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更新于：2025-08-31
Epinastine Hydrochloride
盐酸依匹斯汀
更新于：2025-08-31
概要
基本信息
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C16H16ClN3 |
InChIKeyVKXSGUIOOQPGAF-UHFFFAOYSA-N |
CAS号108929-04-0 |
关联
50
项与 盐酸依匹斯汀 相关的临床试验CTR20243732
盐酸依匹斯汀片在健康受试者中的单中心、随机、开放、单次给药、两制剂、两序列、两周期、双交叉、空腹及餐后状态下的生物等效性研究
CTR20234212
0.1%STN1011403滴眼液治疗过敏性结膜炎的多中心随机评价者盲态阳性对照试验
CTR20231572
0.05%盐酸依匹斯汀滴眼液治疗中国过敏性结膜炎患者的有效性和安全性的随机、双盲、阳性药平行对照、多中心临床研究
100 项与 盐酸依匹斯汀 相关的临床结果
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100 项与 盐酸依匹斯汀 相关的转化医学
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100 项与 盐酸依匹斯汀 相关的专利（医药）
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255
项与 盐酸依匹斯汀 相关的文献（医药）2025-07-16BIOLOGICAL & PHARMACEUTICAL BULLETIN
Second-Generation H<sub>1</sub>-Receptor Antagonists, Mequitazine, Azelastine and Desloratadine Activate Caspase-8, Caspase-3, and Gasdermin E and Induce Cell Death Showing Pyroptotic-Like Features in Macrophages at Excessively High Concentrations
Article
作者: Ito, Akane ; Nakajima, Mitsunari ; Sawamoto, Atsushi ; Okuyama, Satoshi
Histamine H1 receptor (H1R) is expressed in various cells, including neurons, smooth muscle cells, hepatocytes, T and B cells, neutrophils, dendritic cells, monocytes, and macrophages. Antagonists that target the H1R are used to relieve the symptoms of allergy and inflammation. Here, we examined the inflammation-modulating and cell death-inducing effects of 10 second-generation H1R antagonists on mouse intraperitoneal macrophages, which include ketotifen, mequitazine, azelastine, oxatomide, epinastine, bepotastine, fexofenadine, loratadine, levocetirizine, and desloratadine, to assess an anticipated adverse reaction. Three of these antagonists, namely, mequitazine, azelastine, and desloratadine, induced the secretion of interleukin-1α (IL-1α), a marker of pyroptosis and an inflammatory cytokine, from the macrophages at excessively high concentrations, while reducing the secretion of another inflammatory cytokine, IL-6. We found that the macrophages treated with the 3 antagonists showed pyroptotic-like, but not apoptotic-like, morphology and died. Western blotting analysis revealed that caspase-8, caspase-3, and gasdermin E (GSDME), but not gasdermin D, were cleaved and activated in the macrophages. These results suggest that second-generation H1R antagonists such as mequitazine, azelastine, and desloratadine induce pyroptotic-like cell death accompanied by caspase-8, caspase-3, and GSDME activation in macrophages.
2025-06-26Cureus Journal of Medical Science
Topical Innovation: A Report on Epinastine Eyelid Cream for Patients With Mild Atopic Keratoconjunctivitis
Article
作者: Mimura, Tatsuya ; Fukagawa, Kazumi
Allergic conjunctivitis is a common ocular disorder that significantly impacts patients' quality of life. Conventional treatments, primarily anti-allergic and corticosteroid eye drops, require frequent administration, posing adherence challenges. Poor compliance is a major barrier to effective management, particularly in pediatric and elderly patients. Recently, a novel 0.5% epinastine topical eyelid cream, designed for once-daily application, has been introduced as an alternative treatment. However, no clinical reports for atopic keratoconjunctivitis have assessed its efficacy and safety in real-world practice. This study presents a clinical report on the use of 0.5% epinastine topical eyelid cream in three patients with allergic conjunctivitis and atopic dermatitis, evaluating its therapeutic efficacy, adherence, and tolerability. We examined three cases of allergic conjunctivitis associated with atopic dermatitis treated with once-daily 0.5% epinastine topical eyelid cream. Clinical outcomes were assessed using an allergic conjunctivitis severity score based on objective findings. Adherence and safety were also evaluated. All patients exhibited rapid symptom improvement, with significant reductions in ocular pruritus, conjunctival hyperemia, and eyelid dermatitis. By week four, allergic conjunctivitis severity scores had improved markedly in all cases (from baseline scores of 8-13 to 3-6). No adverse effects or treatment discontinuations were observed. Notably, all patients reported high adherence and ease of use, with reduced reliance on eye drops. This case series provides the clinical evidence supporting the efficacy and tolerability of 0.5% epinastine topical eyelid cream for allergic conjunctivitis, particularly in patients with coexisting atopic dermatitis. The once-daily application may enhance adherence and serve as a viable alternative or adjunct to conventional eye drops. Further large-scale studies are warranted to validate these findings.
2025-06-04Cureus Journal of Medical Science
Efficacy of Topical Epinastine Eyelid Cream for Perennial Allergic Conjunctivitis: A Prospective Study
Article
作者: Kawaguchi, Ayaka ; Fukushima, Atsuki ; Tabuchi, Hitoshi ; Tanabe, Mao ; Tanaka, Hayato
INTRODUCTION:
Antihistamine eye drops are first-line treatments for allergic conjunctivitis; however, patient compliance and ocular itch exacerbation during medication intervals remain challenging. This study investigated the clinical application of 0.5% topical epinastine eyelid cream in patients with symptomatic perennial allergic conjunctivitis already using antihistamine eye drops.
