzyme kinetics can be applied in a number of drug metabolism applications. The concept for this chapter arose from a simple discussion on selecting appropriate time points to most efficiently assess metabolite profiles in a human Phase 1a clinical study (Subheading 4). By considering enzyme kinetics, a logical approach to the issue was derived. The dialog was an important learning opportunity for the participants in the discussion, and we have endeavored to capture this experience with other questions related to determination of K m and V max parameters, a consideration of the value of hepatocytes versus liver microsomes and enzyme inhibition parameters.