IDO-IN-2

Details:

IDO-IN-2 is a potent IDO1 inhibitor(IC50=10 nM) with desirable pharmaceutical properties, which is poised to start clinical trials in cancer patients.
IC50 Value: 10 nM [1]
Target: IDO1
in vitro: In cellular assays,IDO-IN-2 selectively inhibits human IDO1 with IC(50) values of approximately 10nM, demonstrating little activity against other related enzymes such as IDO2 or tryptophan 2,3-dioxygenase (TDO) [1]. In coculture systems of human allogeneic lymphocytes with dendritic cells (DCs) or tumor cells,IDO-IN-2 inhibition of IDO1 promotes T and natural killer (NK)-cell growth, increases IFN-gamma production, and reduces conversion to regulatory T (T(reg))-like cells. IDO1 induction triggers DC apoptosis, whereas IDO-IN-2 reverses this and increases the number of CD86 (high) DCs, potentially representing a novel mechanism by which IDO1 inhibition activates T cells [1].
in vivo: Consistent with its effects in vitro, administration of IDO-IN-2 to tumor-bearing mice significantly inhibits tumor growth in a lymphocyte-dependent manner [1]. A single dose of IDO-IN-2 or IDO-IN-2 results in efficient and durable suppression of Ido1 activity in the plasma of treated mice and dogs, the former to levels seen in Ido1-deficient mice [2].
Clinical trial: A Phase 2 Study of the IDO Inhibitor IDO-IN-2 Versus Tamoxifen for Subjects With Biochemical-recurrent-only EOC, PPC or FTC Following Complete Remission With First-line Chemotherapy.