LY3381916

LY3381916 is an orally available, highly selective, and potent small molecule inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1). It binds preferentially to the apo form of IDO1 (lacking heme), rather than the mature heme-bound enzyme. By inhibiting IDO1 activity and reducing kynurenine production in tumor cells, it restores and promotes proliferation and activation of immune cells such as dendritic cells, natural killer cells, and T lymphocytes. This leads to a reduction in tumor-associated regulatory T-cells and may induce a cytotoxic T-cell response against IDO1-expressing tumors. The drug has demonstrated brain penetration in preclinical models. Developed by Eli Lilly for use as monotherapy or in combination with anti-PD-L1 antibody therapy (LY3300054), it is being investigated primarily for advanced solid tumors including triple-negative breast cancer and non-small cell lung cancer[1][2][4][5][7].

Other names

N-[(1R)-1-[2,3-dihydro-1-[(tetrahydro-2H-pyran-4-yl)carbonyl]-1H-indol-5-yl]ethyl]-4-fluoro-benzamide2166616-75-5