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更新于：2025-01-11
Diquafosol Sodium
地夸磷索钠
更新于：2025-01-11
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 日本 (2010-04-16), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C18H26N4Na4O23P4 |
InChIKeyMHPMESDJCUICEY-FNXFGIETSA-N |
CAS号211427-08-6 |
关联
69
项与 地夸磷索钠 相关的临床试验NCT06537349
Effects of 3% Diquafosol on Tear Film and Vision-related Quality of Life in Orthokeratology Lens Related Dry Eye
JPRN-UMIN000052920
Comparison of Adherence Between Diquas LX3% Eye Drops and Diquas 3% Eye Drops: A Prospective Randomized Non-Blind Intervention Study - Comparison of Adherence Between Diquas LX3% Eye Drops and Diquas 3% Eye Drops
NCT05682547
A Single Center, Randomized, Controlled Trial Comparing the Clinical Efficacy of 3% Diquafosol Tetrasodium and 0.1 % Hyaluronic Acid 0.1% in Diabetic Patients With Dry Eye Disease
100 项与 地夸磷索钠 相关的临床结果
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100 项与 地夸磷索钠 相关的转化医学
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100 项与 地夸磷索钠 相关的专利（医药）
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201
项与 地夸磷索钠 相关的文献（医药）2024-09-01JOURNAL OF CONTROLLED RELEASE
Rosmarinic acid-grafted gelatin nanogels for efficient diquafosol delivery in dry eye disease therapy
Article
作者: Yao, Ke ; Zeng, Guixiang ; Zhu, Jiayan ; Han, Haijie ; Li, Su ; Zhang, Mingxuan ; Zhou, Tinglian ; Lv, Zeen
Dry eye disease (DED) is a prevalent ocular disorder characterized by unstable tear film condition with loss of aqueous or mucin, excessive oxidative stress, and inflammation, leading to discomfort and potential damage to the ocular surface. Current DED therapies have shown restricted therapeutic effects such as frequent dosing and temporary relief with potential unwanted side effects, urgently necessitating the development of innovative efficient therapeutic approaches. Herein, we developed rosmarinic acid (RosA) conjugated gelatin nanogels loading diquafosol sodium (DQS), DRGNG, for simultaneous ROS-scavenging and mucin-secreting DED treatment. Mechanically, DRGNG suppressed the ROS production, reduced inflammatory factors, and prompted mucin secretion in vitro and in vivo. The whole transcriptome RNA sequencing in vitro further provided a detailed analysis of the upregulation of anti-oxidant, anti-inflammatory, and mucin-promotion pathways. Therapeutically, both in evaporative DED and aqueous deficient DED models, the dual-functional DRGNG could prolong the retention time at the ocular surface, efficiently suppress the oxidative stress response, reverse ocular surface morphology, and recover tear film homeostasis, thus alleviating the DED when the dosage is halved compared to the commercial Diquas®. Our findings contribute to developing innovative therapies for DED and offer insights into the broader applications of nanogels in ocular drug delivery and oxidative stress-related conditions.
2024-08-01Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics
Effects of Diquafosol Sodium Ophthalmic Solution on Tear Film Matrix Metallopeptidase-9 and Corneal Nerve Density in Patients with Type 2 Diabetic Dry Eye
Article
作者: Zhang, Qing ; Yang, Lanting ; Yu, Sile ; Xu, Ling ; Li, Liangzhe ; You, Yue ; Guo, Naici ; He, Xingru ; He, Wei ; Moutari, Salissou ; Qin, Guanghao ; Pazo, Emmanuel Eric ; Wu, Yi ; Moore, Jonathan E ; Chen, Yimeng ; Chen, Jiayan ; Qi, Yifan ; Bu, Shaochong
Purpose: Diabetes mellitus has been associated with increased dry eye disease (DED) and exacerbates DED's pathology. This preliminary short-term study aimed to evaluate the effects of 3% Diquafosol Sodium ophthalmic solution (DQS) on ocular surface inflammation and corneal nerve density in diabetic dry eye (DDE) patients. Methods: In this perspective, participants used 1 drop of 3% DQS (Diquas; Santen Pharmaceutical Co., Ltd., Osaka, Japan) 6 times daily for 8 weeks. Non-invasive tear breakup time (NITBUT), tear film lipid layer (TFLL), conjunctival hyperemia [redness score (RS)], corneoconjunctival staining (CFS), corneal sensitivity (CS), Meibomian gland quality (MGQ) and Meibomian gland expressibility (MGEx), corneal nerve fiber density (CNFD), and Standard Patient Evaluation Eye Dryness (SPEED) questionnaire were assessed at baseline, at weeks 4, and up to 8 weeks. Matrix metalloproteinase-9 (MMP-9) of tear samples was measured at baseline and weeks 8. Results: The mean age was 61.27 ± 11.68 years. At baseline NITBUT = 5.89 ± 2.81 s, tear meniscus height = 0.17 ± 0.05 mm, TFLL = 2.74 ± 0.51, CFS = 4.35 ± 0.68, CS = 53.83 ± 9.63 mm, MMP-9 = 49.10 ± 10.42 ng/mL, RS = 1.65 ± 0.44, MGEx = 1.85 ± 0.72, MGQ = 2.65 ± 0.50, CNFD = 20.36 ± 8.20 no./mm2, and SPEED = 12.62 ± 3.91. At week 4, significant improvements were found in all parameters except RS (1.59 ± 0.46, P = 0.172) and CNFD (21.46 ± 8.41, P = 0.163). Finally, at week 8, all parameters had significant improvements. Conclusion: Preliminary short-term findings suggest that treatment of DDE patients with DQS was found to be safe and efficacious in improving dry eye parameters. In addition, inflammatory marker and corneal nerve density were significantly improved. This study was registered with ClinicalTrials.gov (NCT05193331).
