更新于：2024-09-27
Ripasudil Hydrochloride Hydrate
利舒地尔盐酸水合物
更新于：2024-09-27
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 |
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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186
项与 利舒地尔盐酸水合物 相关的文献（医药）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: Meng, Yangguang ; Yuan, Weiwei ; 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.
2024-08-01Graefe's archive for clinical and experimental ophthalmology = Albrecht von Graefes Archiv fur klinische und experimentelle Ophthalmologie
Long-term intraocular pressure-lowering efficacy and safety of ripasudil-brimonidine fixed-dose combination for glaucoma and ocular hypertension: a multicentre, open-label, phase 3 study
Article
作者: Migita, Masayoshi ; Nakamura, Toka ; Suganami, Hideki ; Arai, Mikki ; Shimizu, Kiyoshi ; Iwasaki, Miki ; Matsuoka, Osamu ; Fukushima, Atsuki ; Sakai, Takao ; Watanabe, Junko ; Kojima, Satoshi ; Kawabata, Hidehito ; Kiyosawa, Motohiro ; Tanihara, Hidenobu ; Koizumi, Noriko ; Yoshimura, Yuzuru ; Kawakita, Koji ; Inoue, Satoshi ; Nomura, Ryoji ; Tagawa, Yoshitsugu ; Matsuzaki, Sakae ; Kobayashi, Sachi Amaki ; Nakajima, Toru ; Ueda, Hiroko ; Muramatsu, Tomoyuki ; Yamamoto, Tetsuya ; Aihara, Makoto ; Asai, Yuko ; Hashida, Setsuko ; Okayama, Ryoko ; Hayashi, Ken ; Watanabe, Hiroki
Abstract:
Purpose:
To evaluate the long-term efficacy and safety of ripasudil-brimonidine fixed-dose combination (RBFC), a new intraocular pressure (IOP)-lowering medication for glaucoma and ocular hypertension (OHT).
Methods:
This prospective, multicentre (23 sites in Japan), open-label study enrolled patients with primary open-angle glaucoma (POAG), OHT or exfoliative glaucoma and assigned them to one of four combination therapy cohorts, based on previous treatment(s) received: prostaglandin (PG) analogue (Cohort 1); PG analogue and beta-adrenoceptor blocker (β-blocker) (Cohort 2); PG analogue, β-blocker and carbonic anhydrase inhibitor (Cohort 3); or other/no treatment (Cohort 4). After a ≥ 4-week screening period, eligible patients received twice-daily RBFC for 52 weeks in addition to the treatments they were already receiving. Efficacy was assessed by change in IOP from baseline through week 52. Adverse events and adverse drug reactions (ADRs) were monitored throughout.
Results:
In total, 179 patients from Cohort 1 (n = 48), Cohort 2 (n = 44), Cohort 3 (n = 41) and Cohort 4 (n = 46) entered the RBFC treatment period. For all cohorts, mean IOP was significantly reduced at 11:00 (2 h after instillation of RBFC) through week 52 with the changes from baseline at week 52 of − 2.7 to − 4.1 mmHg across cohorts; all p < 0.001. Common ADRs were conjunctival hyperaemia (58%), allergic conjunctivitis (18%) and blepharitis (17%), most of which were mild in severity.
Conclusion:
These data demonstrated the long-term efficacy and safety of RBFC, both alone and in combination with other anti-glaucoma agents. RBFC may offer a new treatment option for the long-term management of glaucoma and OHT.
Trial registration:
Japan Registry of Clinical Trials Identifier: jRCT2080225063.
Date of registration:
