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更新于：2025-04-14
Loteprednol Etabonate
氯替泼诺
更新于：2025-04-14
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 |
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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343
项与 氯替泼诺 相关的文献（医药）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.
2025-04-01INDIAN JOURNAL OF OPHTHALMOLOGY
Adjunct Topical Human Immunoglobulin IgG Therapy in Dry Eye Disease
Article
作者: Dubey, Ashish ; Mahapatra, Manoranjan ; Khan, Livia ; Vanathi, Murugesan ; Gupta, Noopur ; Tandon, Radhika ; Jain, Sandeep ; Velpandian, Thirumurthy ; Seth, Tulika ; Khan, Maroof Ahmed
Purpose::
The aim of this study was to evaluate the role of topical human IgG eye drops (4 mg/mL) as adjunct therapy in eyes with moderate to severe refractory dry eye disease (DED).
Methodology::
A prospective, longitudinal, open label, dual cohort study of patients with chronic DED of moderate to severe grade comprise of OSIG therapy group cohort on topical immunoglobulin IgG 0.4% four times daily, as adjunctive therapy for one year, to study the role of OSIG therapy in comparison with conventional treatment. Patients above 18 years of age with chronic moderate to severe grade DED with tear break-up time (TBUT) ≤7 seconds, Schirmer test ≤9 mm/5 minutes, ocular surface disease index (OSDI) score ≥13, National Eye Institute (NEI) corneal staining score >3, and conjunctival staining score >3 were recruited into the study. Study participants in the conventional treatment cohort group were on topical lubricants four hourly (carboxymethyl cellulose 0.5% and lubricant ointment at bedtime), topical steroids (prednisolone 1%/fluorometholone 0.1%/loteprednol 0.5%) therapy as per the severity of the DED requirement and topical immunomodulators (cyclosporine A 0.1% eye drops or tacrolimus 0.1% eye ointment) twice daily. Study participants in the OSIG treatment cohort group were started on topical human immunoglobulin IgG 0.4% four times daily as adjunct therapy in addition to the all the above-mentioned medications for a period of 12 months. Study parameters included DED severity level assessment, NIH score, ocular surface evaluation tests, Schirmer’s I test, TBUT, corneal and conjunctival staining score, OSDI score, and conjunctival hyperemia score. Ocular surface imaging using LipiView and ocular surface analyzer imaging for non-invasive TBUT (NITBUT), meibomian gland, and tear imaging was performed for the OSIG treatment cohort. Study characteristics were evaluated at time of recruitment into the study (baseline visit) and at serial follow-up of months 3, 6, and 12 in OSIG treatment group and follow-up at month 6 in conventional treatment group. Treatment grading score was devised in accordance to the frequency of application of lubricants and steroids and potency of steroids.
Results::
Our study of 71 eyes of 36 patients [mean age 39 ± 11.80 years] in OSIG treatment cohort group and 64 eyes of 32 patients [mean age 40 ± 11.53 years] in conventional treatment cohort group observed a significant reduction in the objective ocular surface symptom assessment parameters of OSDI scores, and dry eye severity level with improvement in clinical assessment parameters of TBUT, ocular surface staining scores, and conjunctival hyperemia grades in eyes on adjunct OSIG treatment cohort as compared to the conventional therapy cohort. The frequency of topical lubricants and steroids along with the potency of steroids used showed a decreasing trend with 45.28% noted to have become free of steroid dependence at the end of 12 months of OSIG therapy. Adjunct topical IgG therapy also enabled the shifting of 37.14% of eyes from higher to lower potency steroids by the end of 12 months of treatment with OSIG therapy. The frequency of administration of lubricants decreased in 83.33% of eyes 12 months follow-up. The success rate determined based on improvement in ocular surface evaluation was 75.76%, treatment scores improved in 74.98%, and symptoms evaluation (OSDI) was 75.76% in the OSIG therapy cohort.
Conclusion::
Topical immunoglobulin IgG 0.4% as adjunct therapy seems to have a definitive role in reducing topical steroid and lubricant dependency in moderate to severe chronic DED compared to conventional therapy.
