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Glaucoma refers to a group of related eye disorders that have in common an optic neuropathy associated with visual function loss. It is one of the leading causes of irreversible blindness worldwide. Glaucoma can damage vision gradually so it may not be noticed until the disease is at an advanced stage.
Ripasudil (K-115) is a newly approved glaucoma treatment that is able to achieve potent IOP-lowering effects via its action as a selective Rho kinase inhibitor. K-115 is the first Rho-kinase inhibitor ophthalmic solution developed for the treatment of glaucoma and ocular hypertension in Japan 2014.
Rho-kinase (Rho-associated coiled-coil containing protein kinase; ROCK), a member of the serine-threonine protein kinases, is an effector protein of low molecular weight protein, Rho. Rho kinase binds with Rho to form a Rho/Rho-kinase complex, and regulates various physiological functions, such as smooth muscle contraction, chemotaxis, neural growth, and gene expression.
ROCK has two isoforms, ROCK-1 and ROCK-2, which are extensively distributed throughout in various tissues. Both ROCK-1 and ROCK-2 are also widely-expressed in ocular tissues including the ciliary muscles, trabecular meshwork, iris, and retina, among others. ROCK inhibitors have demonstrated efficacy in reducing intraocular pressure (IOP).
Most aqueous outflow occurs via the trabecular meshwork, with the remainder via the uveal scleral pathway. Current IOP lowering medications focus on increasing uveal scleral outflow or decreasing production, or combination of both. The only medication that influences trabecular outflow is pilocarpine, but due to negative side effects pilocarpine is not commonly prescribed.