Tan Jit Kai, Steel David H, Ahmad Sajjad, Viswanathan Ananth, Mathew Rashmi G, Khaw Peng Tee, Henein Christin
King's College London, London, UK; UCL Institute of Ophthalmology, London, UK.
Sunderland Eye Infirmary, Sunderland, UK; Biosciences Institute, Newcastle University, Newcastle Upon Tyne, UK.
Surv Ophthalmol. 2025 Apr 16. doi: 10.1016/j.survophthal.2025.03.008.
The therapeutic potential of rho kinase (ROCK) inhibitors in ophthalmology is gaining attention, given their multifaceted role in cellular regulation, particularly within ocular pathologies. This review synthesizes findings from clinical and preclinical studies on the efficacy and safety of ROCK inhibitors across glaucoma, corneal, and retinal diseases. We performed a systematic database search in Ovid MEDLINE and Ovid Embase on 5th April 2022 using the following keywords: 'primary open angle glaucoma', 'glaucoma surgery', 'corneal wound healing', 'corneal endothelial dysfunction', 'diabetic retinopathy', 'diabetic macular oedema', 'age-related macular degeneration', 'rho kinase inhibitor', 'rho-kinase inhibitor', rock inhibitor', 'ripasudil', 'netarsudil' and 'fasudil'. Abstracts were screened for relevant studies and results summarized in tables. The analysis of trials done for ROCK inhibitors reveals that they are safe and efficacious drugs, demonstrating noninferiority to existing medical treatments and effective when combined with existing treatments, and are approved for use in treating glaucoma, but not corneal or retinal diseases. Questions remain, however, regarding optimal dosage, patient selection, and cost-effectiveness. ROCK inhibitors demonstrate significant efficacy in reducing intraocular pressure by improving aqueous humour outflow. Additionally, ROCK inhibitors show promise in enhancing endothelial cell migration, thus providing a novel treatment avenue for corneal diseases such as Fuchs endothelial dystrophy. In retinal conditions, including diabetic retinopathy and age-related macular degeneration, ROCK inhibitors reduce vascular permeability, inflammation, and fibrosis, stabilising disease progression.
鉴于Rho激酶(ROCK)抑制剂在细胞调节中具有多方面作用,尤其是在眼部疾病中,其在眼科的治疗潜力正受到关注。本综述综合了关于ROCK抑制剂在青光眼、角膜疾病和视网膜疾病中的疗效与安全性的临床和临床前研究结果。我们于2022年4月5日在Ovid MEDLINE和Ovid Embase数据库中进行了系统检索,使用了以下关键词:“原发性开角型青光眼”“青光眼手术”“角膜伤口愈合”“角膜内皮功能障碍”“糖尿病性视网膜病变”“糖尿病性黄斑水肿”“年龄相关性黄斑变性”“Rho激酶抑制剂”“rho-激酶抑制剂”“ROCK抑制剂”“ripasudil”“netarsudil”和“fasudil”。筛选摘要以获取相关研究,并将结果汇总成表格。对ROCK抑制剂进行的试验分析表明,它们是安全有效的药物,与现有药物治疗相比不逊色,与现有治疗联合使用时有效,已被批准用于治疗青光眼,但未被批准用于治疗角膜或视网膜疾病。然而,关于最佳剂量、患者选择和成本效益仍存在问题。ROCK抑制剂通过改善房水流出在降低眼压方面显示出显著疗效。此外,ROCK抑制剂在促进内皮细胞迁移方面显示出前景,从而为诸如Fuchs内皮营养不良等角膜疾病提供了一种新的治疗途径。在包括糖尿病性视网膜病变和年龄相关性黄斑变性在内的视网膜疾病中,ROCK抑制剂可降低血管通透性、炎症和纤维化,稳定疾病进展。