METHODOLOGY:
Fourteen patients with perennial allergic conjunctivitis using antihistamine eye drops were prescribed 0.5% topical epinastine eyelid cream. Patients applied the cream once daily before bedtime. Questionnaires assessed medication compliance, 24-hour ocular itch scores, and daytime quality of life (QOL). Statistical analysis used a mixed-effect model for repeated measures.
RESULTS:
All 14 patients completed the proactive eyelid cream medication. Ocular itch scores significantly decreased from baseline to the next morning (P = 0.003). Daytime QOL scores showed significant changes between baseline and first and second applications (P < 0.001 for both).
CONCLUSIONS:
A 0.5% topical epinastine eyelid cream demonstrates potential as a convenient, once-daily treatment for allergic conjunctivitis, offering consistent symptom control and improved patients' QOL. Further long-term studies are recommended to validate these initial findings.
100 项与 盐酸依匹斯汀 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 |
|---|---|---|---|
| 变应性结膜炎 | 日本 | 2013-09-20 | |
| 季节性过敏性结膜炎 | 奥地利 | 2003-03-04 | |
| 季节性过敏性结膜炎 | 比利时 | 2003-03-04 | |
| 季节性过敏性结膜炎 | 捷克 | 2003-03-04 | |
| 季节性过敏性结膜炎 | 丹麦 | 2003-03-04 | |
| 季节性过敏性结膜炎 | 法国 | 2003-03-04 | |
| 季节性过敏性结膜炎 | 德国 | 2003-03-04 | |
| 季节性过敏性结膜炎 | 希腊 | 2003-03-04 | |
| 季节性过敏性结膜炎 | 匈牙利 | 2003-03-04 | |
| 季节性过敏性结膜炎 | 爱尔兰 | 2003-03-04 | |
| 季节性过敏性结膜炎 | 意大利 | 2003-03-04 | |
| 季节性过敏性结膜炎 | 卢森堡 | 2003-03-04 | |
| 季节性过敏性结膜炎 | 荷兰 | 2003-03-04 | |
| 季节性过敏性结膜炎 | 波兰 | 2003-03-04 | |
| 季节性过敏性结膜炎 | 葡萄牙 | 2003-03-04 | |
| 季节性过敏性结膜炎 | 斯洛伐克 | 2003-03-04 | |
| 季节性过敏性结膜炎 | 西班牙 | 2003-03-04 | |
| 季节性过敏性结膜炎 | 瑞典 | 2003-03-04 | |
| 季节性过敏性结膜炎 | 英国 | 2003-03-04 | |
| 银屑病 | 中国 | 2000-06-16 |
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 |
|---|---|---|---|---|
| 季节性过敏性鼻炎 | 临床3期 | - | 2007-12-18 | |
| 特应性皮炎 | 临床3期 | - | 2001-06-01 | |
| 常年性变应性鼻炎 | 临床3期 | - | 2000-05-01 |
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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
| - | 30 | 範製膚鹽鑰鏇廠製網窪(夢膚製齋鹹積製鹽鹹簾): p = < 0.0001 更多 | 积极 | 2024-09-01 | |||
安慰剂 | |||||||
临床3期 | 87 | (Epinastine (DE-114) Ophthalmic Solution) | 顧蓋憲願構廠觸鬱範鹹(窪艱蓋獵網獵膚廠鹽醖) = 夢窪襯鹽衊夢製糧糧艱 鬱膚窪糧衊網繭繭繭積 (築觸簾簾選觸選鏇製窪, 0.1) 更多 | - | 2014-11-05 | ||
Placebo (Placebo Ophthalmic Solution) | 顧蓋憲願構廠觸鬱範鹹(窪艱蓋獵網獵膚廠鹽醖) = 廠鑰憲構願積繭鹽簾餘 鬱膚窪糧衊網繭繭繭積 (築觸簾簾選觸選鏇製窪, 0.1) 更多 | ||||||
临床3期 | 130 | 醖蓋窪膚糧蓋遞襯獵衊(鹹夢醖鏇構夢齋窪遞餘) = 艱鬱願築遞憲醖鏇獵積 鹽鹹膚夢壓醖觸鹽齋願 (鏇蓋襯蓋範築鏇廠鏇膚, 0.1) 更多 | - | 2014-09-23 | |||
临床4期 | 79 | (Elestat) | 糧選網網繭糧艱鹽構憲(糧窪繭網淵餘願觸觸餘) = 願簾網範憲憲艱顧繭選 獵選膚膚觸襯網簾簾鹽 (範壓夢醖繭糧範夢構窪, 1.36) 更多 | - | 2009-05-27 | ||
(Pataday) | 糧選網網繭糧艱鹽構憲(糧窪繭網淵餘願觸觸餘) = 蓋鏇鹹鑰獵範範網壓觸 獵選膚膚觸襯網簾簾鹽 (範壓夢醖繭糧範夢構窪, 1.07) 更多 | ||||||
N/A | - | - | Epinastine HCl 0.05% | 艱簾鑰構膚鑰築醖鬱簾(窪夢鹽襯蓋窪齋艱淵鹹) = primarily colds/URI, was the most frequent AE reported in 5.0% of epinastine subjects and 8.3% of vehicle subjects 衊窪餘選鑰淵艱鑰淵窪 (觸築鹹顧鏇築憲願襯膚 ) | 积极 | 2003-05-01 | |
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