预约演示
更新于：2025-04-15
Levocetirizine Hydrochloride
盐酸左西替利嗪
更新于：2025-04-15
概要
基本信息
简介左西替利嗪是一种小分子药物，通过 H1 受体发挥其治疗作用，作为拮抗剂对抗各种过敏性疾病，如呼吸系统超敏反应、皮炎和湿疹。该药物由UCB研发，于 2001 年 2 月获得 FDA 批准。该药物通过抑制H1 受体的活性发挥作用，随后减少由组胺释放引起的炎症。左西替利嗪提高了疗效，同时最大限度地减少了旧抗组胺药的有害副作用。 |
药物类型 小分子化药 |
别名 2-(2-{4-[(R)-(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)acetic acid、Airitis、Elzinex + [21] |
作用方式 拮抗剂 |
作用机制 H1 receptor拮抗剂(组胺H1受体拮抗剂) |
原研机构 |
在研机构 |
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C21H27Cl3N2O3 |
InChIKeyPGLIUCLTXOYQMV-GHVWMZMZSA-N |
CAS号130018-87-0 |
关联
115
项与 盐酸左西替利嗪 相关的临床试验CTRI/2025/03/082777
Comparison of efficacy, safety, and cost-effectiveness of levocetirizine, fexofenadine, and bilastine in treatment of allergic rhinitis: A randomized, open-label, parallel-group study - NIL
NCT06632405
Camrelizumab Plus Nab-paclitaxel and Anti-histamine Drug Levocetirizine in Metastatic or Recurrent Triple-negative Breast Cancer: a Randomized, Double-arm, Phase 2 Randomized Controlled Trial
NCT06816784
COMPARISON OF OUTCOME OF AUTOLOGOUS SERUM THERAPY VS LEVOCETRIZINE IN THE TREATMENT OF CHRONIC URTICARIA
100 项与 盐酸左西替利嗪 相关的临床结果
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100 项与 盐酸左西替利嗪 相关的转化医学
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100 项与 盐酸左西替利嗪 相关的专利（医药）
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987
项与 盐酸左西替利嗪 相关的文献（医药）2025-04-01EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY
Considerations of sex in bioequivalence assessments: does sex affect pharmacokinetic variability between evaluation formulations?
Article
作者: Jeong, Seung-Hyun ; Jang, Ji-Hun
BACKGROUND:
Bioequivalence assessment determines the equivalence between drug formulations and is primarily used to demonstrate that a generic product is equivalent to its reference. The sex of the drug consumer is a major consideration in bioequivalence assessment, but specific ratios or absolute criteria for sex composition are usually not specified.
PURPOSE:
This study explored whether the sex of participants in a bioequivalence assessment could significantly affect the pharmacokinetic variability between formulations and decision outcomes. In bioequivalence studies, the sex composition should reflect the drug's target population, but it is often acceptable to limit it to healthy adult males. Therefore, it is essential to consider the variation in bioequivalence results according to sex.
METHODS:
Levocetirizine and rabeprazole enteric-coated tablets were chosen as investigational agents, and clinical trial data for these were used in the bioequivalence analysis. This analysis was conducted both with and without considering sex, and the final determination of equivalence was based on whether the 90% confidence interval for the ratio of standard pharmacokinetic parameters between the reference and test formulations fell within the 80 to 125% range. Additionally, principal component analysis (PCA) was performed to determine whether there were significant differences in the targeted pharmacokinetic parameter values between drug formulations across each sex group.
RESULTS:
Bioequivalence of levocetirizine's reference and test formulations was confirmed, independent of sex. For rabeprazole, bioequivalence was established in males-even without considering sex-but not in females, based on extended criteria for drugs with significant pharmacokinetic variability. The PCA results also showed that there were significant differences (P < 0.05) in the distribution of pharmacokinetic parameters of rabeprazole by gender and formulation. This indicates that equivalence assessments may vary based on pharmacokinetic differences related to sex among subjects in bioequivalence studies. Thus, it was shown that sex may influence pharmacokinetic variability between reference and test formulations of the same drug.
CONCLUSION:
This study provided valuable insights into the role of sex in bioequivalence studies. For drugs exhibiting significant pharmacokinetic differences between sexes, it is crucial to recognize that bioequivalence results may vary based on the sex ratio in the participant group. Therefore, further analysis and interpretation, taking sex-related factors into account, will be necessary during bioequivalence evaluations.
2025-04-01INTERNATIONAL JOURNAL OF PHARMACEUTICS
Development of a stable fixed-dose combination of Montelukast Sodium and Levocetirizine Dihydrochloride using multi-layering API coating technology
Article
作者: Chae, Yu-Byeong ; Lim, Chae-Yong ; Shin, Seo-Young ; Hwang, Sung-Joo ; Yang, Jung-Ho ; Oh, Dong-Joon
PURPOSE:
This study aimed to develop a combination drug containing Montelukast Sodium and Levocetirizine Dihydrochloride using Multi-Layering API Coating Technology (M-LAC Tech) to prevent chemical interactions, enhance stability, and enable sequential drug release.
