Vital to academic researchers, the medical field, and especially to biotech and pharmaceutical scientists, metabolomics is a rapidly expanding field that will provide a key link between functional biology (phenotypes) and the inner workings of cells in tissues or whole organisms. In , expert researchers provide readers with the current state of metabolomic development and the integration of metabolomics with transcriptomics and proteomics, illustrated by research efforts related to toxicology and pharmacology. The detailed contributions deal with topics ranging from sample preparation and considerations, both laboratory and clinical, analytical methodologies for metabolite and isotopomer profiling, metabolic flux modeling, database construction, and the integration of ‘omics for systems biochemical understanding, amongst other topics. Thorough and authoritative, serves as an ideal reference for all those who wish to further pursue this promising area of study.