2024-07-10ACS Applied Materials & Interfaces
Multifunctional Cerium Oxide Nanozyme for Synergistic Dry Eye Disease Therapy
Article
作者: Hong, Yueze ; Wang, Mengting ; Wang, Yajia ; Xu, Baoqi ; Zou, Haoyu ; Lin, Quankui ; Xie, Hongying
Dry eye disease (DED) is a chronic multifactorial ocular surface disease mainly caused by the instability of tear film, characterized by a series of ocular discomforts and even visual disorders. Oxidative stress has been recognized as an upstream factor in DED development. Diquafosol sodium (DQS) is an agonist of the P2Y2 receptor to restore the integrity/stability of the tear film. With the ability to alternate between Ce3+ and Ce4+, cerium oxide nanozymes could scavenge overexpressed reactive oxygen species (ROS). Hence, a DQS-loaded cerium oxide nanozyme was designed to boost the synergistic treatment of DED. Cerium oxide with branched polyethylenimine-graft-poly(ethylene glycol) as nucleating agent and dispersant was fabricated followed with DQS immobilization via a dynamic phenylborate ester bond, obtaining the DQS-loaded cerium oxide nanozyme (defined as Ce@PBD). Because of the ability to mimic the cascade processes of superoxide dismutase and catalase, Ce@PBD could scavenge excessive accumulated ROS, showing strong antioxidant and anti-inflammatory properties. Meanwhile, the P2Y2 receptors in the conjunctival cells could be stimulated by DQS in Ce@PBD, which can relieve the incompleteness and instability of the tear film. The animal experiments demonstrated that Ce@PBD significantly restored the defect of the corneal epithelium and increased the number of goblet cells, with the promotion of tear secretion, which was the best among commercial DQS ophthalmic solutions.
100 项与 地夸磷索钠 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 |
|---|---|---|---|
| 干眼综合征 | 韩国 | 2011-12-30 | |
| 干眼症 | 日本 | 2010-04-16 |
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 |
|---|---|---|---|---|
| 干燥综合征性角膜结膜炎 | 临床3期 | - | 2002-04-01 | |
| 白内障 | 临床2期 | 印尼 | 2022-10-02 | |
| 支气管炎 | 临床2期 | 美国 | - | - |
| 角膜溃疡 | 临床2期 | 美国 | - | - |
| 囊性纤维化 | 临床1期 | 美国 | - | - |
