Rho Kinase (ROCK) Inhibitors in the Treatment of Glaucoma and Glaucoma Surgery: A Systematic Review of Early to Late Phase Clinical Trials
<b>Background/Objectives</b>: Primary open-angle glaucoma (POAG) is an anterior optic neuropathy that can lead to irreversible vision loss if untreated. Prostaglandin analogues are the first-line treatment, but new drug classes, such as rho kinase (ROCK) inhibitors, are being explored. T...
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MDPI AG
2025-04-01
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| author | Jit Kai Tan Peng Tee Khaw Christin Henein |
| author_facet | Jit Kai Tan Peng Tee Khaw Christin Henein |
| author_sort | Jit Kai Tan |
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| description | <b>Background/Objectives</b>: Primary open-angle glaucoma (POAG) is an anterior optic neuropathy that can lead to irreversible vision loss if untreated. Prostaglandin analogues are the first-line treatment, but new drug classes, such as rho kinase (ROCK) inhibitors, are being explored. This review evaluates the efficacy and safety of ROCK inhibitors in treating POAG based on completed trials, comparing results with available natural history data and identifying areas for further research. <b>Methods</b>: A systematic database search was conducted in Ovid MEDLINE and Ovid Embase on 5 April 2022 using the following keywords: ‘glaucoma’, ‘rho kinase inhibitor’, ‘rho-kinase inhibitor’, ‘rock inhibitor’, ‘ripasudil’, ‘netarsudil’, and ‘fasudil’. Abstracts were screened for relevant studies and results summarized in tables. <b>Results</b>: The analysis of trials conducted for ROCK inhibitors reveals that they are a safe and efficacious drug to treat POAG, demonstrating non-inferiority to existing medical treatments. Comparison of data to natural history studies was inconclusive due to the lack of natural history studies and their limitations. The results showed ROCK inhibitors to be effective when combined with existing medical treatments. However, questions remain regarding the optimal dosage, patient selection, and cost-effectiveness. Outcome measures for future trials should be expanded to include additional methods of monitoring disease progression as well as patient quality-of-life. <b>Conclusions</b>: ROCK inhibitors have emerged with a favorable safety profile, efficaciously attenuating intraocular pressure. To elucidate their long-term therapeutic value and safety comprehensively, further independent, large-scale, prospective randomized controlled trials are warranted. Such studies are pivotal to augment our understanding of this emergent medication class. |
| format | Article |
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| institution | OA Journals |
| issn | 1424-8247 |
| language | English |
| publishDate | 2025-04-01 |
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| spelling | doaj-art-8e97dd2e589844d7a4823bb2aa12e6632025-08-20T02:18:20ZengMDPI AGPharmaceuticals1424-82472025-04-0118452310.3390/ph18040523Rho Kinase (ROCK) Inhibitors in the Treatment of Glaucoma and Glaucoma Surgery: A Systematic Review of Early to Late Phase Clinical TrialsJit Kai Tan0Peng Tee Khaw1Christin Henein2Guy’s Campus, King’s College London, London SE1 1UL, UKNational Institute for Health and Care Research Biomedical Research Centre for Ophthalmology, Moorfields Eye Hospital and University College London Institute of Ophthalmology, London EC1V 2PD, UKNational Institute for Health and Care Research Biomedical Research Centre for Ophthalmology, Moorfields Eye Hospital and University College London Institute of Ophthalmology, London EC1V 2PD, UK<b>Background/Objectives</b>: Primary open-angle glaucoma (POAG) is an anterior optic neuropathy that can lead to irreversible vision loss if untreated. Prostaglandin analogues are the first-line treatment, but new drug classes, such as rho kinase (ROCK) inhibitors, are being explored. This review evaluates the efficacy and safety of ROCK inhibitors in treating POAG based on completed trials, comparing results with available natural history data and identifying areas for further research. <b>Methods</b>: A systematic database search was conducted in Ovid MEDLINE and Ovid Embase on 5 April 2022 using the following keywords: ‘glaucoma’, ‘rho kinase inhibitor’, ‘rho-kinase inhibitor’, ‘rock inhibitor’, ‘ripasudil’, ‘netarsudil’, and ‘fasudil’. Abstracts were screened for relevant studies and results summarized in tables. <b>Results</b>: The analysis of trials conducted for ROCK inhibitors reveals that they are a safe and efficacious drug to treat POAG, demonstrating non-inferiority to existing medical treatments. Comparison of data to natural history studies was inconclusive due to the lack of natural history studies and their limitations. The results showed ROCK inhibitors to be effective when combined with existing medical treatments. However, questions remain regarding the optimal dosage, patient selection, and cost-effectiveness. Outcome measures for future trials should be expanded to include additional methods of monitoring disease progression as well as patient quality-of-life. <b>Conclusions</b>: ROCK inhibitors have emerged with a favorable safety profile, efficaciously attenuating intraocular pressure. To elucidate their long-term therapeutic value and safety comprehensively, further independent, large-scale, prospective randomized controlled trials are warranted. Such studies are pivotal to augment our understanding of this emergent medication class.https://www.mdpi.com/1424-8247/18/4/523glaucomaprimary open-angle glaucomaocular hypertensionrho kinase inhibitorsglaucoma filtration surgeryfibrosis |
| spellingShingle | Jit Kai Tan Peng Tee Khaw Christin Henein Rho Kinase (ROCK) Inhibitors in the Treatment of Glaucoma and Glaucoma Surgery: A Systematic Review of Early to Late Phase Clinical Trials Pharmaceuticals glaucoma primary open-angle glaucoma ocular hypertension rho kinase inhibitors glaucoma filtration surgery fibrosis |
| title | Rho Kinase (ROCK) Inhibitors in the Treatment of Glaucoma and Glaucoma Surgery: A Systematic Review of Early to Late Phase Clinical Trials |
| title_full | Rho Kinase (ROCK) Inhibitors in the Treatment of Glaucoma and Glaucoma Surgery: A Systematic Review of Early to Late Phase Clinical Trials |
| title_fullStr | Rho Kinase (ROCK) Inhibitors in the Treatment of Glaucoma and Glaucoma Surgery: A Systematic Review of Early to Late Phase Clinical Trials |
| title_full_unstemmed | Rho Kinase (ROCK) Inhibitors in the Treatment of Glaucoma and Glaucoma Surgery: A Systematic Review of Early to Late Phase Clinical Trials |
| title_short | Rho Kinase (ROCK) Inhibitors in the Treatment of Glaucoma and Glaucoma Surgery: A Systematic Review of Early to Late Phase Clinical Trials |
| title_sort | rho kinase rock inhibitors in the treatment of glaucoma and glaucoma surgery a systematic review of early to late phase clinical trials |
| topic | glaucoma primary open-angle glaucoma ocular hypertension rho kinase inhibitors glaucoma filtration surgery fibrosis |
| url | https://www.mdpi.com/1424-8247/18/4/523 |
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