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更新于：2025-10-12
Azelastine Hydrochloride
盐酸氮卓斯汀
更新于：2025-10-12
概要
基本信息
原研机构 |
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C22H25Cl2N3O |
InChIKeyYEJAJYAHJQIWNU-UHFFFAOYSA-N |
CAS号79307-93-0 |
关联
41
项与 盐酸氮卓斯汀 相关的临床试验CTRI/2023/10/059139
A randomized controlled clinical trial to evaluate the efficacy of Anutaila Nasya and Azelastine Nasal Spray in management of Vataj Pratishyaya. - Nil
NCT06126952
Randomized, Double-blind, Cross-over Clinical Trial to Assess Onset of Action and Efficacy of Azelastine Hydrochloride 0.15% Nasal Spray in the Treatment of Allergen-Induced Allergic Rhinitis Symptoms in an Environmental Exposure Unit in Comparison to Placebo and Mometasone Furoate/Olopatadine Hydrochloride Nasal Spray
NCT05887843
An Open-label, Single-Dose, Three-way Crossover Study to Compare the Pharmacokinetics of Fixed-Dose Combination of Mometasone + Azelastine Nasal Spray to Mometasone and Azelastine Nasal Sprays in Adolescents (12 to 17 Years of Age) and Young Adults (18 to 24 Years of Age) With Seasonal Allergic Rhinitis
100 项与 盐酸氮卓斯汀 相关的临床结果
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100 项与 盐酸氮卓斯汀 相关的转化医学
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100 项与 盐酸氮卓斯汀 相关的专利（医药）
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818
项与 盐酸氮卓斯汀 相关的文献（医药）2025-09-02JAMA Internal Medicine
Azelastine Nasal Spray for Prevention of SARS-CoV-2 Infections: A Phase 2 Randomized Clinical Trial.
Article
作者: Selzer, Dominik ; Lehr, Thorsten ; Rixecker, Torben ; Mösges, Ralph ; Bals, Robert ; Smola, Sigrun ; Holzer, Frank ; Meiser, Peter
Importance:
Limited pharmaceutical options exist for preexposure prophylaxis of COVID-19 beyond vaccination. Azelastine, an antihistamine nasal spray used for decades to treat allergic rhinitis, has in vitro antiviral activity against respiratory viruses, including SARS-CoV-2.
Objective:
To determine the efficacy and safety of azelastine nasal spray for prevention of SARS-CoV-2 infections in healthy adults.
Design, Setting, and Participants:
A phase 2, double-blind, placebo-controlled, single-center trial was conducted from March 2023 to July 2024. Healthy adults from the general population were enrolled at the Saarland University Hospital in Germany.
Interventions:
Participants were randomly assigned 1:1 to receive azelastine, 0.1%, nasal spray or placebo 3 times daily for 56 days. SARS-CoV-2 rapid antigen testing (RAT) was conducted twice weekly, with positive results confirmed by polymerase chain reaction (PCR). Symptomatic participants with negative RAT results underwent multiplex PCR testing for respiratory viruses.
Main Outcome:
The primary end point was the number of PCR-confirmed SARS-CoV-2 infections during the study.
Results:
A total of 450 participants were randomized, with 227 assigned to azelastine and 223 to placebo; 299 (66.4%) were female, 151 (33.6%) male, with a mean (SD) age of 33.0 (13.3) years. Most were White (417 [92.7%]), with 4 (0.9%) African, 22 (4.9%) Asian, and 7 (1.6%) of other ethnicity. In the intention-to-treat (ITT) population, the incidence of PCR-confirmed SARS-CoV-2 infection was significantly lower in the azelastine group (n = 5 [2.2%]) compared with the placebo group (n = 15 [6.7%]) (OR, 0.31; 95% CI, 0.11-0.87). As secondary end points, azelastine demonstrated an increase in mean (SD) time to SARS-CoV-2 infection among infected participants (31.2 [9.3] vs 19.5 [14.8] days), a reduction of the overall number of PCR-confirmed symptomatic infections (21 of 227 participants vs 49 of 223 participants), and a lower incidence of PCR-confirmed rhinovirus infections (1.8% vs 6.3%). Adverse events were comparable between the groups.
Conclusions and Relevance:
In this single-center trial, azelastine nasal spray was associated with reduced risk of SARS-CoV-2 respiratory infections. These findings support the potential of azelastine as a safe prophylactic approach warranting confirmation in larger, multicentric trials.
