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Rho 相关激酶抑制剂:青光眼治疗的演进策略。

Rho-Associated Kinase Inhibitors: Evolving Strategies in Glaucoma Treatment.

机构信息

Kellogg Eye Center, University of Michigan, Ann Arbor, MI, USA.

Wilmer Eye Institute and Bloomberg School of Public Health, The Johns Hopkins University, Baltimore, MD, USA.

出版信息

Drugs. 2019 Jul;79(10):1031-1036. doi: 10.1007/s40265-019-01130-z.

DOI:10.1007/s40265-019-01130-z
PMID:31134520
Abstract

Glaucoma, a group of progressive optic neuropathies with similar patterns of tissue loss, is primarily treated with medical therapy, followed by laser therapy and, later, incisional surgery. Aside from the introduction of prostaglandin analogs, topical carbonic anhydrase inhibitors, and topical alpha-agonists in the 1990s, no new pharmaceutical agents to lower intraocular pressure (IOP) have been introduced for approximately 20 years. The Rho kinase inhibitors represent a new class of glaucoma medications that inhibit the downstream pathway of the Rho family of small G-proteins to increase outflow from the conventional (trabecular) outflow pathway in the eye. Several of these Rho kinase inhibitors, ripasudil and netarsudil, have recently reached the market and are used in clinical practice in several countries. A fixed-dose combination of latanoprost and netarsudil was also very recently approved (2019) by the US FDA. Several other novel agents are undergoing clinical trials. These drugs are poised to act as adjuncts to already established medical therapy for further lowering of IOP in the treatment of glaucoma.

摘要

青光眼是一组具有相似组织丧失模式的进行性视神经病变,主要采用药物治疗,其次是激光治疗,最后是手术治疗。除了在 20 世纪 90 年代引入前列腺素类似物、局部碳酸酐酶抑制剂和局部α激动剂之外,大约 20 年来,没有新的降眼压药物问世。Rho 激酶抑制剂代表了一类新的青光眼药物,它抑制 Rho 家族小分子 G 蛋白的下游途径,增加眼睛中传统(小梁)流出途径的流出。最近,这些 Rho 激酶抑制剂中的几种,如 ripasudil 和 netarsudil,已经上市,并在几个国家的临床实践中使用。拉坦前列素和 netarsudil 的固定剂量组合也于 2019 年最近获得美国 FDA 的批准。还有其他几种新型药物正在进行临床试验。这些药物有望作为已经确立的药物治疗的辅助手段,进一步降低青光眼的眼压。

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Am J Ophthalmol. 2018 Feb;186:116-127. doi: 10.1016/j.ajo.2017.11.019. Epub 2017 Dec 1.
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