Epacadostat (1204669-58-8) is a potent (IC50 = 10nM)1 and selective inhibitor of Indoleamine-2,3-dioxygenase 1 (IDO1) with no activity at IDO2 or TDO.2 It restored tryptophan levels and significantly impaired kynurenine generation in CT26 colon carcinoma (IC50 = 76 nM) and PAN02 pancreatic carcinoma (IC50 = 27 nM) cells. Epacadostat increases the number and activity of tumor-infiltrating lymphocytes as well as increasing the ration of effector T cells to regulatory T cells.1,2 Because of these immune system enhancing properties3, it is being investigated as a synergistic agent for use with other immune-oncology agents such as anti-PD-1 and anti-CTL4 antibodies.4,5,6
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