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Setanaxib (formerly GKT137831) is a first-in-class, orally bioavailable small molecule inhibitor of NADPH oxidase (NOX) isoforms 1 and 4. Originally developed by Genkyotex and subsequently acquired by Calliditas Therapeutics (now a subsidiary of Asahi Kasei), setanaxib targets the enzymatic production of reactive oxygen species (ROS) that drive pathological inflammation and fibrotic tissue remodeling. The drug is currently being evaluated in several Phase 2 and Phase 3 clinical trials for conditions such as primary biliary cholangitis (PBC), Alport syndrome, idiopathic pulmonary fibrosis (IPF), and diabetic kidney disease. In addition to its anti-fibrotic properties, setanaxib is being investigated in oncology for its potential to inhibit cancer-associated fibroblasts (CAFs), thereby enhancing the efficacy of immunotherapies in solid tumors.
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