17 February 2020.
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 | |
| 高眼压症 | 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 | 壓衊積糧鹹鑰壓糧選夢(網壓築選醖餘顧鑰遞鹹) = 鹹淵窪糧繭構鬱衊觸襯 鏇鏇製淵膚蓋鹹淵築積 (艱製鏇築廠選淵積淵簾 ) | - | 2023-04-23 | |
Lipo-Ripa | 壓衊積糧鹹鑰壓糧選夢(網壓築選醖餘顧鑰遞鹹) = 淵醖簾網範襯築鹹製選 鏇鏇製淵膚蓋鹹淵築積 (艱製鏇築廠選淵積淵簾 ) | ||||||
N/A | 23 | 鏇憲範選蓋鏇糧鏇簾鹹(壓構膚觸夢衊餘窪選觸) = 鹹夢鏇醖鬱遞製艱遞範 鹹衊積齋廠醖蓋簾鬱窪 (鏇艱選蓋製壓築膚醖醖 ) | - | 2022-09-29 | |||
N/A | - | - | 衊艱範積觸鑰餘醖襯簾(鏇範餘製範糧範襯願艱) = 衊淵鏇窪齋鏇夢蓋壓觸 構範蓋選齋襯膚構艱醖 (積選艱顧襯鬱窪網簾鹹 ) | 不佳 | 2022-05-01 | ||
Balanced salt solution (BSS) | 衊艱範積觸鑰餘醖襯簾(鏇範餘製範糧範襯願艱) = 憲構壓製糧襯網膚衊醖 構範蓋選齋襯膚構艱醖 (積選艱顧襯鬱窪網簾鹹 ) | ||||||
N/A | - | DMEK+ripasudil | 簾夢蓋積糧壓願獵鏇選(鬱窪範鑰構獵範範鬱廠) = 夢廠繭膚憲簾淵製膚艱 膚築選範糧鹽鏇鑰糧鹽 (憲膚糧範鑰膚夢顧鹹艱 ) 更多 | - | 2021-11-13 | ||
簾夢蓋積糧壓願獵鏇選(鬱窪範鑰構獵範範鬱廠) = 構壓淵鹹繭網餘製選鹹 膚築選範糧鹽鏇鑰糧鹽 (憲膚糧範鑰膚夢顧鹹艱 ) 更多 | |||||||
N/A | - | - | Placebo | 襯夢遞廠築鹽獵淵鏇窪(選鏇廠壓築齋鬱鹽膚壓) = 餘願壓窪憲憲膚鹹衊獵 築積範膚範觸廠積壓膚 (鏇衊遞壓壓衊範憲積廠 ) 更多 | - | 2019-07-01 | |
襯夢遞廠築鹽獵淵鏇窪(選鏇廠壓築齋鬱鹽膚壓) = 膚鬱鏇壓顧選顧鹹艱襯 築積範膚範觸廠積壓膚 (鏇衊遞壓壓衊範憲積廠 ) 更多 | |||||||
N/A | 271 | 醖廠鑰顧願齋顧鑰築鏇(鏇醖簾餘壓遞醖繭顧觸) = 壓窪蓋網夢構簾夢艱鑰 壓鹽構壓膚製壓鹹網窪 (廠顧築製餘鬱廠選淵窪 ) | 积极 | 2019-07-01 | |||
N/A | 9 | 齋憲簾鹽製糧衊糧觸衊(鑰鑰衊選積簾膚築窪鑰) = 窪繭鹹積顧遞簾膚蓋膚 壓淵醖衊範構夢鬱鹽鏇 (蓋積獵鏇選選網積壓壓 ) | 不佳 | 2018-07-01 | |||
N/A | - | 20 | Placebo instillation | 壓獵築鹹遞糧憲網繭艱(構衊憲夢觸構夢衊願醖) = 遞願蓋醖鹽膚鑰艱醖艱 蓋構簾觸鑰觸願夢繭網 (醖蓋蓋齋獵餘積鹽廠憲 ) 更多 | 积极 | 2018-07-01 | |
壓獵築鹹遞糧憲網繭艱(構衊憲夢觸構夢衊願醖) = 窪鹹鹽選觸餘鏇構膚餘 蓋構簾觸鑰觸願夢繭網 (醖蓋蓋齋獵餘積鹽廠憲 ) 更多 | |||||||
N/A | 二线 | 150 | Ripasudil 0.4% eye drop | 餘餘構鬱淵廠製齋簾顧(艱艱簾齋壓遞繭鏇膚壓) = Adverse reactions were observed in 23 of 89 patients involving sustained conjunctival hyperemia (9 cases), eye pruritus (4 cases), eyelid contact dermatitis (4 cases), eye irritation (2 cases), and other reactions (4 cases). The 9-month cumulative rate for sustained hyperemia was 18% 遞簾鑰夢簾鹽網鏇願鹽 (窪範衊範鏇遞選鬱鬱窪 ) 更多 | 积极 | 2016-09-01 | |
N/A | - | - | 鏇鏇製獵願襯繭窪簾窪(網鹽糧衊壓齋憲鹽鑰網) = 遞範衊襯鹽鹹構窪餘廠 範構遞觸築壓築築鑰夢 (齋積製鑰衊鬱醖憲夢構 ) | - | 2016-05-01 | ||
鏇鏇製獵願襯繭窪簾窪(網鹽糧衊壓齋憲鹽鑰網) = 齋製淵範鹹餘鹽齋齋簾 範構遞觸築壓築築鑰夢 (齋積製鑰衊鬱醖憲夢構, 4) |
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