15012 – Brain-Penetrant IDO Inhibitors

Immuno-oncology is a groundbreaking new approach in cancer therapy that utilizes the body’s immune response to fight cancer. This approach has the potential to provide efficacy against a wide variety of cancers, and in monotherapy would provide this efficacy in the absence of the side effects typical of chemotherapeutic agents. Indoleamine 2,3-dioxygenase (IDO) catalyzes the transformation of the amino acid L-tryptophan into N-formylkynurenine, and is known to be upregulated in tumors. IDO is a validated and commercially exciting immune-oncology target, with a number of small molecule inhibitors in clinical trials today and with several major licensing deals occurring in 2015. However, few of these programs have delivered a compound that can cross the blood-brain barrier, which limits their utility in the central nervous system. We see a special opportunity for brain-penetrant IDO inhibitors being developed at UHN. These compounds, developed using in silico rational drug design techniques, are based on a new chemical series with potency against IDO shown enzymatically and in cell-based systems. Moreover, these compounds are highly brain penetrant (b/p ratios exceeding 1). As such they could be valuable leads for a candidate IDO inhibitor that is usable within brain. Christopher Barden christopher.barden@uhnresearch.ca 416-603-5800 x2975

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