The worldwide scientific community is in agreement that the activities of metabolic enzymes greatly
impact the efficacies of anticancer drugs. Elucidation of the influences of these drugs on metabolism, especially
that occurring in the liver, appears to be an extremely important step in the development of new anticancer drugs.
Considering the continuous need to search for safe and effective chemotherapeutics, studies of the metabolism of
new potent drugs are very important and should be included in the modern, innovative drug development pipeline.
This article summarizes most of the current metabolic case studies involving anticancer drug development. Firstly,
the impacts of diverse metabolic enzymes, particularly cytochrome P450, and the utilities of a few model in vitro
enzymatic systems are described. Then, different analytical techniques, with particular emphasis on liquid chromatography-
mass spectrometry detection and structural elucidation, are discussed. Finally, some computer-aided strategies for decisionmaking
in the drug design process are described. Recent advances in drug development, including microdosing, in vitro-in vivo correlation
and pharmacologic audit trail, are also discussed in relation to metabolic studies.