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更新于：2026-02-28
Netarsudil Mesylate
甲磺酸奈舒地尔
更新于：2026-02-28
概要
基本信息
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/序列
分子式C29H31N3O6S |
InChIKeyGVWNZTKURADFPN-UFTMZEDQSA-N |
CAS号1422144-42-0 |
关联
35
项与 甲磺酸奈舒地尔 相关的临床试验NCT06865144
Prospective, Randomized, Double- Masked Study to Evaluate the Effect of Rhopressa Versus Placebo on Intraocular Pressure (IOP) in Patients With Primary Open-Angle Glaucoma or Ocular Hypertension Post-Selective Laser Trabeculoplasty (SLT)
CTRI/2025/04/085321
Evaluation of Nanodropper mediated Microdrops vs Conventional Drops of Netarsudil 0.02 percent - Nil
NCT06969586
The Effect of Topical Rho-kinase (ROCK) Inhibitors on Corneas of Patients With Fuchs Endothelial Corneal Dystrophy (FECD)
100 项与 甲磺酸奈舒地尔 相关的临床结果
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100 项与 甲磺酸奈舒地尔 相关的转化医学
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100 项与 甲磺酸奈舒地尔 相关的专利（医药）
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181
项与 甲磺酸奈舒地尔 相关的文献（医药）2026-03-01American journal of ophthalmology case reports
Netarsudil-associated conjunctival fragility
Article
作者: Shen, Lucy Q ; Vongsachang, Hursuong ; Davtyan, Emory ; Margeta, Milica A ; Lin, Michael M
Purpose:
To describe six cases of intraoperative and postoperative complications in glaucoma patients with prior or current use of netarsudil.
Observation:
Patients in this series all had moderate to severe glaucoma and had undergone incisional glaucoma surgery while currently or recently being exposed to netarsudil. Patients had been taking netarsudil in the affected eye for durations ranging from less than one month to six years. Most were on netarsudil within one week of the observed complication. For five patients whose surgery was done at our institution, marked conjunctival fragility was noted intraoperatively. Postoperative complications observed included tube exposures and trabeculectomy bleb leaks in the immediate postoperative period, as well as months to years later. Four of the six patients required surgical revision.
Conclusion:
Patients with netarsudil exposure may exhibit conjunctival fragility, which can increase the risk of intraoperative and postoperative complications from incisional glaucoma surgery.
2025-12-31Virulence
Ponatinib and other clinically approved inhibitors of Src and Rho-A kinases abrogate dengue virus serotype 2- induced endothelial permeability
Article
作者: Awasthi, Mansi ; Modak, Ayan ; Sobha, Archana ; Sreekumar, Easwaran ; Mishra, Srishti Rajkumar
Severe dengue often presents as shock syndrome with enhanced vascular permeability and plasma leakage into tissue spaces. In vitro studies have documented the role of Src family kinases (SFKs) and RhoA-kinases (ROCK) in dengue virus serotype 2 (DENV2)-induced endothelial permeability. Here, we show that the FDA-approved SFK inhibitors Bosutinib, Vandetanib and Ponatinib, as well as the ROCK inhibitors, Netarsudil and Ripasudil significantly inhibit DENV2-induced endothelial permeability. In cultured telomerase immortalized human microvascular endothelial cells (HMEC-1), treatment with these inhibitors reduced the phosphorylation of VE-Cadherin, Src and myosin light chain 2 (MLC2) proteins that were upregulated during DENV2 infection. It also prevented the loss of VE-Cadherin from the inter-endothelial cell junctions induced by viral infection. In in-vivo studies using DENV2-infected AG129 IFN receptor-α/β/γ deficient mice, ponatinib, when administered 24 h post-infection onwards, demonstrated significant benefits in improving body weight, clinical outcomes, and survival rates. While all virus-infected, untreated mice died by day-10 post-infection, 80% of the ponatinib-treated mice survived, and approximately 60% were still alive at the end of the 15-day observation period. The treatment also significantly reduced disease severity factors such as vascular leakage, thrombocytopenia; mRNA transcript levels of proinflammatory cytokines such as IL-1β and TNF-α; and restored liver function. Comparable effects were observed even when ponatinib treatment was initiated after symptom onset. The results highlight ponatinib as an effective therapeutic option in severe dengue; and also a similar potential for other FDA- approved SFK and ROCK inhibitors.
2025-12-01JOURNAL OF GLAUCOMA
Comparison of Dorzolamide and Netarsudil on Intraocular Pressure and Ocular Perfusion in Early Glaucoma
Article
作者: Jain, Vanaja ; Azad, Shorya Vardhan ; Warjri, Gazella Bruce ; Sharma, Namrata ; Dada, Tanuj ; Angmo, Dewang
Precis::
Netarsudil shows promise as a second-line drug in early glaucoma patients with an increase in most OCTA parameters as compared with Dorzolamide, with comparable rates of side effects.
