NLG919

Description: NLG919 analog (RG6078 analog; GDC-0919 analog; GDC0919 analog; IDO-IN-7; NLG-919 analog) is a novel, potent and orally bioavailable inhibitor of IDO (indoleamine-(2, 3)-dioxygenase) pathway with potential immunomodulating and antitumor activity. It inhibits IDO1 with Ki/EC50 of 7 nM/75 nM in cell-free assays. IDO1 catalyzes the conversion of tryptophan into kynurenine. By inhibiting IDO1 and decreasing kynurenine in tumor cells, NLG919 analog increases tryptophan levels, restores the proliferation and activation of immune cells (e.g. NK cells, T-lymphocytes), leading to a reduction in tumor-associated regulatory T-cells.

References: J Immunother Cancer. 2014 Jul 7; 2:21; AACR; Cancer Res 2013; 73(8 Suppl):Abstract nr 491.