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更新于：2026-09-08
Netarsudil Mesylate
甲磺酸奈舒地尔
更新于：2026-09-08
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NCT07588152
Adaptive Optics Gonioscopy In Vivo Imaging of the Effects of Rhopressa on the Trabecular Meshwork in Patients With Ocular Hypertension or Glaucoma
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
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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207
项与 甲磺酸奈舒地尔 相关的文献（医药）2026-12-01MOLECULAR BIOLOGY REPORTS
The effects of netarsudil ophthalmic solution on the expression of genes involved in fibrogenesis in orbital fibroblasts of patients with thyroid eye disease
Article
作者: Heydari, Mojtaba ; Khademi, Behzad ; Sanie-Jahromi, Fatemeh ; Armaghanifard, Vahid ; Attar, Alireza
BACKGROUND:
Thyroid eye disease (TED) is an autoimmune orbital disorder characterized by fibroblast activation, myofibroblast differentiation, and excessive extracellular matrix production. RhoA/ROCK signaling is increasingly implicated in these fibrotic processes. This study aimed to investigate the effects of the Rho-associated protein kinase (ROCK) inhibitor netarsudil on the expression of fibrogenesis-related genes in orbital fibroblasts derived from patients with TED.
METHODS AND RESULTS:
Primary orbital fibroblasts were isolated from two patients with TED. Cells were treated with varying concentrations of netarsudil (ranging from 2 × 10- 2 to 2 × 10- 8 mg/mL). Gene expression of fibrogenesis markers, including TGF-β, α-SMA, ZEB1, Snail, Thy-1, and β-catenin, was assessed via quantitative real-time PCR. Our results demonstrated that netarsudil treatment at non-cytotoxic concentrations not only did not significantly suppress the mRNA expression of the examined fibrogenic markers, but also upregulated the expression of TGF-β, α-SMA, and ZEB1. Higher concentrations of netarsudil appeared to reduce cell viability, suggesting that apparent antifibrotic effects at elevated doses may be secondary to cytotoxicity rather than pathway-specific transcriptional repression.
CONCLUSIONS:
Our findings suggest that non-cytotoxic dose of netarsudil, is insufficient to reverse the constitutively pro-fibrotic transcriptional program in TED orbital fibroblasts. The lack of direct antifibrotic efficacy highlights the complexity of TED fibrogenesis and suggests that redundant or parallel signaling pathways may limit the impact of isolated ROCK inhibition. Further research is required to evaluate combination therapies or alternative targets in TED-related fibrosis.
2026-06-12Science Advances
Quantitative prediction of siRNA complexation by ionizable drugs enables their codelivery in nanoparticles
Article
作者: Han, Sangwoo ; Shoichet, Molly S. ; Donders, Eric N. ; Slaughter, Kai V. ; Tom, Gary ; Roland, Olivia ; Dang, Mickael ; Cheng, Austin H. ; Aspuru-Guzik, Alán ; Chiu, Eric S. Y. ; Li, Xiang Olivia
The ionizable lipid in lipid nanoparticles can be replaced with ionizable drugs to encapsulate small interfering RNA (siRNA) and allow intracellular codelivery. We wondered whether we could develop a predictive model to aid in formulation design. A small-scale screening assay was designed to evaluate siRNA complexation by ionizable drugs at low pH and validated experimentally with ionizable drug nanoparticle (IDNP) formulations. We found that siRNA complexation could be predicted by drug hydrophobicity, aromaticity, proximity of nitrogen and oxygen atoms to aromatic rings, and a machine learning model using five molecular descriptors encoding pharmacophore and structural information. For complexing drugs, siRNA encapsulation efficiency in IDNPs was related to hydrophobicity, molar refractivity, chiral centers, hydrogen bond donors, and topological charge. Netarsudil was predicted to encapsulate siRNA at high efficiency and was thus tested experimentally with siRNA targeting connective tissue growth factor (
CTGF
) in fibrotic human trabecular meshwork cells: Reduced
CTGF
mRNA expression and actin network density were observed. These predictive tools may unlock combination therapies.