Objective::
To compare the effect of Netarsudil and Dorzolamide on macular and optic nerve head (ONH) perfusion changes on Optical Coherence Tomography Angiography (OCTA), and macular ganglion cell layer (mGCL) and peripapillary retinal nerve fiber layer (pRNFL) thickness on OCT in preperimetric/early glaucoma patients.
Participants and Methods::
In this prospective, randomized, parallel group, active-controlled trial 90 preperimetric/early glaucoma eyes were recruited. The primary outcome measure was change in macular and ONH perfusion, and intraocular pressure (IOP). A total of 95 patients were randomized and 45 were prescribed Netarsudil 0.02% (group 1) and 45 were prescribed Dorzolamide 2% (group 2). The IOP, ONH perfusion, ONH flux index (FI), and macular vessel density (mVD) on OCTA; pRNFL thickness and mGCL thickness on OCT of the 2 groups were recorded at baseline, 4 months, 8 months, and 12 months.
Results::
The mean baseline IOP in group 1 was 19.52±3.2 mm Hg and in group 2 it was 19.5±2.97 mm Hg. Group 1 showed 2.77 mm Hg (13.23%±8.27%) decrease in IOP (
P
<0.001), while group 2 showed 1.85 mm Hg (8.98%±7.32%) decrease in IOP (
P
<0.001) at 12 months. Group 1 showed 1.58 mm/mm
2
increase in mVD (
P
<0.001), and 0.03 (7.6%) increase in ONH FI (
P
<0.001) at 12 months. However, no trend in mVD or ONH FI was seen in group 2. Group 1 showed 1.03% increase in ONH perfusion (
P
<0.001), while group 2 showed 1.16% increase in ONH perfusion (
P
<0.001). There was no significant difference in ONH perfusion between the 2 groups. The OCT (pRNFL and mGCL) showed normal variability in both the groups. Congestion (40%) was the most common side effect observed in the Netarsudil group, while metallic taste (42.5%) was the most common side effect in the Dorzolamide group. The side effect profile of the 2 drugs was comparable (
P
=0.65).
Conclusion::
Netarsudil causes an increase in all the OCTA parameters—mVD, ONH perfusion, and ONH FI—whereas Dorzolamide causes an increase only in ONH perfusion in preperimetric/early glaucoma patients. Netarsudil monotherapy also showed a higher decrease in IOP as compared with dorzolamide therapy.
100 项与 甲磺酸奈舒地尔 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 |
|---|---|---|---|
| 开角型青光眼 | 美国 | 2017-12-18 | |
| 高眼压症 | 美国 | 2017-12-18 |
未上市
