Potential Role of Rho-Associated Protein Kinase Inhibitors for Glaucoma Treatment

Basilio      Colligris; Almudena      Crooke; Fernando      Huete; Jesus      Pintor

doi:10.2174/187221412800604554

Abstract

Rho kinase inhibitors are widely considered as a new treatment for glaucoma. Rho kinase inhibition has been shown in vitro and in vivo to lower intraocular pressure. Furthermore in the first clinical reports involving healthy human subjects, the results were quite promising. The potential of this new class of medicines is enormous in a field where there were not many developments lately. The inhibition of Rho kinase lowers the intraocular pressure by increasing the outflow through the trabecular meshwork. Increased blood flow to the optic nerve and a possible delay of optic nerve cell death has also been reported. As a consequence, the exploration of pharmacological inhibitors of Rho kinase signaling is actively being pursued by a number of pharmaceutical companies such as Senju Pharmaceuticals, Novartis, Kowa, Santen, Aerie, Inspire and others. In this article, we review the latest patents in this field, with their corresponding literature, regarding Rho kinase inhibitors for the treatment of intraocular pressure and summarize the many roles of Rho kinase signaling in the eye.

Keywords: Glaucoma, heteroaromatic compounds, inhibitors, intraocular pressure, Rho-kinase, trabecular meshwork, Rho-associated protein kinase inhibitors, anti-glaucoma drugs, ROCK inhibitors, Schlemm´s canal