Linrodostat mesylate

Linrodostat (BMS-986205) mesylate is a selective irreversible inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), which effectively inhibits IDO1-HEK293 mesylate cells with an IC50 value of 1.1 nM. Linrodostat mesylate demonstrates good pharmacological activity in advanced cancer[1].

IDO1: 1.1 nM (IC₅₀)

[1] Richards T, et al. Cell based functional assays for IDO1 inhibitor screening and characterization. Oncotarget. 2018 Jul 20;9(56):30814-30820. DOI:10.18632/oncotarget.25720
[2] Lillian L. Siu, et al. Abstract CT116: BMS-986205, an optimized indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor, is well tolerated with potent pharmacodynamic (PD) activity, alone and in combination with nivolumab (nivo) in advanced cancers in a phase 1/2a trial. AACR; Cancer Res. 2017; 77 (13 Suppl): Abstract nr CT116. DOI:10.18632/oncotarget.25720