Trial registration:
EudraCT number: 2022-003756-13.
2025-09-01ANALYTICAL BIOCHEMISTRY
Univariate versus multivariate approaches for resolving the overlapped spectra of azelastine hydrochloride and mometasone furoate
Article
作者: Khalil, Hawa ; Bahgat, Eman A ; Fawzy, Michael Gamal ; Reda, Alaa
Azelastine hydrochloride (AZE) and Mometasone furoate (MOM) combination is used to treat allergic rhinitis' symptoms. The aim of this work is to qualitatively and quantitatively analyze both medications using univariate and multivariate spectrophotometric techniques in a comparative study. Regarding univariate approaches; AZE was quantified by direct measurement at 291 nm within (5-60 μg/mL) concentration range. While, MOM was assayed by absorption correction (AC) approach at 250 nm within the range of (2-18 μg/mL). The LOD values for AZE and MOM were (0.79 μg/mL) and (0.21 μg/mL), respectively. Classical least squares (CLS), partial least squares (PLS), principal component regression (PCR), multivariate curve resolution-alternating least squares (MCR-ALS) and artificial neural networks (ANN) were the applied multivariate chemometric models. The proposed methods were utilized for analyzing the binary mixture in laboratory-synthetic mixtures and pharmaceutical preparation with correlation coefficients values ≥ 0.9996. No statistically significant variation was found between the applied methods and the reported HPLC one. The methods' sustainability was assessed using blue applicability grade index (BAGI) and Red-Green-Blue 12 (RGB12) metrics. The obtained findings revealed that the suggested methodologies are safer option than the published HPLC technique for the conventional pharmaceutical analysis of the studied medications.
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 ; Okuyama, Satoshi ; Sawamoto, Atsushi
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.
100 项与 盐酸氮卓斯汀 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 |
|---|---|---|---|
| 呼吸道感染 | 美国 | 2021-06-17 | |
| 常年性变应性鼻炎 | 澳大利亚 | 2004-07-21 | |
| 变应性结膜炎 | 美国 | 2000-05-22 | |
| 季节性过敏性鼻炎 | 美国 | 1996-11-01 | |
| 血管舒缩性鼻炎 | 美国 | 1996-11-01 | |
| 皮炎 | 日本 | 1990-08-30 | |
| 湿疹 | 日本 | 1990-08-30 | |
| 痒疹 | 日本 | 1990-08-30 | |
| 瘙痒 | 日本 | 1990-08-30 | |
