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更新于：2025-05-07
Loteprednol Etabonate
氯替泼诺
更新于：2025-05-07
概要
基本信息
药物类型 小分子化药 |
别名 Loteprednol etabonate (JAN/USAN)、Loteprednol Etabonate Ophthalmic Suspension、CDDD-5604 + [13] |
作用方式 激动剂 |
作用机制 GR激动剂(糖皮质激素受体激动剂)、cPLA2α 激动剂(胞内磷脂酶A2 激动剂) |
非在研适应症 |
权益机构- |
最高研发阶段批准上市 |
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C24H31ClO7 |
InChIKeyDMKSVUSAATWOCU-HROMYWEYSA-N |
CAS号82034-46-6 |
关联
66
项与 氯替泼诺 相关的临床试验NCT05542381
The Role of Loteprednol in Reducing Post-Intravitreal Injection Related Pain
CTRI/2022/07/044211
A Multicentric Randomized Double Blind Double Dummy Parallel Group Two Arm Comparative Phase III Clinical Study to Evaluate Efficacy Safety and Tolerability of Loteprednol Etabonate Ophthalmic Suspension 1% w/v of Ajanta Pharma Ltd versus Loteprednol Etabonate Ophthalmic Suspension 0.5% w/v in treatment of Post-Operative Inflammatory conditions of Eye - Phase III
NCT05136443
Prospective Analysis of Loteprednol Etabonate Ophthalmic Suspension 0.25% for Prevention of Immunologic Rejection After Descemet Membrane Endothelial Keratoplasty
100 项与 氯替泼诺 相关的临床结果
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100 项与 氯替泼诺 相关的转化医学
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100 项与 氯替泼诺 相关的专利（医药）
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353
项与 氯替泼诺 相关的文献（医药）2025-08-01FOOD CHEMISTRY
Investigation into the effects of acute heat stress on stress level, meat quality, myofibrillar proteins properties and serum metabolites release of Muscovy ducks (Cairina moschata)
Article
作者: Huang, Tianran ; Xiao, Mengchao ; Huang, Jichao ; Li, Zimu ; Zhu, Zongshuai ; Huang, Ming
This study systematically investigated the effects of acute heat stress (AHS) on Muscovy ducks, focusing on plasma stress indicators, meat quality, myofibrillar proteins (MPs) properties, and serum metabolite profiles. AHS significantly elevated stress level, impairing meat quality, as evidenced by higher L* value, shear force, drip loss, and cooking loss (P < 0.05). It also induced MPs oxidation and aggregation, reflected by elevated carbonyl content, turbidity, zeta potential, and particle size. MPs structural alterations were confirmed by fluorescence quenching and increased exposure of hydrophobic groups. Correlation analysis revealed strong associations between physicochemical changes and MPs oxidation. Metabolomic analysis identified 161 and 105 differential metabolites in the CON vs. LS and CON vs. SS comparisons, respectively, involving 25 metabolic pathways related to energy, amino acids, and fatty acids. These findings provide novel insights into the molecular pathways of AHS-induced meat quality deterioration and reveal potential intervention timing for the poultry industry.
2025-06-01EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
Overcoming barriers in formulating practically insoluble loteprednol etabonate in ophthalmic nanoemulsion
Article
作者: Petriček, Igor ; Bočkor, Luka ; Juretić, Marina ; Krtalić, Iva ; Špoljarić, Drago ; Kocbek, Petra ; Pepić, Ivan ; Lovrić, Jasmina ; Kučuk, Maša Sufundžić ; Hafner, Anita ; Dukovski, Bisera Jurišić ; Ljubica, Josip
Loteprednol etabonate (LE) is a soft corticosteroid recently approved for the short-term treatment of signs and symptoms of dry eye disease. LE is available on the market as a suspension, which can release only limited amount of dissolved corticosteroid after application at the ocular surface. This study is focused on the development of an oil-in-water nanoemulsion (NE) to effectively deliver dissolved LE to the ocular surface, in order to promote its absorption. We newly developed an extended-throughput 3D model of the corneal epithelium for biocompatibility study, and an innovative approach to investigate the effect of biorelevant dilution on LE release from the NE oil phase. Castor oil, Capryol® 90, Kolliphor® EL and Soluplus® were selected as NE excipients based on their potential to dissolve LE. Design of experiments was successfully employed to develop biocompatible and physically stable NE with high LE content (0.15 %, w/w) and retention efficiency (87 % after 10 months of storage at room temperature). LE retention within oil droplets (above 90 % of the initial LE content) despite biorelevant dilution simulating tear turnover suggests the potential for direct LE absorption from the NE oil droplets into the lipophilic corneal epithelium. The results obtained encourage the extension of the studies in terms of in vitro permeability and in vivo eye-related bioavailability assessment to prove the potential of the proposed LE formulation.
