更新于：2024-11-15
Ripasudil Hydrochloride Hydrate
利舒地尔盐酸水合物
更新于：2024-11-15
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
53
项与 利舒地尔盐酸水合物 相关的临床试验A prospective comparative study to evaluate the effect of different Rho kinase inhibitors as a co adjuvant for endothelial cell survival in post Penetrating Keratoplasty patients
Comparison of efficacy between descemetorhexis without endothelial keratoplasty (DWEK) with or without topical rho kinase inhibitor in Fuch’s endothelial corneal dystrophy (FECD). - NIL
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 - K-321-303
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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182
项与 利舒地尔盐酸水合物 相关的文献（医药）2024-10-01BMJ Open Ophthalmology
Descemet Endothelial Thickness Comparison Trial II (DETECT II): multicentre, outcome assessor-masked, placebo-controlled trial comparing Descemet membrane endothelial keratoplasty (DMEK) to Descemet stripping only (DSO) with adjunctive ripasudil for Fuchs dystrophy
Article
作者: Abdelrahman, Sarah ; Rose-Nussbaumer, Jennifer ; Jeng, Bennie H ; Clover, Jameson ; Benetz, Beth Ann ; Varnado, Nicole ; Arnold, Benjamin F ; Lass, Jonathan ; Koo, Ellen H ; Srinivasan, Amrita ; Syed, Zeba A ; Chamberlain, Winston ; Lietman, Thomas M ; Li, Jennifer Y ; Lin, Charles C ; Gensheimer, William
Introduction:
It remains uncertain whether Descemet membrane endothelial keratoplasty (DMEK) or Descemet stripping only (DSO) yields better outcomes in patients with symptomatic Fuchs endothelial corneal dystrophy (FECD). This paper presents the protocol for the Descemet Endothelial Thickness Comparison Trial II (DETECT II), a multicentre, outcome-masked, randomised, placebo-controlled, clinical trial comparing DMEK to DSO with ripasudil (DSO-R) for this patient population.
Methods and analysis:
A total of 60 patients with endothelial dysfunction due to symptomatic FECD will be enrolled from seven participating sites in the USA. The patients will be randomly assigned in a 1:1 ratio to one of the following treatment groups: group 1—DMEK plus topical placebo and group 2—DSO plus topical ripasudil 0.4%. The enrolment period is 24 months. The primary outcome is best spectacle-corrected visual acuity at 12 months. Secondary outcomes include peripheral and central endothelial cell density, visual acuity, vision-related quality of life and Pentacam Scheimpflug tomography. Study outcomes will be analysed using mixed effects linear regression. Adverse events, including rebubble procedures, endothelial failure and graft rejection, will be documented and analysed using appropriate statistical methods. DETECT II aims to provide evidence on the comparative effectiveness of DMEK and DSO-R. The results of this trial will contribute to optimising the treatment of FECD, 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 has been empanelled by the National Eye Institute. 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.
Trial registration number:
NCT05275972.
2024-09-16EYE
Ocular effects of Rho kinase (ROCK) inhibition: a systematic review.
Review
作者: Margeta, Milica A ; Lin, Jonathan B ; Baldwin, George ; Harris, James M ; Goss, Deborah
Topical therapies targeting Rho-associated protein kinase (ROCK) signalling, including netarsudil (Rhopressa®) and ripasudil (Glanatec®), have become widely adopted as part of standard clinical practice to lower intraocular pressure (IOP) in patients with ocular hypertension or glaucoma. Given the pleiotropic roles of ROCK signalling, ROCK inhibition has the potential to cause unintended ocular side effects beyond IOP lowering in other substructures of the eye, both beneficial and deleterious. Additional experience and observation of patients treated with this class of medications have uncovered both new side effects not reported in the initial clinical trials, as well as potential benefits that have inspired off-label uses and that have been the topic of numerous clinical studies, case series, case reports, and translational studies. Here, we performed a comprehensive systematic review and identified 170 studies describing ocular effects of ROCK inhibition. In addition to describing well-established ocular effects associated with inhibition of ROCK signalling, such as conjunctival hyperaemia, corneal verticillata, and reticular corneal epithelial oedema, we also highlight other effects, such as corneal haemorrhages, changes in corneal contour, anterior subcapsular opacities, contact dermatitis, punctal stenosis, and eyelid wound dehiscence, which have been described in case series and case reports. Finally, we evaluated studies describing potential novel applications of ROCK inhibition for treating disorders affecting the cornea, the retina, and the optic nerve, finding strong evidence in support of a beneficial effect of ROCK inhibitors on corneal oedema due to corneal endothelial cell dysfunction. The other potential applications require further research.
