OSI’s research takes place on campuses in Farmingdale, New York and Boulder, Colorado. Our preclinical research teams are comprised of experts in high-throughput screening and assay design, medicinal chemistry and structure-based design, biochemistry and enzymology, cell biology and signal transduction, DMPK (Drug Metabolism and Pharmacokinetics) and pharmacology. Research efforts are focused on developing single agent anti-cancer molecular targeted therapies (MTTs) and on developing rational multi-targeted combinations through mechanism-based approaches.

OSI’s Oncology research is focused on understanding the science of the Epithelial Mesenchymal Transition (EMT) in solid tumors in order to develop more effective and safe mechanism-based therapeutic agents. We are among the first to describe observations suggesting that EGFR TKI sensitivity may be determined by the EMT status of a tumor.

Our observations, and those of our collaborators, have shown that for one of our compounds, erlotinib, tumor cell sensitivity is governed at least in part by the expression of Epithelial-like cell markers E-cadherin and ErbB3, whereas loss of E-cadherin and acquisition of Mesenchymal-like cellular markers (such as vimentin and fibronectin) governs aspects of erlotinib resistance in solid tumors. These and related observations have been extended by others in the oncology community, and we believe that EMT will continue to have a major clinical impact on the efficacy of certain molecular targeted therapies. OSI believes that understanding the science of EMT will profoundly impact how MTTs will be combined in the clinic and will this lead to the successful development of rational combinations of MTTs in cancer.