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
Abstract
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.
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.