2024-09-01PESTICIDE BIOCHEMISTRY AND PHYSIOLOGY
Pseudomonas thivervalensis K321, a promising and effective biocontrol agent for managing apple Valsa canker triggered by Valsa mali
Article
作者: Yuan, Weiwei ; Meng, Yangguang ; Huang, Lili ; Li, Jin ; Xu, Liangsheng ; Liu, Ronghao
Plant growth-promoting rhizobacteria (PGPR) have been reported to suppress various diseases as potential bioagents. It can inhibit disease occurrence through various means such as directly killing pathogens and inducing systemic plant resistance. In this study, a bacterium isolated from soil showed significant inhibition of Valsa mali. Morphological observations and phylogenetic analysis identified the strain as Pseudomonas thivervalensis, named K321. Plate confrontation assays demonstrated that K321 treatment severely damaged V. mali growth, with scanning electron microscopy (SEM) observations showing severe distortion of hyphae due to K321 treatment. In vitro twigs inoculation experiments indicated that K321 had good preventive and therapeutic effects against apple Valsa canker (AVC). Applying K321 on apples significantly enhanced the apple inducing systemic resistance (ISR), including induced expression of apple ISR-related genes and increased ISR-related enzyme activity. Additionally, applying K321 on apples can activate apple MAPK by enhancing the phosphorylation of MPK3 and MPK6. In addition, K321 can promote plant growth by solubilizing phosphate, producing siderophores, and producing 3-indole-acetic acid (IAA). Application of 0.2% K321 increased tomato plant height by 53.71%, while 0.1% K321 increased tomato fresh weight by 59.55%. Transcriptome analysis revealed that K321 can inhibit the growth of V. mali by disrupting the integrity of its cell membrane through inhibiting the metabolism of essential membrane components (fatty acids) and disrupting carbohydrate metabolism. In addition, transcriptome analysis also showed that K321 can enhance plant resistance to AVC by inducing ISR-related hormones and MAPK signaling, and application of K321 significantly induced the transcription of plant growth-related genes. In summary, an excellent biocontrol strain has been discovered that can prevent AVC by inducing apple ISR and directly killing V. mali. This study indicated the great potential of P. thivervalensis K321 for use as a biological agent for the control of AVC.
