NADPH oxidase 1 (NOX1) and NOX4 generate reactive oxygen species (ROS) that are critical in regulating a variety of cellular functions but also contribute to many diseases.GKT137831 is a dual inhibitor of both NOX1 and NOX4 with Ki values in the range of 100 to 150 nM in cell-free assays of ROS production.It shows only weak inhibitory activity against NOX2 or xanthine oxidase and does not block neutrophil oxidative burst, scavenge ROS, or have antioxidant activity.GKT137831 displays good oral bioavailability with high plasma concentrations in vivo and attenuates liver fibrosis in mice.It reduces hypoxia-induced pulmonary vascular cell proliferation, ameliorates dopaminergic neuronal death, and provides renoprotection in long-term diabetic nephropathy.

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