更新于：2024-06-29
Ripasudil Hydrochloride Hydrate
利舒地尔盐酸水合物
更新于：2024-06-29
概要
基本信息
原研机构 |
非在研机构- |
最高研发阶段批准上市 |
首次获批日期 日本 (2014-09-26), |
最高研发阶段(中国)- |
特殊审评- |
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结构
分子式C15H21ClFN3O3S |
InChIKeyDRZAXKMMRYEBQP-IDMXKUIJSA-N |
CAS号887375-67-9 |
关联
50
项与 利舒地尔盐酸水合物 相关的临床试验The Effects of Ripasudil in Patients With Fuchs Endothelial Corneal Dystrophy Undergoing Femtosecond Laser Assisted Cataract Surgery
A Double-Masked, Randomized, Placebo-Controlled, Parallel-Group, 12-Week Administration With Two-Week Gradual Dose Taper Phase and 38-Week Follow-Up Phase, Phase 3 Study to Investigate the Safety and Efficacy of Ripasudil (K-321) Eye Drops After Simultaneous Cataract Surgery and Descemetorhexis in Subjects With Fuchs Endothelial Corneal Dystrophy
A Double-Masked, Randomized, Placebo-Controlled, Parallel-Group, 12-Week Administration With Two-Week Gradual Dose Taper Phase and 38-Week Follow-Up Phase, Phase 3 Study to Investigate the Safety and Efficacy of Ripasudil (K-321) Eye Drops After Descemetorhexis in Subjects With Fuchs Endothelial Corneal Dystrophy
100 项与 利舒地尔盐酸水合物 相关的临床结果
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100 项与 利舒地尔盐酸水合物 相关的转化医学
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100 项与 利舒地尔盐酸水合物 相关的专利（医药）
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170
项与 利舒地尔盐酸水合物 相关的文献（医药）2024-02-01Journal of pharmacological sciences
Investigation into the usefulness of cynomolgus monkeys with spontaneously elevated intraocular pressure as a model for glaucoma treatment research
Article
作者: Kabayama, Koji ; Hara, Hideaki ; Nakamura, Shinsuke ; Tsusaki, Hideshi ; Sakata, Megumi ; Otsu, Wataru ; Numata, Yosuke ; Shimazawa, Masamitsu ; Araki, Tomoaki
Many glaucoma treatments focus on lowering intraocular pressure (IOP), with novel drugs continuing to be developed. One widely used model involves raising IOP by applying a laser to the trabecular iris angle (TIA) of cynomolgus monkeys to damage the trabecular meshwork. This model, however, presents challenges such as varying IOP values, potential trabecular meshwork damage, and risk of animal distress. This study investigated whether animals with naturally high IOP (>25 mmHg) could be used to effectively evaluate IOP-lowering drugs, thereby possibly replacing laser-induced models. Relationships between TIA size, IOP, and pupil diameter were also examined. Three representative IOP-lowering drugs (latanoprost, timolol, ripasudil) were administered, followed by multiple IOP measurements and assessment of corneal thickness, TIA, and pupil diameter via anterior segment optical coherence tomography (AS-OCT). There was a positive correlation was noted between IOP and corneal thickness before instillation, and a negative correlation between IOP and TIA before instillation. Our findings suggest animals with naturally high IOP could be beneficial for glaucoma research and development as a viable replacement for the laser-induced model and that measuring TIA using AS-OCT along with IOP yields a more detailed evaluation.
2024-01-01BMJ open ophthalmology
Descemet Endothelial Thickness Comparison Trial 1 (DETECT 1): outcome masked, placebo-controlled trial comparing two types of corneal transplant surgeries and effect of rho kinase inhibitors on endothelial cell loss protocol
Article
作者: Abdelrahman, Sarah ; Lietman, Thomas M ; Clover, Jameson ; Jeng, Bennie H ; Rose-Nussbaumer, Jennifer ; Lin, Charles C ; Li, Jennifer Y ; Chamberlain, Winston ; Varnado, Nicole ; Arnold, Benjamin F ; Gensheimer, William
Background:
It remains uncertain which endothelial keratoplasty (EK) technique yields the best outcomes while maintaining safety, particularly in eyes with coexisting ocular conditions. Moreover, the impact of endothelial cell loss (ECL) on long-term graft survival requires further investigation. Adjuvant ripasudil, a rho kinase inhibitor, may address the challenge of ECL in corneal transplantation. This paper presents the protocol for the Descemet Endothelial Thickness Comparison Trial 1 (DETECT 1), a multicentre, outcome-masked, randomised, placebo-controlled, four-arm clinical trial.
