Humans are unavoidably exposed to a variety of environmental toxicants and combinations thereof, resulting in an increased risk for a number of diseases. The emerging field of toxicoproteomics has been boosted by quantitative and qualitative proteomic technologies and its increasing applications in toxicology research. The discipline is focused on the proteomic studies of toxicity, caused in response to toxic chemicals and environmental exposures, both in episodes of acute exposure to toxicants along with the long-term development of disease. Toxicoproteomics uses the discovery potential of proteomics in toxicology research by applying global protein measurement technologies to biofluids and tissues after host exposure to injurious agents. This field is challenging too, largely due to the shear size of the proteome and the massive data that are generated by it. Hence, improved toxicoproteomics studies applying advanced methodologies must be carried out to pave the way for commencing a new phase in toxicology research. In this regard, this study reviewed recent studies applying proteomic analysis to toxicological research, and the proteomic technologies and their capabilities with exemplary studies from biology and medicine. Expanding the repertoire of identified predictive biomarkers of toxicants exposure by toxicoproteomic studies will provide critical tools in the evaluation of their safety and design of appropriate measures to minimize adverse effects.