Metabolomics: Bridging Chemistry and Biology in Drug Discovery and Development

Purpose of Review: Metabolism, as a ubiquitous biological process, plays a decisive role in the wellbeing of cells, organs, and whole body. Since the endpoint of pharmacological intervention is to either recover or sustain the wellbeing of targeted biological systems, examining metabolic events reveals useful information on diseases and drug treatment. Based on its omics nature and capacity to examine both drug and endogenous metabolism, metabolomics is an ideal systems biology tool to examine chemical and metabolic events in drug discovery and development. Recent Findings: Ongoing and potential applications of metabolomics in drug discovery and development include biomarker identification, bioactive compound identification, drug metabolism, metabolic profiling, and mechanistic investigation. Corresponding to four stages of drug discovery and development, why and how metabolomics is used in each stage of drug discovery and development are explained and discussed in four respective sections of this review. Summary: Since metabolites, the direct targets of metabolomic analysis, are the end products of gene-, protein-, microbe-, and signal molecule-mediated biological processes, metabolomics possesses many functions that are irreplaceable by other system biology tools. Even though its application is still in the germination phase, metabolomics is a promising platform to bridge chemistry and biology in drug discovery and development.