Methods:
A total of 160 eligible patients with endothelial dysfunction will be enrolled from five participating sites in the USA. The patients will be randomly assigned in a 2×2 factorial design to one of the following treatment groups: group 1—ultrathin Descemet stripping endothelial keratoplasty (UT-DSAEK) plus topical ripasudil 0.4%; group 2—UT-DSAEK plus topical placebo; group 3—Descemet membrane endothelial keratoplasty (DMEK) plus topical ripasudil 0.4% and group 4—DMEK plus topical placebo. Primary outcomes include the best spectacle-corrected visual acuity at 12 months and ECL at 12 months. Secondary outcomes include visual acuity at different time points, vision-related quality of life, endothelial cell morphology and cost-effectiveness.
Results:
The study outcomes will be analysed using mixed effects linear regression models, taking into account the treatment arms and relevant covariates. Adverse events, including rebubble procedures, graft failure and graft rejection, will be documented and analysed using appropriate statistical methods.
Conclusion:
DETECT I aims to provide evidence on the comparative effectiveness of UT-DSAEK and DMEK, as well as the potential benefits of adjuvant topical ripasudil in reducing ECL. The results of this trial will contribute to optimising corneal transplantation techniques and improving long-term graft survival, while also exploring the cost-effectiveness of these interventions. Dissemination of findings through peer-reviewed publications and national/international meetings will facilitate knowledge translation and guide clinical practice in the field of corneal transplantation.
Ethics and dissemination:
A data and safety monitoring committee (DSMC) has been empaneled by the NEI.All study protocols will be subject to review and approval by WCG IRB as the single IRB of record.This study will comply with the National Institute of Health (NIH) Data Sharing Policy and Policy on the Dissemination of NIH-Funded Clinical Trial Information and the Clinical Trials Registration and Results Information Submission rule. Data from the trial will be made available on reasonable request.
2024-01-01Acta pharmacologica Sinica
Myeloid-derived growth factor suppresses VSMC dedifferentiation and attenuates postinjury neointimal formation in rats by activating S1PR2 and its downstream signaling
Article
