Purpose of Review <p>In this review article, specific emphasis is on evolution of metabolomics in cancer research, metabolomics workflow, general understanding of liquid chromatography – mass spectrometry (LC-MS) based platform for quantitation of metabolites, their biological interpretation and the application in carcinogenesis and cancer prevention by dietary phytochemicals.</p> Recent&#xa0;Findings <p>Metabolomics is increasingly becoming a preferred approach for next generation metabolic screening and has profound impact on medical practice. Metabolomics describes the end products of biochemical processes which are greatly influenced by genetic and environmental factors. Metabolic alterations can be linked to potential biochemical reactions/enzymes and their corresponding genes. Thus, these results can be further validated via multi-omics approach including genomics, transcriptomics and proteomics. However, challenges exist within and between omic-domain data integration considering complex biochemical regulation including organism versus tissue versus cellular level processes, epigenetics, transcriptional and post translational modifications. Metabolomics can reflect the steady state or dynamic state of metabolism because metabolites are highly dynamic in space and time.</p> Summary <p>Metabolomic analysis of biological samples exhibit the possibility to determine mechanism of action of anti-cancer agents, biomarker discovery and impact of genetic alterations.</p>