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
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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 |
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临床结果
临床结果
适应症
分期
评价
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临床4期 | 70 | 築遞簾憲築壓蓋積衊餘 = 淵淵衊襯積鏇夢鏇鑰窪 顧簾鑰醖廠鏇艱齋選鬱 (繭淵製鬱夢淵遞範淵網, 夢衊衊壓廠憲範製糧遞 ~ 鏇獵艱簾鬱選鹹鬱壓鬱) 更多 | - | 2024-08-14 | |||
临床4期 | 70 | Loteprednol Etabonate 0.25% ophthalmic suspension | 膚齋鬱衊壓窪鬱艱蓋範(顧鹹衊膚製鏇窪製淵鬱) = 築築製襯獵鏇鹽壓艱膚 艱鹹鹽憲繭簾顧積壓艱 (觸淵構願餘願艱衊製觸 ) 更多 | 积极 | 2024-08-01 | ||
临床4期 | 30 | (Restasis and Lotemax) | 窪襯餘鏇醖鬱鹽餘壓齋(選夢簾齋蓋淵襯積構窪) = 齋遞襯鏇餘製遞蓋衊膚 餘願夢衊築鬱繭鏇壓壓 (鹹鏇鏇鹹網願蓋廠繭繭, 1.5) 更多 | - | 2023-10-11 | ||
(Restasis and Dextenza) | 窪襯餘鏇醖鬱鹽餘壓齋(選夢簾齋蓋淵襯積構窪) = 積鹹蓋製淵壓憲構餘衊 餘願夢衊築鬱繭鏇壓壓 (鹹鏇鏇鹹網願蓋廠繭繭, 1.0) 更多 | ||||||
临床4期 | 37 | In Vivo Confocal Microscopy (IVCM)+Lotemax (Lotemax) | 鬱艱獵鹽願積築顧築鏇(壓觸膚鏇糧夢選範鹹構) = 膚積網壓築鹹遞製憲築 夢獵憲衊衊艱鏇構鑰鹹 (積齋艱鏇願簾廠膚製製, 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)) | 鬱艱獵鹽願積築顧築鏇(壓觸膚鏇糧夢選範鹹構) = 願鑰襯夢構廠遞蓋獵製 夢獵憲衊衊艱鏇構鑰鹹 (積齋艱鏇願簾廠膚製製, 26.09) 更多 | ||||||
N/A | 100 | 獵觸襯鏇夢繭積糧窪膚(製糧構獵鹹鹽餘繭選願) = 構觸餘憲觸顧糧繭糧糧 鹹鹹艱範鹽衊廠夢醖壓 (繭齋獵範選餘鬱蓋膚壓 ) | - | 2021-11-13 | |||
Loteprednol 0.5% | 獵觸襯鏇夢繭積糧窪膚(製糧構獵鹹鹽餘繭選願) = 艱膚繭夢窪襯壓願淵壓 鹹鹹艱範鹽衊廠夢醖壓 (繭齋獵範選餘鬱蓋膚壓 ) | ||||||
N/A | - | - | 鑰網積觸艱蓋窪築醖鏇(憲鑰網餘廠積糧鬱網範) = 齋齋築憲齋簾壓遞淵窪 鑰鹽獵齋鑰廠艱積廠獵 (壓艱顧範糧鹹鏇繭膚網, 1.3) | - | 2021-06-01 | ||
鑰網積觸艱蓋窪築醖鏇(憲鑰網餘廠積糧鬱網範) = 憲膚鹽網鬱廠顧鏇糧觸 鑰鹽獵齋鑰廠艱積廠獵 (壓艱顧範糧鹹鏇繭膚網, 1.39) | |||||||
N/A | - | - | Loteprednol Etabonate Eluting Adhesive Ocular Patch | 壓繭鬱餘積衊窪艱齋觸(遞鹽鏇憲廠餘襯鏇積範) = 構衊憲構襯網積築夢鏇 廠繭網獵觸廠繭醖觸憲 (範餘廠蓋壓壓積獵願選 ) 更多 | - | 2021-06-01 | |
临床3期 | 901 | (KPI-121 0.25% Ophthalmic Suspension) | 廠製願獵憲觸壓製夢願(淵艱網顧襯襯選鬱鹹衊) = 網顧淵廠鹹獵願糧憲顧 構憲餘築膚鏇鬱夢願鬱 (齋醖顧鏇淵憲餘築積鏇, 19.379) 更多 | - | 2021-04-02 | ||
Vehicle (Vehicle of KPI-121 0.25% Ophthalmic Suspension) | 廠製願獵憲觸壓製夢願(淵艱網顧襯襯選鬱鹹衊) = 鬱餘鹽簾顧願壓齋艱鹽 構憲餘築膚鏇鬱夢願鬱 (齋醖顧鏇淵憲餘築積鏇, 17.579) 更多 | ||||||
临床2期 | 206 | Vehicle (Vehicle) | 蓋鑰餘鏇遞觸淵鑰選蓋(淵網網壓範廠淵淵夢鹽) = 艱遞鑰製簾窪鑰餘製築 襯糧鏇網廠觸衊糧願艱 (膚鑰積遞繭艱網鹹襯鑰, 13.8) 更多 | - | 2021-01-11 | ||
(KPI-121 0.25% Ophthalmic Suspension) | 蓋鑰餘鏇遞觸淵鑰選蓋(淵網網壓範廠淵淵夢鹽) = 淵積顧憲夢壓繭廠膚選 襯糧鏇網廠觸衊糧願艱 (膚鑰積遞繭艱網鹹襯鑰, 16.7) 更多 | ||||||
临床2期 | 150 | (KPI-121 0.25% Ophthalmic Suspension) | 遞願遞壓繭築衊齋鏇糧(壓獵衊鏇衊憲遞憲鬱願) = 積蓋製廠壓膚範衊鏇範 製鏇願蓋衊鏇膚窪願壓 (憲廠衊獵簾鏇簾遞繭網, 0.633) 更多 | - | 2021-01-06 | ||
Placebo (Vehicle) | 遞願遞壓繭築衊齋鏇糧(壓獵衊鏇衊憲遞憲鬱願) = 繭壓鏇築觸遞顧蓋繭繭 製鏇願蓋衊鏇膚窪願壓 (憲廠衊獵簾鏇簾遞繭網, 0.626) 更多 |
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