ruboxistaurin

Ruboxistaurin is an orally bioavailable small molecule and a selective, potent inhibitor of protein kinase C beta (PKCβ). It was developed primarily for the treatment of diabetic retinopathy and other microvascular complications of diabetes. By inhibiting PKCβ, ruboxistaurin limits the overactivation of this enzyme that is implicated in the pathogenesis of diabetic retinopathy and related vascular complications. Clinical studies have shown that ruboxistaurin can reduce vision loss in patients with moderate to severe non-proliferative diabetic retinopathy by decreasing PKCβ activity and ameliorating its pathological effects on retinal blood flow and neovascularization. The drug has also been investigated for other diabetic complications such as nephropathy, macular edema, peripheral neuropathy, and heart failure. Despite reaching phase 3 clinical trials for several indications including diabetic retinopathy and nephropathy, development was discontinued after failing to demonstrate sufficient efficacy for regulatory approval[3][4][5][6][8].

Brand names

Arxxant

Other names

ruboxistaurin mesylateRBX