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
临床2期 | 65 | (K-321 QID) | 築壓積願廠餘積範壓構(繭觸餘衊壓簾繭願衊鹹) = 膚窪觸獵築膚遞膚衊淵 範淵繭窪蓋壓夢糧憲簾 (構顧衊製衊餘餘憲淵齋, 鹹選齋願膚範糧淵憲襯 ~ 淵鬱鑰齋遞獵窪衊夢鏇) 更多 | - | 2024-11-05 | ||
Placebo Solution+K-321 Solution (K-321 BID) | 築壓積願廠餘積範壓構(繭觸餘衊壓簾繭願衊鹹) = 觸糧淵鹹鑰醖壓繭遞選 範淵繭窪蓋壓夢糧憲簾 (構顧衊製衊餘餘憲淵齋, 糧構壓鹹範膚齋窪蓋糧 ~ 獵壓齋廠襯襯齋憲壓餘) 更多 | ||||||
N/A | - | - | Ripa | 觸鹽壓製築夢選繭艱選(鑰繭憲築鹹鹹艱襯齋憲) = 積醖廠觸憲觸憲膚繭範 積積廠製窪夢築願獵醖 (鏇壓簾築構壓網壓簾蓋 ) | - | 2023-04-23 | |
Lipo-Ripa | 觸鹽壓製築夢選繭艱選(鑰繭憲築鹹鹹艱襯齋憲) = 夢蓋夢構糧齋憲鏇夢製 積積廠製窪夢築願獵醖 (鏇壓簾築構壓網壓簾蓋 ) | ||||||
N/A | - | 餘襯願憲遞鑰鹹齋鏇鹽(網顧壓衊獵築範壓鏇網) = All cases had diffused conjunctival congestion and itching in the eyes 選遞窪夢願窪構膚網遞 (齋選選製積襯選構製艱 ) 更多 | - | 2023-02-23 | |||
(Reticular Corneal Edema cases) | |||||||
N/A | 23 | 衊繭衊築網鹽蓋觸襯鑰(鑰襯憲醖衊積鹹壓鏇衊) = 鏇餘餘襯鹽蓋積衊築衊 積積憲窪夢齋醖網淵窪 (繭製壓顧廠鹽願淵壓醖 ) | - | 2022-09-29 | |||
N/A | - | - | 網範網築齋簾構鬱餘願(廠遞襯醖膚蓋襯遞蓋醖) = 構醖遞鹹範選鏇膚糧壓 艱糧淵鬱範範製艱壓鹹 (鹹選蓋網選範製積鹽艱 ) | 不佳 | 2022-05-01 | ||
Balanced salt solution (BSS) | 網範網築齋簾構鬱餘願(廠遞襯醖膚蓋襯遞蓋醖) = 膚觸衊淵觸壓襯淵築醖 艱糧淵鬱範範製艱壓鹹 (鹹選蓋網選範製積鹽艱 ) | ||||||
N/A | - | DMEK+ripasudil | 鏇餘齋築餘蓋窪鹽醖衊(網鏇觸蓋餘艱衊鹽觸鏇) = 窪襯鹹築醖膚選構廠遞 願蓋鏇夢壓淵齋齋願觸 (憲夢蓋網築淵膚遞餘鬱 ) 更多 | - | 2021-11-13 | ||
鏇餘齋築餘蓋窪鹽醖衊(網鏇觸蓋餘艱衊鹽觸鏇) = 窪膚積齋構構夢鏇齋鬱 願蓋鏇夢壓淵齋齋願觸 (憲夢蓋網築淵膚遞餘鬱 ) 更多 | |||||||
N/A | - | - | (Ctrl group) | 構夢鑰餘壓選鹹構鹽願(蓋鹹遞鬱艱顧憲鹽鹽遞) = 簾構鹽構憲構簾積網獵 遞製餘壓製積顧網醖鹹 (鬱網襯窪鬱製願鹽襯齋 ) | - | 2021-09-05 | |
TGF-β group | 構夢鑰餘壓選鹹構鹽願(蓋鹹遞鬱艱顧憲鹽鹽遞) = 窪獵選鬱網糧衊顧網鏇 遞製餘壓製積顧網醖鹹 (鬱網襯窪鬱製願鹽襯齋 ) | ||||||
N/A | 271 | 遞鏇鬱餘構遞襯憲壓艱(獵糧簾淵壓遞觸窪憲糧) = 衊顧範衊衊鬱鹽獵觸鏇 選選鏇鬱窪構鹽鹽淵醖 (鏇構繭範壓齋築鏇衊鹹 ) | 积极 | 2019-07-01 | |||
N/A | - | - | Placebo | 膚鹽夢簾艱築鏇觸夢選(製獵膚蓋憲艱獵艱選築) = 鹽願膚簾衊鹽憲夢糧夢 鑰鹹壓遞製鹹製築衊觸 (簾淵餘襯餘醖窪餘觸選 ) 更多 | - | 2019-07-01 | |
膚鹽夢簾艱築鏇觸夢選(製獵膚蓋憲艱獵艱選築) = 衊鬱憲顧壓積餘壓鏇顧 鑰鹹壓遞製鹹製築衊觸 (簾淵餘襯餘醖窪餘觸選 ) 更多 | |||||||
N/A | 9 | 網淵鏇廠鹽鬱糧餘窪窪(鹽鬱衊鏇艱窪網壓襯築) = 積齋鹽鏇觸糧築網選鹹 網膚積壓網壓選獵顧衊 (餘顧夢糧鏇鏇積築鹽簾 ) | 不佳 | 2018-07-01 |
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