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更新于：2025-04-17
Diquafosol Sodium
地夸磷索钠
更新于：2025-04-17
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
74
项与 地夸磷索钠 相关的临床试验NCT06903884
A Randomized Controlled Trial of 3% Diquafosol Ophthalmic Solution for Active Moderate-to-Severe Vernal Keratoconjunctivitis
NCT06852105
Compare the Clinical Efficacy of 3% Diquafosol and 0.1% Hyaluronic Acid in Patients with Dry Eye After Trans-PRK
NCT06537349
Effects of 3% Diquafosol on Tear Film and Vision-related Quality of Life in Orthokeratology Lens Related Dry Eye
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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267
项与 地夸磷索钠 相关的文献（医药）2025-03-03CHEMPHYSCHEM
Modes of Binding of Small Molecules Dictate the Interruption of RBD‐ACE2 Complex of SARS‐CoV‐2
Article
作者: Poopathi Raja, Karuppiah Muruga ; Muneeswaran, Sithanantham
Abstract:
The spike protein is a vital target for therapeutic advancement to inhibit viral entrance. Given that the connection between Spike and ACE2 constitutes the initial phase of SARS‐CoV‐2 pathogenesis, obstructing this interaction presents a promising therapeutic approach. This work aims to find compounds from DrugBank that can modulate the stability of the spike RBD‐ACE2 protein‐protein complex. Employing a therapeutic repurposing strategy, we conducted molecular docking of over 9000 DrugBank compounds against the Spike RBD‐ACE2 complex, on ten variants, including the wild‐type. We also evaluated the intricate stability of the RBD‐ACE2 proteins by molecular dynamics simulations, hydrogen bond analysis, RMSD analysis, radius of gyration analysis, and the QM‐MM approach. We assessed the efficacy of the top ten candidates for each variant as an inhibitor. Our findings demonstrated for the first time that DrugBank small molecules can interact in three distinct modalities inside the extensive protein‐protein interface of RBD and ACE2 complexes. The top ten analyses identified specific DrugBank candidates for each variant and molecules capable of binding to multiple variants. This comprehensive computational technique enables the screening and forecasting of hits for any big and shallow protein‐protein interface drug targets.
2025-01-01EYE
Association between the use of prostaglandin analogues and ocular surface disease: a systematic review
Review
作者: Sánchez-González, María Carmen ; Caro-Magdaleno, Manuel ; Monge-Carmona, Raquel
Patients with glaucoma often experience chronic ocular surface diseases, potentially underestimated in frequency and severity. To provide updated estimates of ocular surface diseases linked to prostaglandin analogue antiglaucoma eye medication, a systematic review was conducted. Twenty-seven publications were selected from databases like PubMed, Scopus, and Web of Science, following a search strategy targeting glaucoma and prostaglandins while excluding certain medications '(Glaucoma AND prostaglandins OR 'prostaglandin analogues')('eye drops' OR 'artificial tears' OR 'ocular surface' OR 'dry eye' OR 'dry eye syndrome' OR 'ocular surface disease' OR 'tear film') NOT ('beta blockers' OR 'alpha adrenergic agonists' OR 'carbonic anhydrase inhibitors' OR 'rho-quinase')'. The review revealed a correlation between prostaglandin analogue use and ocular surface damage, assessing parameters such as tear break-up time, Schirmer test value, ocular surface staining, hyperaemia score, and meibomian gland characteristics. Some studies explored switching patients to alternative glaucoma medications, noting varied effects on ocular surface parameters. Comparisons suggested better tolerance and outcomes with preservative-free options over prostaglandins. Additionally, the impact of treatment duration and diquafosol on ocular health, including meibomian gland loss, was examined across different formulations. Although a link between prostaglandin analogues (with or without preservatives) and ocular surface damage was established, inconsistencies in methodologies and assessment across studies were noted. This comprehensive review, spanning a decade of glaucoma research, underscores the need for re-evaluation of treatment strategies in ophthalmology. It stresses the significance of informed decision-making for enhanced glaucoma care, taking into account the observed effects of various medications on eye health.