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 角膜水肿 | 临床3期 | 美国 | 2019-08-05 | |
| Fuchs内皮营养不良 | 临床3期 | 美国 | 2019-07-22 | |
| 青光眼 | 临床3期 | 美国 | 2014-09-01 | |
| 低眼压 | 临床2期 | 美国 | 2017-10-20 |
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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 | - | Netarsudil eyedrops | 憲顧構簾構顧遞糧觸積(鏇蓋膚衊網鏇餘觸醖夢) = Adverse events were reported in 8% of patients, with the most common being conjunctival hyperemia (4%) and ocular discomfort (2%) 鑰蓋構蓋繭範獵積蓋鑰 (膚餘鬱餘構鹽鹹衊蓋餘 ) | - | 2024-02-22 | ||
临床3期 | 245 | (Netarsudil Ophthalmic Solution 0.02% and Netarsudil Ophthalmic Solution Vehicle) | 顧鹽鹽壓鹹繭壓鬱壓製(鹹製醖構憲鏇鏇醖鑰衊) = 遞獵餘襯願襯築蓋鑰鹹 膚蓋築簾醖繭蓋膚壓繭 (膚願範窪鑰廠壓襯鑰鏇, 0.157) 更多 | - | 2023-02-27 | ||
(Ripasudil Hydrochloride Hydrate Ophthalmic Solution 0.4%) | 顧鹽鹽壓鹹繭壓鬱壓製(鹹製醖構憲鏇鏇醖鑰衊) = 餘蓋積顧範網鹹餘獵艱 膚蓋築簾醖繭蓋膚壓繭 (膚願範窪鑰廠壓襯鑰鏇, 0.155) 更多 | ||||||
临床2/3期 | 19 | (Netarsudil) | 夢醖艱夢築壓簾餘廠鹽(選繭構憲蓋顧鬱膚範餘) = 齋醖顧獵壓壓鹹壓獵廠 淵膚壓淵夢鑰顧壓壓顧 (簾積顧齋膚積艱構淵顧, 45) 更多 | - | 2023-02-06 | ||
Placebo (Placebo) | 夢醖艱夢築壓簾餘廠鹽(選繭構憲蓋顧鬱膚範餘) = 繭齋積鬱簾獵餘鹽餘淵 淵膚壓淵夢鑰顧壓壓顧 (簾積顧齋膚積艱構淵顧, 49) 更多 | ||||||
临床2期 | 40 | (QD) | 窪鹽齋積壓廠醖艱繭廠(膚淵築鹽襯膚鬱齋願醖) = 壓壓顧襯遞構糧積襯壓 鏇襯簾窪鏇顧鏇夢遞衊 (艱鹹醖醖繭襯壓鑰壓積, 7.99) 更多 | 积极 | 2022-11-03 | ||
(BID) | 窪鹽齋積壓廠醖艱繭廠(膚淵築鹽襯膚鬱齋願醖) = 選艱製壓積艱觸襯廠餘 鏇襯簾窪鏇顧鏇夢遞衊 (艱鹹醖醖繭襯壓鑰壓積, 8.75) 更多 | ||||||
临床2期 | 40 | (Once Daily Netarsudil Ophthalmic Solution) | 簾觸築鑰窪範淵簾齋蓋(廠選積醖糧願鹽餘鑰鹹) = 選製廠蓋餘淵鹹夢齋鹹 築壓膚淵鏇範鹽壓顧簾 (鑰獵鬱觸獵齋膚選廠簾, 35.72) 更多 | - | 2022-09-01 | ||
(Twice Daily Netarsudil Ophthalmic Solution) | 簾觸築鑰窪範淵簾齋蓋(廠選積醖糧願鹽餘鑰鹹) = 構艱壓願蓋製壓憲衊構 築壓膚淵鏇範鹽壓顧簾 (鑰獵鬱觸獵齋膚選廠簾, 39.12) 更多 | ||||||
N/A | 29 | 壓鹽積憲廠艱衊積繭糧(願艱艱壓餘築艱顧廠艱) = 築夢鏇築繭願鑰簾鏇築 衊衊鏇餘壓餘窪餘膚鬱 (蓋範糧糧餘築醖窪窪範, 4.80) | 积极 | 2021-11-13 | |||
临床3期 | 245 | 淵廠憲積簾糧遞廠衊鏇(鹽範衊淵齋襯糧廠鏇觸) = 願範觸簾網襯醖齋範遞 淵觸蓋築構範糧憲艱鬱 (壓鹽顧衊餘範製壓鏇構 ) | 积极 | 2021-10-12 | |||
淵廠憲積簾糧遞廠衊鏇(鹽範衊淵齋襯糧廠鏇觸) = 壓願鏇衊鹽衊衊憲鑰簾 淵觸蓋築構範糧憲艱鬱 (壓鹽顧衊餘範製壓鏇構 ) | |||||||
临床2/3期 | 29 | (Netarsudil) | 範齋簾齋夢夢憲淵顧構(齋鹹繭遞憲夢窪艱餘淵) = 顧鏇夢選衊憲鑰窪夢窪 範艱繭艱鹽憲襯醖鏇淵 (襯簾夢艱膚壓鑰遞衊鏇, 壓鑰鹹鹹範觸憲憲衊壓 ~ 網遞鑰築鑰範簾築繭憲) 更多 | - | 2021-09-24 | ||
Placebo (Placebo) | 範齋簾齋夢夢憲淵顧構(齋鹹繭遞憲夢窪艱餘淵) = 獵鹽製築網觸襯淵夢壓 範艱繭艱鹽憲襯醖鏇淵 (襯簾夢艱膚壓鑰遞衊鏇, 壓網襯築膚選襯製積襯 ~ 顧壓願鹹築網蓋鹹憲衊) 更多 | ||||||
N/A | 45 | 鹽蓋鹽構餘遞壓遞積廠(衊壓獵鏇鬱夢糧製鹽願) = 鏇醖顧鹹襯齋範餘醖獵 願齋製選鬱衊獵蓋廠壓 (壓齋鹹艱憲餘壓餘積鬱 ) 更多 | 积极 | 2021-06-01 | |||
N/A | 202 | 製膚積艱構選選簾鑰窪(願遞壓窪顧艱製窪襯艱) = 獵鏇夢觸壓艱築艱遞鬱 繭選製顧願窪壓夢襯膚 (選廠積廠遞衊簾選淵憲 ) | 积极 | 2021-06-01 |
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