Drug Metabolites: General Features and Most Applicable Analytical Methods of Studies

Abstract

Drug discovery and development is a multi and interdisciplinary process that includes chemistry and biology understanding. Though, drug discovery is an expensive and time-consuming process, promoting the lack of new drugs approval in recent years. In general, most of the drugs are established based on a macromolecular target, which is vital to disease progression. However, in many cases, the mechanism of drug-macromolecular target interaction is complex and not understood. All this missed information is strongly dependent on the physicalal-chemical stability and behavior of the molecule inside the cell, which is correlated to its metabolism resistance and entrance into the cell through the cellular membrane, respectively. Thus, bioanalysis often provides enough data about these molecular characteristics and helps to figure out new information about these subjects. In this context, the study of the metabolism of parental compound plays a key role in bioanalysis and, consequently in drug discovery. For a long time, the study of metabolism represented a huge challenge in medicinal chemistry, but with the technological advancements, many powerful techniques were developed and, currently, the metabolomics fields are essential steps in the process of discovering a new drug. Herein, we briefly discuss the biological aspects of the drug metabolism, focusing on the most used analytical tools to better understand the metabolite generation, and consequently, their chemical and biological characteristics.