Department of Ophthalmology, Royal Melbourne Hospital, Melbourne, Victoria, Australia.
Centre for Eye Research Australia, Melbourne, Victoria, Australia.
Clin Exp Ophthalmol. 2023 Jul;51(5):472-483. doi: 10.1111/ceo.14224. Epub 2023 Apr 10.
Rho kinase (ROCK) inhibitors have emerged as a key therapeutic class of interest in ophthalmology over the last decade. Promising in vitro studies laid the foundations for the development of novel therapeutic agents that target the ROCK signalling pathway in ocular disease, with subsequent clinical trials supporting their use. Corneal endothelial disease, glaucoma, and vitreoretinal disease are the major pathologies in which ROCK inhibitors have been investigated to date. Ripasudil and netarsudil represent the current leaders in this pharmaceutical group, having been extensively validated and approved for use in glaucoma in some countries. Less substantial evidence exists for fasudil in ophthalmic use. ROCK inhibitors are also increasingly used in cultured endothelial cell grafting and as an adjunct to aid in endothelial cell migration and replication in Descemet's stripping procedures or Descemet's membrane injuries. This review has synthesised both established and emerging research to provide a practical guide to prescribing in this drug class. Drug efficacies, side effect profiles, and the demographic and clinical characteristics of appropriate drug candidates are discussed.
在过去的十年中，Rho 激酶（ROCK）抑制剂已成为眼科治疗的一个重要研究领域。有前途的体外研究为开发针对眼部疾病 ROCK 信号通路的新型治疗药物奠定了基础，随后的临床试验支持了这些药物的应用。角膜内皮疾病、青光眼和玻璃视网膜疾病是迄今为止 ROCK 抑制剂研究的主要病理学疾病。利匹司特和那他司特是该药物组的当前领导者，已在一些国家广泛验证并批准用于青光眼。法舒地尔在眼科应用中的证据则较少。ROCK 抑制剂也越来越多地用于培养的内皮细胞移植，并作为一种辅助手段，以帮助内皮细胞在撕囊或 Descemet 膜损伤过程中迁移和复制。本综述综合了已确立和新兴的研究成果，为该药物类别提供了实用的处方指南。讨论了药物的疗效、副作用概况以及合适药物候选物的人口统计学和临床特征。