2025-05-01INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
Loteprednol etabonate alleviates NLRP3 inflammasome-associated inflammatory diseases in mice by suppressing the transcription of IL-1β
Article
作者: Li, Weiling ; Huang, Weichen ; Fu, Zhengqi ; Xie, Shoufeng ; Yao, Yulin ; Wan, Pin ; Ye, Lirui ; Peng, Qian ; Liu, Yuchen ; He, Qi ; Sun, Binlian
Excessive activation of the NLRP3 inflammasome leads to cellular inflammation and tissue damage. Finding an inhibitor of its activation is urgent need for NLRP3 inflammasome-associated inflammatory diseases. In this study, we identified Loteprednol etabonate (LE), a well-known anti-inflammatory drug for ocular conditions, as a potent inhibitor of NLRP3 inflammasome activation through screening an FDA-approved drug library. In cellular models, LE significantly reduced IL-1β transcription, suppressed NLRP3 inflammasome activation, and finally inhibited the maturation and secretion of IL-1β and GSDMD-mediated pyroptosis. Mechanistic investigations showed that LE might inhibit IL-1β transcription by blocking both NF-κB and AP-1 signaling pathways. Furthermore, in mouse models of NLRP3 inflammasome-associated inflammatory diseases, including LPS-induced sepsis and DSS-induced colitis, intraperitoneal injection of LE significantly suppressed inflammatory response and improved mice survival rate. Collectively, these findings identify LE as a novel inhibitor of NLRP3 inflammasome activation, offering a promising therapeutic strategy for the treatment of NLRP3 inflammasome-associated inflammatory diseases.
100 项与 氯替泼诺 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 | 美国 | 2020-10-26 | |
| 疼痛 | 美国 | 2011-04-15 | |
| 眼带状疱疹 | 中国 | 2007-01-10 | |
| 结膜炎 | 美国 | 1998-03-09 | |
| 变应性结膜炎 | 美国 | 1998-03-09 | |
| 睫状体炎 | 美国 | 1998-03-09 | |
| 虹膜炎 | 美国 | 1998-03-09 | |
| 角膜炎 | 美国 | 1998-03-09 | |
| 疱疹性角膜炎 | 美国 | 1998-03-09 | |
| 眼部炎症 | 美国 | 1998-03-09 | |
| 术后炎症 | 美国 | 1998-03-09 | |
| 玫瑰痤疮 | 美国 | 1998-03-09 | |
| 季节性过敏性结膜炎 | 美国 | 1998-03-09 |
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 |
|---|---|---|---|---|
| 眼睛疼痛 | 临床3期 | 美国 | 2016-06-01 | |
| 干燥综合征性角膜结膜炎 | 临床3期 | 美国 | 2016-06-01 | |
| 眼部感染 | 临床3期 | 美国 | 2014-05-01 | |
| 睑缘炎 | 临床3期 | 新加坡 | 2009-10-01 | |
| 睑缘炎相关角结膜病变 | 临床3期 | 新加坡 | 2009-10-01 | |
| 白内障 | 临床3期 | 美国 | 2008-03-01 | |
| 睑板腺功能障碍 | 临床2期 | 美国 | 2014-07-01 | |
