(3R,4S)-1-(L-alanyl)-3-amino-4-(3-boronopropyl)pyrrolidine-3-carboxylic acid

CB-1158 (INCB-01158) is a potent, selective, oral available Arginase inhibitor with IC50 of 98 nM; reduces tumor growth, increases the number of tumor infiltrating CD8+ T-cells, and increases the level of Th1/NK/M1-associated chemokines, cytokines, and activation markers in the tumor microenvironment in combination with checkpoint inhibitors in mice bearing LLC tumors; a novel immuno-oncology agent targeting the immunosuppressive effects of tumor-infiltrating myeloid cells; high oral bioavailability.Solid TumorsPhase 2 Clinical