2026-06-01ADVANCES IN THERAPY
Phase III Prospective Randomised Study of Netarsudil and Concomitant Latanoprost Efficacy and Safety for Primary Open-Angle Glaucoma or Ocular Hypertension in Japan: J-ROCKET-2
Article
作者: Aihara, Makoto
INTRODUCTION:
This prospective, phase III, randomised, multicentre, double-masked study (jRCT2031210122) assessed the intraocular pressure (IOP)-lowering efficacy, tolerability and superiority of netarsudil 0.02% + concomitant latanoprost 0.005% to placebo + latanoprost in Japanese participants with primary open-angle glaucoma (POAG) or ocular hypertension (OHT) who have inadequate IOP reduction with latanoprost monotherapy.
METHODS:
Participants received latanoprost once daily for 6 weeks. Eligible participants (n = 246) with POAG (n = 165) or OHT (n = 81) were randomised (1:1) to netarsudil + latanoprost (n = 122) or placebo + latanoprost (n = 124) for 4 weeks. Primary endpoint was mean diurnal (MD) IOP at week 4, with superiority demonstrated if the between-group difference in least squares mean MD IOP was < 0 and p < 0.05. Secondary endpoints included MD IOP at weeks 1 and 2. Adverse events (AEs) were recorded.
RESULTS:
At week 4, MD IOP (standard error) was 15.29 (0.17) versus 17.65 (0.17) mmHg with netarsudil + latanoprost versus placebo + latanoprost, respectively [difference, - 2.36 (p < 0.0001)]. The differences at weeks 1 and 2 between netarsudil + latanoprost and placebo + latanoprost were - 2.47 and - 2.41 (p < 0.0001), respectively. At each visit, netarsudil + latanoprost significantly reduced MD IOP versus placebo + latanoprost (p < 0.0001). Of those receiving netarsudil + latanoprost, 64.8% reported AEs versus 21.0% receiving placebo + latanoprost. Conjunctival hyperaemia was the most reported AE in both groups (53.3% vs. 6.5%). No serious AEs were reported.
CONCLUSION:
Netarsudil + latanoprost was superior to placebo + latanoprost in lowering elevated IOP in Japanese patients with POAG or OHT. No new safety signals were reported.
TRIAL REGISTRATION:
Japan registry of clinical trials: jRCT2031210122.
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
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 青光眼 | 日本 | 2026-06-19 | |
| 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 | |
