Toxicology is the science that deals with the adverse effects of chemical and physical agents on living organisms and biological systems. The University of Saskatchewan first formally recognized the need for developing expertise in this area in 1975, when a coordinator of toxicology research on campus was appointed with the specific mandate to foster toxicology research, and to work towards the establishment of a Toxicology Centre. In 1978, the College of Graduate Studies and Research approved the terms of reference for the establishment of the Toxicology Group, whose members are comprised of scientists with academic or research interests in toxicology at the University, or any of the Federal or Provincial agencies on campus. The widespread expertise of the Toxicology Group provided the foundation for the development of an interdisciplinary graduate program in toxicology, the first of its kind in Canada, which the University approved in 1980. Further support for toxicology was achieved in 1982, when the Government of Saskatchewan and the University of Saskatchewan entered into an agreement to establish a Toxicology Research Centre, with Dr. Bruno Schiefer appointed as Director. The Centre was located on campus in a modern facility, created in 1986 with the assistance of a $2 million contribution from the Federal Government.

In 1996, the Toxicology Research Centre, the Toxicology Group, and the Toxicology Graduate Program were amalgamated into a single functional unit, the Toxicology Centre, with the goal of providing long-term stability and a focus for toxicology activities on campus. This year also marked the appointment of Dr. Karsten Liber as the Centre's Director, succeeding Dr. Schiefer after his many years of dedicated work. Dr. Liber's expertise in environmental toxicology expanded the Centre's existing capabilities in traditional clinical toxicology research and teaching.

Construction began in 2006 on an $11.8-million expansion to the Toxicology Centre, giving it unique capabilities that now make it the foremost university-based Centre in the country for water pollution research. A new 650 m2 Aquatic Toxicology Research Facility (ATRF) allows USask to pursue its goal of becoming a national and international leader in aquatic toxicology research and training. Accompanying research facilities consist of analytical chemistry, biochemistry, and molecular biology laboratories. Renovation of existing facilities also provided critically needed office and student space.

Laboratories at the Toxicology Centre are equipped with a diverse array of modern infrastructure used in toxicological research. Analytical chemistry labs can quantify virtually any inorganic or organic analyte using GC/MS, LC/MS/MS, ion chromatography, atomic absorption spectrometry, spectrophotometry, or spectrofluorometry. A full molecular biology suite includes RT-PCR and RNASeq for transcriptomics and Orbitrap LC/MS/MS for proteomics. Other lab facilities include a cell culture suite, light and fluorescence microscopes, and metabolic chambers. Field research in aquatic and terrestrial ecotoxicology is enabled through several research vessels, trucks, boat/backpack electrofishers, a mobile laboratory, and a variety of other sampling equipment.

The Toxicology Centre has always been closely associated with the adjacent Western College of Veterinary Medicine (WCVM), as well as other academic units on campus such as the College of Arts and Science, College of Agriculture and Bioresources, College of Pharmacy and Nutrition, School of Environment and Sustainability, and Global Institute for Water Security. Collaborations with WCVM faculty, several of which are core faculty at the Toxicology Centre, allow access to small and large mammalian species, which enables more traditional, biomedical toxicology research.