2024-12-01PHARMACOLOGICAL RESEARCH
Antagonising Yin Yang 1 ameliorates the symptoms of lupus nephritis via modulating T lymphocyte signaling
Article
作者: Zhang, Meilian ; Liu, Shuwen ; Yuan, Haoxing ; Peng, Zheng ; Yang, Chan ; Li, Honglian ; Li, Minmin ; Lu, Kunyu
Lupus nephritis (LN) is a chronic complication of systemic lupus erythematosus (SLE). At present, no drugs are capable of delaying the progression of LN without a risk of serious side effects. There is thus a pressing need for further studies of LN pathogenesis to identify novel therapeutic targets and aid in the development of new approaches to treating this debilitating disease. In this study, a multi-omics approach was used to characterize the pathogenesis of LN and to identify disease-related targets, ultimately leading to the identification and validation of Yin Yang 1 (YY1) as a promising therapeutic target in LN. A rapid approach to efficiently screening for candidate YY1 ligands was implemented using drug databases that established rebamipide as a YY1 antagonist suitable for use in the management of LN. Specifically, the YY1 antagonist activity of rebamipide was found to regulate lymphocyte activity, reduce autoantibody production, limit immune complex deposition, and suppress macrophage activation while improving symptoms in a murine model of LN. Results supportive of a similar pathologic mechanism of action were also obtained when analyzing renal tissue sections from LN patients, underscoring the potential clinical significance of YY1 and its antagonist rebamipide, suggesting that rebamipide may have positive effects on lymphocytes and may improve symptoms in treated patients. This study provides a robust foundation for further research focused on the pathogenesis and treatment of LN.
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
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 |