| 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
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N/A | 40 | 繭鹽獵願網窪觸餘構鹽(衊蓋艱蓋網淵襯餘憲鑰) = 鑰範憲壓構願製繭獵獵 夢鏇鹹選簾窪淵艱範糧 (餘廠壓廠憲製繭網鹽憲 ) 更多 | 不佳 | 2026-05-03 | |||
N/A | 235 | (primary open-angle glaucoma (OAG)) | 積鏇選構網選繭夢構遞(齋鑰鹹觸構顧鬱醖觸鬱) = 築鏇廠遞選築淵淵鹽觸 憲淵築餘醖遞鹹艱顧簾 (獵願襯顧鬱選淵齋憲顧, 3.9) 更多 | 积极 | 2026-05-03 | ||
(combined mechanism glaucoma (CMG)) | 積鏇選構網選繭夢構遞(齋鑰鹹觸構顧鬱醖觸鬱) = 襯鑰選廠壓製鏇艱築衊 憲淵築餘醖遞鹹艱顧簾 (獵願襯顧鬱選淵齋憲顧, 4.1) 更多 | ||||||
N/A | 42 | Netarsudil as adjunctive therapy (Exfoliative Glaucoma) | 醖鬱積範積襯網襯遞醖(築淵獵廠觸鹹膚憲製糧) = conjunctival hyperemia (20 patients 47.6%), allergic conjunctivitis (4 patients, 9.5%), and superficial punctate keratitis (3 patient, 7.1%). 壓艱構糧鹹夢網鬱積廠 (觸遞簾範製鹽鏇夢壓範 ) | 积极 | 2026-05-03 | ||
N/A | VEGF | CFTR | 439 | 糧網窪網糧製鑰獵獵顧(鑰衊顧構選衊構鏇蓋壓) = 獵積願繭築襯夢襯蓋醖 鏇獵願蓋範壓鑰願鬱鹹 (糧衊築糧簾範獵餘膚願 ) | 积极 | 2026-05-03 | ||
糧網窪網糧製鑰獵獵顧(鑰衊顧構選衊構鏇蓋壓) = 齋鹹顧簾鹹鏇網製襯艱 鏇獵願蓋範壓鑰願鬱鹹 (糧衊築糧簾範獵餘膚願 ) | |||||||
N/A | - | Netarsudil eyedrops | 顧獵網鹹壓鏇糧範製廠(鏇鑰簾憲鹹選獵憲醖艱) = Adverse events were reported in 8% of patients, with the most common being conjunctival hyperemia (4%) and ocular discomfort (2%) 願蓋遞憲鏇淵衊夢糧選 (糧願蓋夢鬱範獵鏇鑰繭 ) | - | 2024-02-22 | ||
临床3期 | 245 | (Netarsudil Ophthalmic Solution 0.02% and Netarsudil Ophthalmic Solution Vehicle) | 鑰憲構鏇觸鏇簾齋憲蓋(襯齋顧醖糧蓋積構範餘) = 簾願膚積網選製醖願糧 醖選築簾襯獵淵艱餘夢 (襯築積鏇積願鹹艱膚構, 0.157) 更多 | - | 2023-02-27 | ||
(Ripasudil Hydrochloride Hydrate Ophthalmic Solution 0.4%) | 鑰憲構鏇觸鏇簾齋憲蓋(襯齋顧醖糧蓋積構範餘) = 鑰醖簾鬱顧糧膚襯簾選 醖選築簾襯獵淵艱餘夢 (襯築積鏇積願鹹艱膚構, 0.155) 更多 | ||||||
临床2/3期 | 19 | (Netarsudil) | 齋憲製鑰憲願築構選壓(餘築衊鹹廠願製壓製醖) = 簾範繭築齋壓衊獵獵積 艱製憲願艱選遞鑰夢艱 (蓋鹹選夢窪蓋膚積範構, 45) 更多 | - | 2023-02-06 | ||
Placebo (Placebo) | 齋憲製鑰憲願築構選壓(餘築衊鹹廠願製壓製醖) = 憲蓋憲憲醖鏇遞夢願夢 艱製憲願艱選遞鑰夢艱 (蓋鹹選夢窪蓋膚積範構, 49) 更多 | ||||||
临床2期 | 40 | (QD) | 壓鹹構網襯製鹽膚選蓋(鹹顧鑰範艱醖膚憲艱窪) = 鬱願觸鹹選網鬱遞築製 選積壓選觸願構蓋觸壓 (獵築構願願積蓋夢醖夢, 7.99) 更多 | 积极 | 2022-11-03 | ||
(BID) | 壓鹹構網襯製鹽膚選蓋(鹹顧鑰範艱醖膚憲艱窪) = 範蓋範齋觸築構蓋憲觸 選積壓選觸願構蓋觸壓 (獵築構願願積蓋夢醖夢, 8.75) 更多 | ||||||
临床2期 | 40 | (Once Daily Netarsudil Ophthalmic Solution) | 壓艱簾鏇艱鬱選憲繭夢(鹽鏇選顧遞製醖鹽選願) = 鬱淵觸鑰窪選壓齋蓋齋 鹽獵衊獵顧鬱顧鏇廠淵 (鹽願餘醖簾遞鹹衊構範, 35.72) 更多 | - | 2022-09-01 | ||
(Twice Daily Netarsudil Ophthalmic Solution) | 壓艱簾鏇艱鬱選憲繭夢(鹽鏇選顧遞製醖鹽選願) = 齋簾鏇製製顧鏇製衊窪 鹽獵衊獵顧鬱顧鏇廠淵 (鹽願餘醖簾遞鹹衊構範, 39.12) 更多 | ||||||
N/A | 29 | 顧淵鹹襯蓋壓遞艱網觸(憲顧築糧繭憲選醖襯遞) = 廠蓋簾膚觸獵積獵鹹膚 窪觸繭壓簾憲窪願襯蓋 (襯築製壓襯願顧範選醖, 4.80) | 积极 | 2021-11-13 |
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