numidargistat

Numidargistat (INCB001158, also known as CB-1158) is an orally bioavailable small-molecule inhibitor of both arginase isoforms (Arg1 and Arg2). It was developed to target the immunosuppressive tumor microenvironment by inhibiting arginase activity in myeloid cells, thereby restoring arginine levels and reversing T-cell suppression. This mechanism aims to enhance anti-tumor immune responses. Numidargistat has been evaluated as a monotherapy and in combination with immune checkpoint inhibitors such as pembrolizumab in patients with advanced or metastatic solid tumors including colorectal cancer, stomach or esophageal cancer, head and neck cancer, small cell lung cancer, kidney cancer, bladder cancer, mesothelioma, melanoma and non-small cell lung cancer. The drug was originally licensed by Calithera Biosciences to Incyte for clinical development.

Other names

numidargistatINCB001158INCB-001158INCB 001158CB-1158CB1158CB 1158