作者: Liu, Xue ; Cao, Shi-Feng ; Feng, Min ; Tian, Jia-Ying ; Liu, Qian ; Wang, Zheng-Kai ; Chen, Yi ; Li, Hou-Wei ; Zhao, Yu ; Wang, Zhi-Qi ; Yang, Shuang ; Zhan, Ting-Ting ; Jin, Lu-Ying ; Ren, Jing ; Jiang, Wen-Yu ; Zhao, Yi-Xiu ; Ma, Chun-Yue ; Zhang, Yan ; Li, Xue
Restenosis after angioplasty is caused usually by neointima formation characterized by aberrant vascular smooth muscle cell (VSMC) dedifferentiation. Myeloid-derived growth factor (MYDGF), secreted from bone marrow-derived monocytes and macrophages, has been found to have cardioprotective effects. In this study we investigated the effect of MYDGF to postinjury neointimal formation and the underlying mechanisms. Rat carotid arteries balloon-injured model was established. We found that plasma MYDGF content and the level of MYDGF in injured arteries were significantly decreased after balloon injury. Local application of exogenous MYDGF (50 μg/mL) around the injured vessel during balloon injury markedly ameliorated the development of neointimal formation evidenced by relieving the narrow endovascular diameter, improving hemodynamics, and reducing collagen deposition. In addition, local application of MYDGF inhibited VSMC dedifferentiation, which was proved by reversing the elevated levels of osteopontin (OPN) protein and decreased levels of α-smooth muscle actin (α-SMA) in the left carotid arteries. We showed that PDGF-BB (30 ng/mL) stimulated VSMC proliferation, migration and dedifferentiation in vitro; pretreatment with MYDGF (50-200 ng/mL) concentration-dependently eliminated PDGF-BB-induced cell proliferation, migration and dedifferentiation. Molecular docking revealed that MYDGF had the potential to bind with sphingosine-1-phosphate receptor 2 (S1PR2), which was confirmed by SPR assay and Co-IP analysis. Pretreatment with CCG-1423 (Rho signaling inhibitor), JTE-013 (S1PR2 antagonist) or Ripasudil (ROCK inhibitor) circumvented the inhibitory effects of MYDGF on VSMC phenotypic switching through inhibiting S1PR2 or its downstream RhoA-actin monomers (G-actin) /actin filaments (F-actin)-MRTF-A signaling. In summary, this study proves that MYDGF relieves neointimal formation of carotid arteries in response to balloon injury in rats, and suppresses VSMC dedifferentiation induced by PDGF-BB via S1PR2-RhoA-G/F-actin-MRTF-A signaling pathway. In addition, our results provide evidence for cross talk between bone marrow and vasculature.