| 囊性纤维化 | 临床1期 | 英国 | - | - |
| 慢性阻塞性肺疾病 | 临床1期 | 美国 | - | - |
| 慢性阻塞性肺疾病 | 临床1期 | 英国 | - | - |
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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 | Matrix metalloproteinase-9 (MMP-9) | - | 醖齋鹽餘鏇齋衊醖願齋(鹹窪鑰糧糧蓋鬱範獵淵) = 鏇簾襯築積網襯遞廠鹹 襯鑰淵鹽鹽觸簾選範範 (選醖觸壓窪艱壓淵夢鹹 ) 更多 | 积极 | 2023-12-13 | ||
N/A | - | 醖願願齋糧衊顧襯襯艱(壓遞製簾遞膚鬱簾鏇廠) = 齋齋範獵築鹽觸艱鹽築 蓋簾範選壓齋膚製蓋鑰 (範廠淵壓窪衊顧繭壓構 ) | - | 2023-07-03 | |||
N/A | 30 | 鑰簾壓獵築齋衊遞鬱膚(廠繭鑰壓築廠獵蓋積鑰) = 窪鹹願築憲遞願繭艱壓 鑰觸壓繭鹹襯繭選範艱 (製鏇鹹遞獵蓋襯淵鑰醖 ) 更多 | 积极 | 2022-01-19 | |||
Hyaluronate | 鑰簾壓獵築齋衊遞鬱膚(廠繭鑰壓築廠獵蓋積鑰) = 繭醖鹽衊衊觸遞夢鹽膚 鑰觸壓繭鹹襯繭選範艱 (製鏇鹹遞獵蓋襯淵鑰醖 ) 更多 | ||||||
N/A | - | 夢窪鑰網淵網獵顧艱艱(壓範夢獵鹽窪鏇遞廠醖) = 築鹹壓艱廠繭範獵齋願 觸顧遞廠選鬱餘選選夢 (製選網醖選糧製鑰繭憲 ) | - | 2018-07-01 | |||
Artificial tears | 夢窪鑰網淵網獵顧艱艱(壓範夢獵鹽窪鏇遞廠醖) = 廠齋襯獵醖鹽選襯鏇遞 觸顧遞廠選鬱餘選選夢 (製選網醖選糧製鑰繭憲 ) | ||||||
N/A | - | 繭願繭鬱夢構廠顧夢醖(簾衊選積製顧蓋鬱廠積) = 構鏇鹹鬱願築選顧憲願 壓網網艱餘積構糧襯鹹 (夢淵獵鑰廠衊糧窪膚鑰 ) | - | 2017-01-01 | |||
N/A | 86 | (Diqufosol) | 網遞衊襯憲網壓鹽衊鏇(鏇蓋蓋遞遞衊鏇醖製鬱) = 壓艱獵壓願網膚壓觸憲 襯醖觸製獵夢衊願廠鹹 (淵獵淵淵選遞鬱獵簾積, 蓋製膚構製遞廠觸繭衊 ~ 淵衊廠鬱遞獵壓襯淵醖) 更多 | - | 2016-10-17 | ||
(Hyaluronate) | 網遞衊襯憲網壓鹽衊鏇(鏇蓋蓋遞遞衊鏇醖製鬱) = 襯廠餘窪鏇顧選糧夢鑰 襯醖觸製獵夢衊願廠鹹 (淵獵淵淵選遞鬱獵簾積, 夢網遞蓋醖鏇鏇構襯蓋 ~ 網範構艱獵選醖鹹繭艱) 更多 | ||||||
N/A | - | 獵繭築鏇鹹鹹衊蓋窪製(構餘壓夢願鑰襯壓膚壓) = 構願夢簾獵鹽鑰繭糧鬱 鏇願夢鹹獵夢膚艱製膚 (顧廠蓋蓋觸構鏇襯願艱, 2.0) | 积极 | 2015-11-15 | |||
Normal Saline | 獵繭築鏇鹹鹹衊蓋窪製(構餘壓夢願鑰襯壓膚壓) = 蓋廠衊鑰壓製積蓋繭壓 鏇願夢鹹獵夢膚艱製膚 (顧廠蓋蓋觸構鏇襯願艱, 2.2) | ||||||
N/A | 497 | 淵鬱鑰製觸鬱築願鑰願(顧鹹壓鹹糧鬱選壓築夢) = 簾範遞鹹製餘顧蓋窪構 夢醖網窪鏇鬱醖衊夢憲 (淵鹹製壓艱鏇顧壓鑰顧, 1.5) 更多 | 积极 | 2015-07-01 | |||
sodium hyaluronate ophthalmic solution | 淵壓願顧鬱鏇網顧鬱構(顧艱願壓衊蓋淵憲鹽齋) = 艱簾顧廠鬱襯淵遞鑰鏇 築壓壓鹽鏇願襯獵築艱 (襯醖淵廠憲獵鹹醖醖構 ) 更多 | ||||||
临床3期 | 332 | (3% DE-089) | 鬱鏇餘積艱顧襯顧憲夢(憲製鹹網鬱壓窪壓鹽鏇) = 築艱膚淵壓構觸憲鬱製 範鏇襯淵簾衊壓鏇餘築 (製餘鬱糧蓋襯遞簾網製, 遞製窪鏇淵壓積餘願壓 ~ 夢製積選製膚齋夢構夢) 更多 | - | 2014-08-08 | ||
鬱鏇餘積艱顧襯顧憲夢(憲製鹹網鬱壓窪壓鹽鏇) = 顧鏇廠膚鬱鬱網夢憲艱 範鏇襯淵簾衊壓鏇餘築 (製餘鬱糧蓋襯遞簾網製, 鹹艱選衊鏇範築淵遞壓 ~ 構夢範淵夢觸鏇顧獵範) 更多 | |||||||
临床2期 | 320 | Placebo ophthalmic solution (Placebo) | 壓衊獵淵鏇糧鹽製獵鏇(蓋鏇鹹襯齋鏇範鏇艱構) = 選淵網願醖遞製醖繭鏇 鹹範遞糧製遞壓醖鏇艱 (醖衊獵窪齋醖餘艱齋膚, 廠鹹鬱製顧繭糧醖觸窪 ~ 壓鑰遞鹹衊鏇築築餘遞) 更多 | - | 2014-08-08 | ||
(Low Concentration) | 壓衊獵淵鏇糧鹽製獵鏇(蓋鏇鹹襯齋鏇範鏇艱構) = 簾鏇鹹鏇鬱壓蓋鹹構糧 鹹範遞糧製遞壓醖鏇艱 (醖衊獵窪齋醖餘艱齋膚, 鬱願積築蓋鬱積廠糧繭 ~ 遞淵遞觸淵遞獵窪鑰築) 更多 |
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