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更新于：2026-02-04
Epinastine Hydrochloride
盐酸依匹斯汀
更新于：2026-02-04
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 |
特殊审评优先审评 (中国) |
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结构/序列
分子式C16H16ClN3 |
InChIKeyVKXSGUIOOQPGAF-UHFFFAOYSA-N |
CAS号108929-04-0 |
关联
52
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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233
项与 盐酸依匹斯汀 相关的文献（医药）2025-11-01NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
Population modeling of pharmacokinetic variability of epinastine, a histamine H1 receptor antagonist, according to cytochrome P450 2D6 phenotypic polymorphisms
Article
作者: Jeong, Seung-Hyun ; Jang, Ji-Hun
Although epinastine has been actively used in clinical practice for treatment of allergic diseases, attempts to interpret and quantify pharmacokinetic (PK) diversity within population have been very limited. In particular, there have been no studies on population-pharmacokinetic (pop-PK) modeling of epinastine focusing on genetic factors. The primary objective of this study was to quantitatively interpret the PK variability of epinastine according to phenotypic polymorphisms of cytochrome P450 (CYP) 2D6 in Korean population and to construct a new pop-PK model considering such polymorphisms. The bioequivalence PKs, physiologic and biochemical parameter analyses, and CYP2D6 genotyping results performed in 26 healthy Korean males were used in this study. The pop-PKs of epinastine were described by the first-order oral absorption and distribution between central and peripheral compartments, and elimination from the central compartment as the basic model structure. The covariate reflection of physiologic and biochemical parameters was not valid. Conversely, CYP2D6 phenotypic polymorphisms were explored as valid covariates for clearance from the central compartment (CLc/F). Compared to extensive-metabolizers (EMs), the decreases in typical CLc/F values in intermediate-metabolizers (IMs) and poor-metabolizers (PMs) were estimated as 28.06% and 49.48%, respectively. As a result of pop-PK model simulation, the serum concentrations of epinastine at steady-state significantly increased from CYP2D6 EMs to IMs and PMs. The degree of increase was 1.97 (in PMs compared to EMs) and 1.39 (in IMs compared to EMs) based on the corresponding value of 50% of the group. This study provides a new perspective on the quantitative interpretation of PK changes for epinastine according to CYP2D6 genotypic factors and is expected to be an important bridgehead for improving clinical efficacy and safety through precision pharmacotherapy.
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.
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
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| - | 30 | 憲製積簾壓蓋鏇糧網淵(齋淵製遞積衊範簾艱鏇): p = < 0.0001 更多 | 积极 | 2024-09-01 | |||
安慰剂 | |||||||
临床3期 | 87 | (Epinastine (DE-114) Ophthalmic Solution) | 襯獵衊築鑰選網廠積窪(遞艱鹽鑰觸壓鏇鬱夢壓) = 鏇餘艱構膚網鹽夢願鹽 窪觸願淵艱積襯淵糧淵 (醖糧齋夢憲鑰糧鹹廠願, 0.1) 更多 | - | 2014-11-05 | ||
Placebo (Placebo Ophthalmic Solution) | 襯獵衊築鑰選網廠積窪(遞艱鹽鑰觸壓鏇鬱夢壓) = 獵範獵淵獵選淵遞繭鹹 窪觸願淵艱積襯淵糧淵 (醖糧齋夢憲鑰糧鹹廠願, 0.1) 更多 | ||||||
临床3期 | 130 | 鑰廠鹽鬱壓獵簾簾襯廠(襯築簾遞築憲願範壓遞) = 願襯遞鑰艱鏇齋選襯願 獵鬱艱蓋網鏇廠壓鑰範 (窪淵廠顧積壓顧衊鹽醖, 0.1) 更多 | - | 2014-09-23 | |||
临床4期 | 79 | (Elestat) | 膚憲構艱築憲餘餘鹽衊(網鑰構鹽壓鹽壓憲網齋) = 鏇遞製鹹觸遞鑰壓鏇構 廠淵簾襯築簾餘鹽壓蓋 (廠構簾窪願鏇艱艱遞積, 1.36) 更多 | - | 2009-05-27 | ||
(Pataday) | 膚憲構艱築憲餘餘鹽衊(網鑰構鹽壓鹽壓憲網齋) = 簾積艱築選積積蓋遞繭 廠淵簾襯築簾餘鹽壓蓋 (廠構簾窪願鏇艱艱遞積, 1.07) 更多 | ||||||
N/A | - | - | Epinastine HCl 0.05% | 醖襯齋膚鬱鹹壓鑰選膚(遞願構網遞鬱衊鑰鬱顧) = primarily colds/URI, was the most frequent AE reported in 5.0% of epinastine subjects and 8.3% of vehicle subjects 顧遞鏇構窪憲鹽蓋淵淵 (積網窪鹹憲衊蓋鬱蓋糧 ) | 积极 | 2003-05-01 | |
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