Metabolomics is the systematic study of small-molecular-weight substances in cells, tissues and/or whole organisms as influenced by multiple factors including genetics, diet, lifestyle and pharmaceutical interventions. These substances may directly or indirectly interact with molecular targets and thereby influence the risk and complications associated with various diseases, including cancer. Since the interaction between metabolites and specific targets is dynamic, knowledge regarding genetics, susceptibility factors, timing, and degree of exposure to an agent (drug or food component) is fundamental to understanding the metabolome and its potential use for predicting and preventing early phenotypic changes. The future of metabolomics rests with its ability to monitor subtle changes in the metabolome that occur prior to the detection of a gross phenotypic change reflecting disease. The integrated analysis of metabolomics and other 'omics' may provide more sensitive ways to detect changes related to disease and discover novel biomarkers. Knowledge regarding these multivariant characteristics is critical for establishing validated and predictive metabolomic models for cancer prevention. Understanding the metabolome will not only provide insights into the critical sites of regulation in health promotion, but will also assist in identifying intermediate or surrogate cancer biomarkers for establishing preemptive/preventative or therapeutic approaches for health. While unraveling the metabolome will not be simple, the societal implications are enormous.