title: Ripasudil: first global approval.
abstract: Ripasudil hydrochloride hydrate (Glanatec® ophthalmic solution 0.4 %; hereafter referred to as ripasudil) is a small-molecule, Rho-associated kinase inhibitor developed by Kowa Company, Ltd. for the treatment of glaucoma and ocular hypertension. This compound, which was originally discovered by D. Western Therapeutics Institute, Inc., reduces intraocular pressure (IOP) by directly acting on the trabecular meshwork, thereby increasing conventional outflow through the Schlemm's canal. As a result of this mechanism of action, ripasudil may offer additive effects in the treatment of glaucoma and ocular hypertension when used in combination with agents such as prostaglandin analogues (which increase uveoscleral outflow) and β blockers (which reduce aqueous production). The eye drop product has been approved in Japan for the twice-daily treatment of glaucoma and ocular hypertension, when other therapeutic agents are not effective or cannot be administered. Phase II study is underway for the treatment of diabetic retinopathy. This article summarises the milestones in the development of ripasudil leading to the first approval for glaucoma and ocular hypertension.
authors.affiliation: Springer, Private Bag 65901, Mairangi Bay 0754, Auckland, New Zealand, dru@adis.com.
authors.forename: Karly P
authors.initials: KP
authors.lastname: Garnock-Jones
mesh_terms: D000959:Antihypertensive Agents / Q000493:pharmacokinetics / Q000627:therapeutic use; D017322:Clinical Trials, Phase II as Topic; D017277:Drug Approval; D005901:Glaucoma / Q000188:drug therapy* / Q000503:physiopathology; D006801:Humans; D007429:Intraocular Pressure / Q000187:drug effects*; D007546:Isoquinolines / Q000493:pharmacokinetics / Q000627:therapeutic use; D009883:Ophthalmic Solutions / Q000493:pharmacokinetics / Q000627:therapeutic use; D013449:Sulfonamides / Q000493:pharmacokinetics / Q000627:therapeutic use; D014129:Trabecular Meshwork / Q000187:drug effects; D016896:Treatment Outcome; D054460:rho-Associated Kinases / Q000037:antagonists & inhibitors*
chemical_list: D000959:Antihypertensive Agents; D007546:Isoquinolines; C584679:K-115; D009883:Ophthalmic Solutions; D013449:Sulfonamides; D054460:rho-Associated Kinases