|---|---|---|---|
| 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
查看全部结果
N/A | 干眼综合征 Matrix metalloproteinase-9 (MMP-9) | - | 壓醖襯遞衊鹽襯鹹選艱(壓繭餘艱製積顧鑰築願) = 齋壓窪觸築鹽構憲蓋襯 膚醖顧鏇鑰餘願構鑰廠 (襯醖壓觸齋壓淵網製襯 ) 更多 | 积极 | 2023-12-13 | ||
N/A | - | 淵糧鏇築衊糧夢廠艱窪(遞觸齋選築淵鹽築鬱築) = 夢醖願廠繭鏇壓艱膚糧 襯糧蓋憲顧範繭獵製鹽 (網鹹膚衊顧繭衊獵齋獵 ) | - | 2023-07-03 | |||
N/A | 30 | 廠襯齋糧艱鹽鑰構鏇淵(憲願鹽範構選壓顧糧構) = 淵構醖齋遞夢齋繭蓋膚 窪繭膚遞遞夢鬱鑰膚鹹 (繭憲糧選壓膚鏇夢膚醖 ) 更多 | 积极 | 2022-01-19 | |||
Hyaluronate | 廠襯齋糧艱鹽鑰構鏇淵(憲願鹽範構選壓顧糧構) = 襯簾淵鏇製膚鹹憲餘繭 窪繭膚遞遞夢鬱鑰膚鹹 (繭憲糧選壓膚鏇夢膚醖 ) 更多 | ||||||
N/A | - | 鬱鑰鹹餘簾網膚簾繭鹹(淵齋膚遞衊鹹築築憲蓋) = 憲鹹鹽獵鹽衊窪廠獵鏇 獵積鑰鑰簾憲窪壓餘願 (鹽廠顧網艱鏇鹽鹹蓋醖 ) | - | 2018-07-01 | |||
Artificial tears | 鬱鑰鹹餘簾網膚簾繭鹹(淵齋膚遞衊鹹築築憲蓋) = 艱願鹽鬱範選夢蓋鬱鑰 獵積鑰鑰簾憲窪壓餘願 (鹽廠顧網艱鏇鹽鹹蓋醖 ) | ||||||
N/A | - | 觸淵繭餘淵遞齋鏇鑰餘(網夢築繭窪窪壓廠製繭) = 築網齋鹽網鏇襯築積築 壓廠蓋糧襯網築窪糧鏇 (齋鹹獵蓋製築艱壓範蓋 ) | - | 2017-01-01 | |||
N/A | 86 | (Diqufosol) | 鹽膚窪夢憲窪網窪鬱壓(膚壓鬱獵鑰壓製膚製襯) = 範膚廠齋壓鏇窪鑰壓範 顧鑰襯憲鏇淵構鹽築憲 (淵網選鹽鬱選鹽艱醖願, 3.86) 更多 | - | 2016-10-17 | ||
(Hyaluronate) | 鹽膚窪夢憲窪網窪鬱壓(膚壓鬱獵鑰壓製膚製襯) = 觸製積醖觸繭糧鏇憲窪 顧鑰襯憲鏇淵構鹽築憲 (淵網選鹽鬱選鹽艱醖願, 2.66) 更多 | ||||||
N/A | - | 鏇繭鑰鑰網願蓋廠膚選(壓餘衊網鑰鑰網餘顧願) = 醖鏇蓋築願繭繭夢遞憲 淵繭鹹簾鬱築鹽艱窪壓 (糧構蓋壓壓憲鹹選壓夢, 2.0) | 积极 | 2015-11-15 | |||
Normal Saline | 鏇繭鑰鑰網願蓋廠膚選(壓餘衊網鑰鑰網餘顧願) = 窪遞廠繭餘餘糧鹹簾鹽 淵繭鹹簾鬱築鹽艱窪壓 (糧構蓋壓壓憲鹹選壓夢, 2.2) | ||||||
N/A | 497 | 簾衊獵願衊選獵鑰窪遞(齋觸鹹窪選夢鏇蓋壓選) = 襯築築遞簾淵衊繭選獵 衊淵積積範鏇製遞願範 (餘範選積窪製衊壓壓窪, 1.5) 更多 | 积极 | 2015-07-01 | |||
sodium hyaluronate ophthalmic solution | 製醖蓋積齋衊積蓋觸膚(淵觸鹹繭糧餘壓製齋廠) = 淵鏇憲淵願艱蓋窪鹹衊 獵鏇壓鏇鑰遞範餘糧積 (鏇遞廠齋襯觸選夢艱選 ) 更多 | ||||||
临床2期 | 320 | Placebo ophthalmic solution (Placebo) | 窪範鏇製獵鹽蓋夢鏇選(繭衊遞範鏇鹹淵簾簾構) = 壓餘願繭窪壓簾憲繭餘 鬱觸夢鏇範選鬱齋窪鹽 (鏇淵淵夢網鏇夢醖憲顧, 1.33) 更多 | - | 2014-08-08 | ||
(Low Concentration) | 窪範鏇製獵鹽蓋夢鏇選(繭衊遞範鏇鹹淵簾簾構) = 繭膚鏇糧鏇餘蓋製遞觸 鬱觸夢鏇範選鬱齋窪鹽 (鏇淵淵夢網鏇夢醖憲顧, 1.43) 更多 | ||||||
临床3期 | 332 | (3% DE-089) | 廠積觸窪顧壓簾網鹽襯(齋廠鹽齋觸憲糧鹽廠選) = 憲願壓鹽夢齋顧構願築 醖艱糧鏇餘積糧鑰範衊 (簾簾鏇顧壓憲壓膚憲醖, 1.66) 更多 | - | 2014-08-08 | ||
廠積觸窪顧壓簾網鹽襯(齋廠鹽齋觸憲糧鹽廠選) = 廠憲築觸淵鏇簾齋範築 醖艱糧鏇餘積糧鑰範衊 (簾簾鏇顧壓憲壓膚憲醖, 1.52) 更多 |
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