The emerging field of toxicoproteomics has been greatly advanced by quantitative proteomic technologies and their increasing applications in toxicology. The discipline is focused on the proteomic study of toxicity caused by toxic substances, including but not limited to drugs, toxins, environmental stressors, chemicals and any other materials that induce significant pathological responses. Drug safety is a major point of concern during the development phase and clinical application. Identification of toxicity biomarkers, potential drug targets and characterization of toxicity mechanisms represent major research areas for quantitative toxicoproteomics during drug development and evaluation. Further development and application of quantitative proteomic approaches would significantly facilitate the realization of personalized medicine.