Ruboxistaurin – A Promising Drug for Diabetic Retinopathy

Abstract

Diabetic retinopathy is a common complication leading to visual disability. Laser photocoagulation and surgical procedures remains the mainstay of treatment in diabetic retinopathy. Presently there is no approved medical therapy available to delay the development or cure diabetic retinopathy. Ruboxistaurin, a Protein Kinase C-beta (PKC beta) inhibitor, is being developed as an effective treatment to prevent visual loss associated with diabetic retinopathy. Ruboxistaurin is an acyclic derivative of staurosporine belonging to a new class of N- (azacycloalkyl) bisindolylmaleimides. By inhibiting PKC beta, Ruboxistaurin prevents endothelial dysfunction in the retinal vessels in experimental models and displays antiangiogenic property by preventing intraocular neovascularization. In clinical trials, Ruboxistaurin showed no significant effects on the progression of diabetic retinopathy, but delayed the onset of visual loss, improved retinal circulation time and reduced the risk of visual loss. It has also been shown to be effective in patients with severe macular edema as it reduces the retinal leakage. In trials, the drug was well tolerated. Ruboxistaurin is under evaluation by FDA and once approved, would emerge as a promising therapeutic approach for treating diabetic retinopathy by preventing visual loss.