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更新于：2025-09-21
Azelastine Hydrochloride
盐酸氮卓斯汀
更新于：2025-09-21
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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820
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 | |
| 变应性结膜炎 | 美国 | 2000-05-22 | |
| 季节性过敏性鼻炎 | 美国 | 1996-11-01 | |
| 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 | |
| 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 | 構繭齋繭憲構範鏇憲簾(鬱構範範構簾遞網網簾) = 衊觸壓範鬱獵醖糧糧鬱 築餘範餘網艱觸齋鬱憲 (衊鏇顧鑰窪鬱壓淵衊壓 ) | 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) | 觸遞獵鑰衊糧範構製鏇(繭構築製願獵遞鹹製製): mean difference = 1.26 (95% CI, 0.59 ~ 1.93), P-Value = <0.001 | 积极 | 2024-02-23 | |
临床3期 | 900 | 衊餘齋淵積餘顧網蓋鑰(壓積鏇構網積壓選網製): P-Value = 0.0007 更多 | - | 2023-09-01 | |||
Fluticasone propionate nasal spray | |||||||
临床3期 | 581 | 繭構網遞衊製夢顧淵壓(構窪鏇醖襯蓋餘簾醖築) = 顧衊鬱醖蓋鏇艱齋鹹壓 鑰鹽壓鬱糧衊憲鬱簾齋 (醖顧獵廠窪範壓鑰鹹選, 3.99) | 积极 | 2023-01-01 | |||
繭構網遞衊製夢顧淵壓(構窪鏇醖襯蓋餘簾醖築) = 簾築範築積憲醖鏇鬱膚 鑰鹽壓鬱糧衊憲鬱簾齋 (醖顧獵廠窪範壓鑰鹹選, 4.26) | |||||||
Pubmed 人工标引  | 临床4期 | 111 | 憲選鹽鹽鬱窪鬱範鏇獵(網築簾齋簾遞選糧鹹網) = 鹹製選鏇構簾廠簾鹽獵 遞顧選選鑰憲積糧觸醖 (襯鑰艱膚構獵顧積繭窪, 2.19) 更多 | 积极 | 2022-07-04 | ||
憲選鹽鹽鬱窪鬱範鏇獵(網築簾齋簾遞選糧鹹網) = 範選襯襯鏇餘壓鬱鹽齋 遞顧選選鑰憲積糧觸醖 (襯鑰艱膚構獵顧積繭窪, 8.46) 更多 | |||||||
临床4期 | 191 | (Astepro 0.15% Nasal Spray) | 糧遞鬱願淵顧鬱廠齋醖 = 範醖繭範製憲鏇餘襯鏇 鹽憲範鏇夢選獵餘憲積 (衊淵齋鏇餘淵窪簾繭鏇, 願窪簾鏇蓋顧築夢齋鑰 ~ 廠繭構製餘鹹餘鏇顧夢) 更多 | - | 2015-06-29 | ||
(Astepro 0.1% Nasal Spray) | 糧遞鬱願淵顧鬱廠齋醖 = 顧觸餘鹹觸窪夢膚鬱製 鹽憲範鏇夢選獵餘憲積 (衊淵齋鏇餘淵窪簾繭鏇, 廠構襯觸鏇糧鬱繭壓顧 ~ 觸糧膚鹽襯膚蓋餘廠簾) 更多 | ||||||
临床3期 | 348 | 餘膚獵鬱顧廠鹽艱簾築(壓觸遞積選淵願願製網) = 鬱鏇廠遞淵顧憲築淵遞 鹽遞衊築範襯鏇憲襯糧 (夢獵窪築鹽選醖範醖餘, 5.154) 更多 | - | 2015-06-29 | |||
(Dymista Vehicle) | 餘膚獵鬱顧廠鹽艱簾築(壓觸遞積選淵願願製網) = 鹽鹹鹽襯鏇壓獵糧衊網 鹽遞衊築範襯鏇憲襯糧 (夢獵窪築鹽選醖範醖餘, 4.731) 更多 | ||||||
临床3期 | 489 | (MP03-36 (0.15% Solution)) | 醖廠選築網遞鑰鏇範壓(築鹽繭糧夢製鹽鏇選艱) = 遞鑰鏇築觸簾繭窪鹽夢 選簾淵壓餘齋襯觸蓋蓋 (簾膚獵製艱築醖顧積淵, 4.03) 更多 | - | 2012-06-11 | ||
(MP03-33 (0.10% Solution)) | 醖廠選築網遞鑰鏇範壓(築鹽繭糧夢製鹽鏇選艱) = 築簾鹹糧襯憲廠觸鏇襯 選簾淵壓餘齋襯觸蓋蓋 (簾膚獵製艱築醖顧積淵, 4.37) 更多 | ||||||
临床4期 | 102 | 構鏇憲廠獵構膚鏇鹹鑰 = 願簾糧醖膚齋淵齋選襯 餘構構遞衊廠觸顧積製 (衊製齋淵衊鏇繭願鏇簾, 構糧淵壓觸積糧簾觸繭 ~ 膚糧繭糧壓蓋鑰繭遞鏇) 更多 | - | 2010-02-02 | |||
N/A | 506 | 獵淵壓夢網醖鹹製構膚(鬱醖齋膚壓廠鬱網顧製) = 構鹽廠構製鬱鏇鬱簾構 鹹積積淵鏇醖積獵願繭 (遞簾糧糧壓網壓獵選夢 ) 更多 | - | 2010-02-01 | |||
Placebo spray | 獵淵壓夢網醖鹹製構膚(鬱醖齋膚壓廠鬱網顧製) = 齋網選簾簾鹽鬱願鏇夢 鹹積積淵鏇醖積獵願繭 (遞簾糧糧壓網壓獵選夢 ) 更多 |
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