Rho激酶抑制剂在青光眼治疗中的应用:目前的观点和未来的方向。

IF 4.7 2区 医学 Q1 CHEMISTRY, MEDICINAL
Drug Design, Development and Therapy Pub Date : 2025-04-02 eCollection Date: 2025-01-01 DOI:10.2147/DDDT.S515166
Eleftherios Chatzimichail, Eirini Christodoulaki, Panagiotis A G Konstas, Georgios N Tsiropoulos, Efstratia Amaxilati, Konstantin Gugleta, Zisis Gatzioufas, Georgios D Panos
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引用次数: 0

摘要

青光眼是一组以视神经损伤和视野丧失为特征的眼部疾病,是世界范围内不可逆失明的主要原因。青光眼对视力损害和失明具有重要的全球性影响。青光眼的治疗传统上依赖于前列腺素类似物、受体阻滞剂、α激动剂和碳酸酐酶抑制剂等药物,这些药物旨在通过各种机制降低眼压。Rho激酶(ROCK)抑制剂最近作为一类新型抗青光眼药物出现,提供了一种通过常规途径增强房水流出的替代方法。最近的临床研究评估了利帕舒地尔(K-115)和奈沙地尔(AR-13324)在治疗各种类型青光眼方面的疗效和安全性,显示出有希望的结果。比较研究表明,ROCK抑制剂不逊于传统的抗青光眼药物,如-受体阻滞剂和前列腺素。此外,新出现的证据表明它们的神经保护特性,这可能在保护视网膜神经节细胞中起作用。此外,当这些药物与青光眼滤过手术联合使用时,已观察到积极的结果,可能提高手术成功率。不良反应,包括结膜充血,鸡斑性角膜,结膜炎和眼咽炎,已报道使用ROCK抑制剂后。然而,在大多数情况下,这些副作用似乎是微妙的。本综述旨在提供ROCK抑制剂的概述,重点是它们的作用机制、临床疗效、安全性和对眼睛健康的额外益处。此外,还将进一步讨论ROCK抑制剂在青光眼治疗中的潜在应用。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Rho Kinase Inhibitors in Glaucoma Management: Current Perspectives and Future Directions.

Glaucoma is a group of eye conditions characterised by optic nerve damage and visual field loss, representing the leading cause of irreversible blindness worldwide. Glaucoma exerts substantial global impact on visual impairment and blindness. The management of glaucoma has traditionally relied on medications such as prostaglandin analogs, beta-blockers, alpha agonists, and carbonic anhydrase inhibitors, which aim to lower intraocular pressure through various mechanisms. Rho kinase (ROCK) inhibitors have recently emerged as a novel class of antiglaucoma drugs, offering an alternative approach by enhancing aqueous humour outflow through the conventional pathway. Recent clinical studies assessing the efficacy and safety of Ripasudil (K-115) and Netarsudil (AR-13324) have demonstrated promising outcomes in the treatment of various types of glaucoma. Comparative studies have shown that ROCK inhibitors are non-inferior to traditional antiglaucomatous medications, such as beta-blockers and prostaglandins. Additionally, emerging evidence suggests their neuroprotective properties, which may play a role in preserving retinal ganglion cells. Furthermore, positive outcomes have been observed when these agents are used in conjunction with glaucoma filtering surgery, potentially enhancing surgical success rates. Adverse effects, including conjunctival hyperemia, cornea verticillata, conjunctivitis, and blepharitis, have been reported following the use of ROCK inhibitors. However, those side effects appear to be subtle in most cases. This review aims to provide an overview of ROCK inhibitors, focusing on their mechanisms of action, clinical efficacy, safety profiles, and additional benefits for eye health. Furthermore, further potential applications of ROCK inhibitors in glaucoma management are going to be discussed.

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来源期刊
Drug Design, Development and Therapy
Drug Design, Development and Therapy CHEMISTRY, MEDICINAL-PHARMACOLOGY & PHARMACY
CiteScore
9.00
自引率
0.00%
发文量
382
审稿时长
>12 weeks
期刊介绍: Drug Design, Development and Therapy is an international, peer-reviewed, open access journal that spans the spectrum of drug design, discovery and development through to clinical applications. The journal is characterized by the rapid reporting of high-quality original research, reviews, expert opinions, commentary and clinical studies in all therapeutic areas. Specific topics covered by the journal include: Drug target identification and validation Phenotypic screening and target deconvolution Biochemical analyses of drug targets and their pathways New methods or relevant applications in molecular/drug design and computer-aided drug discovery* Design, synthesis, and biological evaluation of novel biologically active compounds (including diagnostics or chemical probes) Structural or molecular biological studies elucidating molecular recognition processes Fragment-based drug discovery Pharmaceutical/red biotechnology Isolation, structural characterization, (bio)synthesis, bioengineering and pharmacological evaluation of natural products** Distribution, pharmacokinetics and metabolic transformations of drugs or biologically active compounds in drug development Drug delivery and formulation (design and characterization of dosage forms, release mechanisms and in vivo testing) Preclinical development studies Translational animal models Mechanisms of action and signalling pathways Toxicology Gene therapy, cell therapy and immunotherapy Personalized medicine and pharmacogenomics Clinical drug evaluation Patient safety and sustained use of medicines.
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