GKT771

GKT771 is a novel small molecule inhibitor that selectively targets NADPH oxidase 1 (NOX1). The compound was developed by Genkyotex (now Calliditas Therapeutics France). In preclinical studies, GKT771 demonstrated antitumor activity by inhibiting tumor angiogenesis and lymphangiogenesis while enhancing the recruitment of immune cells, including proinflammatory macrophages and natural killer T lymphocytes, to the tumor microenvironment[1]. The compound's antitumor activity requires an intact immune system and has shown synergistic effects when combined with checkpoint inhibitors like anti-PD1 antibodies[1]. GKT771 works by blocking the production of reactive oxygen species catalyzed by NOX1, which is highly expressed in colon cancer and promotes tumor growth[1].