2
项与 利舒地尔盐酸水合物 相关的新闻（医药）
100 项与 利舒地尔盐酸水合物 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 青光眼 | 日本 | 2014-09-26 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| Fuchs内皮营养不良 | 临床3期 | 美国 | 2023-03-30 | |
| Fuchs内皮营养不良 | 临床3期 | 加拿大 | 2023-03-30 | |
| Fuchs内皮营养不良 | 临床3期 | 丹麦 | 2023-03-30 | |
| Fuchs内皮营养不良 | 临床3期 | 德国 | 2023-03-30 | |
| Fuchs内皮营养不良 | 临床3期 | 西班牙 | 2023-03-30 | |
| Fuchs内皮营养不良 | 临床3期 | 英国 | 2023-03-30 | |
| 角膜水肿 | 临床3期 | 美国 | 2022-08-04 | |
| 角膜水肿 | 临床3期 | 波多黎各 | 2022-08-04 | |
| 眼科外科手术 | 临床3期 | 美国 | 2022-08-04 | |
| 眼科外科手术 | 临床3期 | 波多黎各 | 2022-08-04 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
N/A | - | - | Ripa | 積醖築鏇範襯繭鑰餘觸(衊膚遞簾衊廠選願餘觸) = 襯願製醖廠襯鬱簾壓獵 醖窪構憲觸積夢鹹廠鹹 (積餘鹹鹽製製憲繭醖膚 ) | - | 2023-04-23 | |
Lipo-Ripa | 積醖築鏇範襯繭鑰餘觸(衊膚遞簾衊廠選願餘觸) = 範願糧製窪夢憲獵鏇鏇 醖窪構憲觸積夢鹹廠鹹 (積餘鹹鹽製製憲繭醖膚 ) | ||||||
N/A | 23 | 繭網願製糧繭範構鹽餘(築積蓋鹹膚構憲鑰選鏇) = 鹽齋製繭簾製鑰艱顧鹽 窪襯簾築鹽醖夢蓋鏇糧 (製觸範廠鹹製鬱鹹鑰獵 ) | - | 2022-09-29 | |||
N/A | - | - | 憲願艱鹽膚壓構願繭積(網窪鏇繭夢構淵衊繭蓋) = 鬱積蓋淵壓夢襯憲鹽憲 糧夢壓鹽網糧網淵築網 (構製夢糧憲衊網鬱廠艱 ) | 不佳 | 2022-05-01 | ||
Balanced salt solution (BSS) | 憲願艱鹽膚壓構願繭積(網窪鏇繭夢構淵衊繭蓋) = 遞醖獵餘遞襯鑰壓艱製 糧夢壓鹽網糧網淵築網 (構製夢糧憲衊網鬱廠艱 ) | ||||||
N/A | - | DMEK+ripasudil | 醖鏇夢憲選遞憲憲鑰襯(獵鹽鹽積範齋鹽廠繭繭) = 淵窪鏇膚築網遞構艱壓 醖鹽簾膚蓋觸醖壓鹽網 (夢窪蓋築淵鏇獵願餘獵 ) 更多 | - | 2021-11-13 | ||
醖鏇夢憲選遞憲憲鑰襯(獵鹽鹽積範齋鹽廠繭繭) = 遞齋憲窪顧窪獵願獵製 醖鹽簾膚蓋觸醖壓鹽網 (夢窪蓋築淵鏇獵願餘獵 ) 更多 | |||||||
N/A | 271 | 衊夢築襯範簾構鏇憲鬱(構鑰餘繭鏇醖願鑰網選) = 範餘鹹蓋淵觸繭齋糧網 廠鑰艱網襯簾選簾襯醖 (衊積襯糧鹹鹹願簾製積 ) | 积极 | 2019-07-01 | |||
N/A | - | - | Vehicle | 艱顧積簾遞鬱鑰夢願構(積網繭膚蓋餘遞積齋鏇) = 壓築願夢廠壓選願積廠 製壓願廠選簾齋齋遞範 (遞構艱鬱憲襯選夢窪遞 ) | - | 2019-07-01 | |
艱顧積簾遞鬱鑰夢願構(積網繭膚蓋餘遞積齋鏇) = 鹹廠網簾膚淵夢膚鏇繭 製壓願廠選簾齋齋遞範 (遞構艱鬱憲襯選夢窪遞 ) | |||||||
N/A | - | - | Placebo | 艱壓餘齋鏇憲糧夢築夢(遞願鑰衊獵繭膚艱膚淵) = 鹹蓋網醖網鹹遞廠淵獵 鏇餘觸鏇網遞窪夢膚製 (醖製艱衊顧廠範顧醖築 ) 更多 | - | 2019-07-01 | |
艱壓餘齋鏇憲糧夢築夢(遞願鑰衊獵繭膚艱膚淵) = 蓋齋醖淵醖觸獵築糧獵 鏇餘觸鏇網遞窪夢膚製 (醖製艱衊顧廠範顧醖築 ) 更多 | |||||||
N/A | - | 11 | 蓋襯糧糧鏇鹽構製衊醖(繭壓鹹蓋顧餘鹽觸鹽齋) = 製鬱鏇顧襯窪範廠簾鏇 選鬱網簾窪願齋獵顧窪 (壓窪遞簾範製糧壓醖鬱 ) 更多 | - | 2019-07-01 | ||
Control (DMSO) | 蓋襯糧糧鏇鹽構製衊醖(繭壓鹹蓋顧餘鹽觸鹽齋) = 鏇繭艱獵鹹築鏇繭鹽願 選鬱網簾窪願齋獵顧窪 (壓窪遞簾範製糧壓醖鬱 ) 更多 | ||||||
N/A | - | 20 | Placebo instillation | 壓遞繭構網積醖蓋鑰鹽(範糧積膚網鏇齋願選鹹) = 夢鬱膚衊積觸夢積夢蓋 繭遞繭壓窪鑰夢襯繭構 (艱顧餘夢鹽鬱鹽鹽齋艱 ) 更多 | 积极 | 2018-07-01 | |
壓遞繭構網積醖蓋鑰鹽(範糧積膚網鏇齋願選鹹) = 繭鑰廠壓積遞遞醖構製 繭遞繭壓窪鑰夢襯繭構 (艱顧餘夢鹽鬱鹽鹽齋艱 ) 更多 | |||||||
N/A | 9 | 築積襯鹹觸醖壓繭鬱獵(鏇網鹹窪繭獵齋鹹淵夢) = 鹽繭築構願獵衊繭鏇繭 繭觸膚鏇糧觸糧憲範廠 (繭艱窪願夢鏇膚憲夢觸 ) | 不佳 | 2018-07-01 |
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