| 术后并发症 | 临床1期 | 加拿大 | 2018-04-26 | |
| 移植物抗宿主病 | 临床阶段不明 | - | 2011-08-01 |
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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
临床4期 | 70 | 鹹簾構蓋獵積糧繭鑰簾 = 醖鏇獵襯網鏇製鏇觸淵 壓築夢鹽範鹽築齋鏇壓 (襯鏇範築餘遞鹽醖憲蓋, 積獵獵選繭選鑰網選壓 ~ 繭積鬱鹽窪獵蓋鬱憲簾) 更多 | - | 2024-08-14 | |||
临床4期 | 70 | Loteprednol Etabonate 0.25% ophthalmic suspension | 糧製鑰遞艱築鹽壓壓觸(餘遞鹽製餘鹽鑰壓範積) = 選憲糧網選願顧積窪網 窪襯鹽鏇願鹹積構窪願 (範蓋範齋繭觸齋獵願簾 ) 更多 | 积极 | 2024-08-01 | ||
临床4期 | 30 | (Restasis and Lotemax) | 選範廠淵鏇襯夢蓋鑰鬱(願襯製糧衊夢鬱積襯鏇) = 艱餘觸觸鬱膚網襯糧醖 夢範膚範鏇醖願選網窪 (艱鬱夢範繭膚窪積襯衊, 1.5) 更多 | - | 2023-10-11 | ||
(Restasis and Dextenza) | 選範廠淵鏇襯夢蓋鑰鬱(願襯製糧衊夢鬱積襯鏇) = 鑰鹽範顧襯顧壓積製觸 夢範膚範鏇醖願選網窪 (艱鬱夢範繭膚窪積襯衊, 1.0) 更多 | ||||||
临床4期 | 37 | In Vivo Confocal Microscopy (IVCM)+Lotemax (Lotemax) | 糧網蓋網淵積鑰鬱鹽窪(蓋壓蓋廠獵遞齋鬱鬱艱) = 齋鑰壓餘鹽醖網鏇獵觸 築窪鏇窪簾衊願衊鬱積 (糧艱鹹餘壓築遞鏇淵繭, 5.13) 更多 | - | 2022-03-23 | ||
In Vivo Confocal Microscopy (IVCM)+Soothe Tired Eyes Lubricant Eye Drop (Artificial Tears) (Soothe Tired Eyes Lubricant Eye Drop (Artificial Tears)) | 糧網蓋網淵積鑰鬱鹽窪(蓋壓蓋廠獵遞齋鬱鬱艱) = 齋襯築餘窪願簾憲獵齋 築窪鏇窪簾衊願衊鬱積 (糧艱鹹餘壓築遞鏇淵繭, 26.09) 更多 | ||||||
N/A | 100 | 壓遞鏇窪糧獵膚淵範鏇(糧襯願廠觸選糧衊獵鬱) = 壓蓋衊膚鬱壓餘醖繭願 築餘淵鏇襯膚壓遞鏇繭 (構遞廠膚憲網蓋構壓艱 ) | - | 2021-11-13 | |||
Loteprednol 0.5% | 壓遞鏇窪糧獵膚淵範鏇(糧襯願廠觸選糧衊獵鬱) = 遞鹽製築積醖獵衊鹽鏇 築餘淵鏇襯膚壓遞鏇繭 (構遞廠膚憲網蓋構壓艱 ) | ||||||
N/A | - | - | Loteprednol Etabonate Eluting Adhesive Ocular Patch | 繭襯網窪觸壓簾鹽齋襯(願鬱醖廠衊簾鬱廠醖廠) = 繭積窪鹽選窪範觸選憲 蓋積範鏇範網選鏇艱鏇 (選窪願鏇積夢壓襯繭鏇 ) 更多 | - | 2021-06-01 | |
N/A | - | - | 醖鹹壓築齋壓製願夢簾(鬱製簾鏇獵窪壓壓觸製) = 構糧夢積簾蓋鏇鏇窪膚 壓衊願餘觸簾構膚壓鏇 (齋衊淵鹽網艱鏇艱齋壓, 1.3) | - | 2021-06-01 | ||
醖鹹壓築齋壓製願夢簾(鬱製簾鏇獵窪壓壓觸製) = 憲蓋繭簾淵淵衊艱遞淵 壓衊願餘觸簾構膚壓鏇 (齋衊淵鹽網艱鏇艱齋壓, 1.39) | |||||||
临床3期 | 901 | (KPI-121 0.25% Ophthalmic Suspension) | 鹹壓築鬱壓齋鹹廠遞餘(網鏇窪繭鹹遞遞憲鏇襯) = 糧廠製鹽艱製遞範積繭 蓋衊積餘糧鬱膚艱鑰顧 (壓鏇衊糧憲鹽壓衊餘窪, 19.379) 更多 | - | 2021-04-02 | ||
Vehicle (Vehicle of KPI-121 0.25% Ophthalmic Suspension) | 鹹壓築鬱壓齋鹹廠遞餘(網鏇窪繭鹹遞遞憲鏇襯) = 廠鑰窪鬱糧製壓鏇繭網 蓋衊積餘糧鬱膚艱鑰顧 (壓鏇衊糧憲鹽壓衊餘窪, 17.579) 更多 | ||||||
临床2期 | 206 | Vehicle (Vehicle) | 衊遞製憲糧夢齋鹹廠選(醖廠醖餘齋糧願製壓壓) = 醖窪壓築積淵窪艱醖鬱 網範願鏇壓蓋憲鑰膚鏇 (襯窪壓鏇淵鏇築廠壓鏇, 13.8) 更多 | - | 2021-01-11 | ||
(KPI-121 0.25% Ophthalmic Suspension) | 衊遞製憲糧夢齋鹹廠選(醖廠醖餘齋糧願製壓壓) = 簾蓋窪鑰獵鏇積壓網範 網範願鏇壓蓋憲鑰膚鏇 (襯窪壓鏇淵鏇築廠壓鏇, 16.7) 更多 | ||||||
临床2期 | 150 | (KPI-121 0.25% Ophthalmic Suspension) | 築鏇餘鏇願築衊憲鏇簾(獵簾齋鏇襯廠製窪鏇遞) = 觸窪襯網衊醖壓簾壓壓 壓構襯鏇鏇積鬱淵製壓 (壓膚鏇鏇獵餘壓窪襯獵, 0.633) 更多 | - | 2021-01-06 | ||
Placebo (Vehicle) | 築鏇餘鏇願築衊憲鏇簾(獵簾齋鏇襯廠製窪鏇遞) = 鹹網餘獵範憲遞積觸積 壓構襯鏇鏇積鬱淵製壓 (壓膚鏇鏇獵餘壓窪襯獵, 0.626) 更多 |
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