Inoue Toshihiro, Tanihara Hidenobu
a Faculty of Life Sciences, Department of Ophthalmology , Kumamoto University , Kumamoto City , Japan.
Expert Opin Pharmacother. 2017 Oct;18(15):1669-1673. doi: 10.1080/14656566.2017.1378344. Epub 2017 Sep 14.
Among the intraocular pressure (IOP)-lowering drugs used in a clinical setting, Rho kinase (ROCK) inhibitors lower IOP by a unique mechanism, namely the depolymerization of intracellular actin in the conventional outflow tissues: the trabecular meshwork (TM) and Schlemm's canal (SC). Furthermore, ROCK inhibitors suppress the production of extracellular matrix by TM cells, which represents a potential alternative method of lowering IOP. Considering that conventional outflow is a dominant pathway in humans, IOP-lowering ROCK inhibitors, delivered in conjunction with other drugs, may be able to treat the glaucomatous eye. Areas covered: Ripasudil hydrochloride hydrate is the first ROCK inhibitor approved for clinical use in Japan (and worldwide) against glaucoma and ocular hypertension. The efficacy of ripasudil, as monotherapy and as an adjunctive medication to prostaglandin analogs and/or adrenergic β-receptor antagonists, has been confirmed in clinical trials. Expert opinion: Considering the unique ROCK-inhibiting mechanism by which ripasudil lowers IOP via its actions on TM and SC endothelial cells, it may be an ideal adjunctive medication for treating glaucoma in the clinic.
在临床使用的降低眼压（IOP）的药物中，Rho激酶（ROCK）抑制剂通过一种独特的机制降低眼压，即使传统房水流出组织（小梁网（TM）和施莱姆管（SC））中的细胞内肌动蛋白解聚。此外，ROCK抑制剂可抑制TM细胞产生细胞外基质，这是一种潜在的降低眼压的替代方法。鉴于传统房水流出途径在人类中占主导地位，与其他药物联合使用的降低眼压的ROCK抑制剂可能能够治疗青光眼。涵盖领域：盐酸水合瑞巴派特是首个在日本（及全球）被批准用于治疗青光眼和高眼压症的临床ROCK抑制剂。瑞巴派特作为单一疗法以及作为前列腺素类似物和/或肾上腺素能β受体拮抗剂的辅助药物的疗效已在临床试验中得到证实。专家意见：考虑到瑞巴派特通过对TM和SC内皮细胞的作用降低眼压的独特ROCK抑制机制，它可能是临床上治疗青光眼的理想辅助药物。