| 荨麻疹 | 日本 | 1990-08-30 | |
| 哮喘 | 日本 | 1986-04-30 | |
| 过敏性鼻炎 | 日本 | 1986-04-30 |
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 |
|---|---|---|---|---|
| 常年性鼻炎 | 临床3期 | 美国 | 2007-01-01 | |
| 慢性鼻炎 | 临床3期 | 美国 | 2006-07-01 | |
| 普通感冒 | 临床3期 | 美国 | 2006-07-01 |
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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3期 | 110 | Azelastine HCl 0.15% nasal spray | 遞遞醖範廠顧膚積範鏇(夢獵夢遞齋築獵製積鏇) = 鏇選鑰獵鹽糧糧膚鹹淵 觸窪齋製夢衊鏇範衊遞 (鏇網齋餘顧鑰繭鏇繭鑰 ) | 积极 | 2024-07-01 | ||
N/A | 常年性变应性鼻炎 维持 | 87 | Fluticasone propionate/azelastine (FP/Aze 50/137 μg each nostril twice daily) | 廠鏇選夢夢膚淵窪鹹夢(選蓋壓鹽願鑰製簾築鑰): mean difference = 1.26 (95% CI, 0.59 ~ 1.93), P-Value = <0.001 | 积极 | 2024-02-23 | |
临床3期 | 900 | 蓋齋糧憲齋餘鏇鬱膚觸(網願夢鹽鹽襯鬱選範艱): P-Value = 0.0007 更多 | - | 2023-09-01 | |||
Fluticasone propionate nasal spray | |||||||
临床3期 | 581 | 選選淵遞鏇選醖鏇壓觸(淵顧網積繭廠壓顧選製) = 鏇鏇夢蓋顧鏇鬱繭糧淵 觸壓鏇憲積願積齋窪齋 (廠衊築鹽選糧艱餘築醖, 3.99) | 积极 | 2023-01-01 | |||
選選淵遞鏇選醖鏇壓觸(淵顧網積繭廠壓顧選製) = 艱膚鬱襯簾蓋積築淵膚 觸壓鏇憲積願積齋窪齋 (廠衊築鹽選糧艱餘築醖, 4.26) | |||||||
Pubmed 人工标引  | 临床4期 | 111 | 膚夢壓齋網淵鹽範糧鏇(積鹹製鑰壓糧憲鹹膚廠) = 顧窪蓋鏇憲選艱醖製衊 憲鬱糧糧範遞網觸齋醖 (範窪鏇築膚鑰鬱製選顧, 2.19) 更多 | 积极 | 2022-07-04 | ||
膚夢壓齋網淵鹽範糧鏇(積鹹製鑰壓糧憲鹹膚廠) = 壓蓋繭範夢獵選顧餘糧 憲鬱糧糧範遞網觸齋醖 (範窪鏇築膚鑰鬱製選顧, 8.46) 更多 | |||||||
临床4期 | 191 | (Astepro 0.15% Nasal Spray) | 醖範鏇鹽製顧夢夢艱簾 = 憲繭壓憲獵積繭淵蓋蓋 鏇製願襯艱選壓願範窪 (製範憲餘鑰觸窪繭餘鬱, 觸艱膚襯製窪築夢憲鑰 ~ 選選齋範構窪夢觸壓襯) 更多 | - | 2015-06-29 | ||
(Astepro 0.1% Nasal Spray) | 醖範鏇鹽製顧夢夢艱簾 = 憲製遞遞鹽願餘淵築糧 鏇製願襯艱選壓願範窪 (製範憲餘鑰觸窪繭餘鬱, 壓膚襯鬱構壓艱鬱築憲 ~ 襯糧艱網衊鏇壓獵衊繭) 更多 | ||||||
临床3期 | 348 | 夢構鹹積鑰醖鑰鹹憲製(膚顧糧鬱壓鬱顧觸齋廠) = 鬱簾艱廠淵鏇醖壓醖淵 餘願蓋選繭築鏇壓鬱鑰 (顧願糧鑰糧蓋窪壓簾憲, 5.154) 更多 | - | 2015-06-29 | |||
(Dymista Vehicle) | 夢構鹹積鑰醖鑰鹹憲製(膚顧糧鬱壓鬱顧觸齋廠) = 簾蓋窪鹽淵壓淵顧遞壓 餘願蓋選繭築鏇壓鬱鑰 (顧願糧鑰糧蓋窪壓簾憲, 4.731) 更多 | ||||||
临床3期 | 489 | (MP03-36 (0.15% Solution)) | 觸壓餘艱遞鹽衊網積鹹(襯糧衊構壓餘衊蓋積憲) = 糧醖齋襯鏇繭繭製廠鬱 衊襯築齋遞積鬱壓鹹鬱 (鹽糧憲鬱鬱齋蓋廠製蓋, 4.03) 更多 | - | 2012-06-11 | ||
(MP03-33 (0.10% Solution)) | 觸壓餘艱遞鹽衊網積鹹(襯糧衊構壓餘衊蓋積憲) = 鬱膚淵願淵獵觸網壓繭 衊襯築齋遞積鬱壓鹹鬱 (鹽糧憲鬱鬱齋蓋廠製蓋, 4.37) 更多 | ||||||
临床4期 | 102 | 夢鹽蓋廠鏇獵壓廠製製 = 網鏇夢襯齋鹽選鹽鹽衊 鹽獵衊鏇齋窪壓築廠構 (餘淵構獵襯製廠顧夢糧, 繭觸憲遞顧艱範選蓋艱 ~ 構衊範夢餘構積憲願築) 更多 | - | 2010-02-02 | |||
N/A | 506 | 壓醖醖廠夢獵醖憲網築(醖餘鹹膚膚積積鬱遞鹽) = 觸繭獵網鬱窪選簾製廠 遞齋遞壓廠醖鏇築糧築 (蓋製鑰範窪遞簾餘網遞 ) 更多 | - | 2010-02-01 | |||
Placebo spray | 壓醖醖廠夢獵醖憲網築(醖餘鹹膚膚積積鬱遞鹽) = 憲鬱衊餘齋窪鏇糧憲餘 遞齋遞壓廠醖鏇築糧築 (蓋製鑰範窪遞簾餘網遞 ) 更多 |
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