METHODS:
A core tablet containing Montelukast Sodium was prepared, followed by a barrier coating layer. Levocetirizine Dihydrochloride was then applied as a drug coating over the barrier layer, ensuring complete separation of the two drugs. M-LAC Tech effectively prevents chemical interactions, overcoming the limitations of conventional single-layer and bilayer tablets. An outer coating was added to protect against environmental factors, resulting in a multi-layered film-coated tablet with improved stability and drug release characteristics.
RESULTS:
The developed tablet reduced size by 50% compared to bilayer tablets, improving patient compliance. The barrier coating effectively prevented drug interactions, ensuring stability, while sequential drug release reduced AUC variability and shortened Tmax, enhancing absorption and efficacy. Compared to the reference "tablet-in-capsule" formulation, which releases both drugs simultaneously, the M-LAC Tech tablet demonstrated superior pharmacokinetic properties through controlled sequential release.
CONCLUSION:
M-LAC Tech enabled the stable incorporation of two drugs in a single dosage form, achieving the smallest tablet size among similar formulations. The technology's ability to block drug interactions and optimize release profiles provides significant clinical advantages. These findings highlight the potential of M-LAC Tech in advancing combination drug development.
2025-03-04JOURNAL OF ASTHMA
Efficacy and safety of montelukast–levocetirizine combination therapy in combined allergic rhinitis and asthma syndrome: a systematic review and meta-analysis
Review
作者: Sun, Jianing ; Shao, Min ; Zheng, Qiling
OBJECTIVE:
This meta-analysis aims to evaluate the efficacy and safety of montelukast combined with levocetirizine in the treatment of allergic rhinitis with asthma, and to provide objective and effective evidence-based medical evidence for clinical use.
DATA SOURCES:
PubMed, Web of Science, Cochrane Library, WANFANG DATA, CNKI, and Chinese BioMedical Literature Database were retrieved to identify records related to montelukast combined with levocetirizine in the treatment of allergic rhinitis with asthma.
STUDY SELECTIONS:
First, the eligibility criteria were employed to screen search results. Then, two investigators independently assessed titles, abstracts, and the full text of all retrieved references to identify potentially eligible studies.
RESULTS:
As of 2024-02-03, a total of six articles were included in this meta-analysis, covering 2,950 patients with allergic rhinitis with asthma. The meta-analysis results exhibited a pooled NSS of -1.28 (95%CI: -1.64 to -0.92), suggesting that the combination of montelukast and levocetirizine was effective in the treatment of nasal symptoms of allergic rhinitis complicated with asthma. The meta-analysis of controlled trials showed that the SMD of NSS in the group of montelukast combined with levocetirizine was -2.56 (95%CI: -2.77 to -2.35). The result indicated that compared with the control group, the combination of montelukast with levocetirizine significantly improved the symptoms of allergic rhinitis.
CONCLUSION:
In summary, this meta-analysis demonstrated the efficacy of montelukast combined with levocetirizine in the treatment of nasal symptoms in AR with asthma, indicating that the combination of montelukast with levocetirizine is more effective in improving symptoms of allergic rhinitis than monotherapy and has good safety.
100 项与 盐酸左西替利嗪 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 |
|---|---|---|---|
| 呼吸道过敏 | 美国 | 2017-01-31 | |
| 超敏反应 | 日本 | 2010-10-31 | |
| 皮炎 | 日本 | 2010-10-27 | |
| 湿疹 | 日本 | 2010-10-27 | |
| 痒疹 | 日本 | 2010-10-27 | |
| 瘙痒 | 日本 | 2010-10-27 | |
| 慢性荨麻疹 | 中国 | 2004-01-21 | |
| 变应性结膜炎 | 中国 | 2004-01-21 | |
| 过敏性鼻炎 | 奥地利 | 2001-08-16 | |
| 过敏性鼻炎 | 比利时 | 2001-08-16 | |
| 过敏性鼻炎 | 塞浦路斯 | 2001-08-16 | |
| 过敏性鼻炎 | 捷克 | 2001-08-16 | |
| 过敏性鼻炎 | 丹麦 | 2001-08-16 | |
| 过敏性鼻炎 | 爱沙尼亚 | 2001-08-16 | |
| 过敏性鼻炎 | 芬兰 | 2001-08-16 | |
| 过敏性鼻炎 | 法国 | 2001-08-16 | |
| 过敏性鼻炎 | 德国 | 2001-08-16 | |
| 过敏性鼻炎 | 希腊 | 2001-08-16 | |
| 过敏性鼻炎 | 匈牙利 | 2001-08-16 | |
| 过敏性鼻炎 | 爱尔兰 | 2001-08-16 |
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 |
|---|---|---|---|---|
| 过敏 | 临床3期 | - | 2003-08-01 | |
| 季节性鼻炎 | 临床3期 | - | 2003-08-01 | |
| 哮喘 | 临床3期 | - | 2002-03-20 | |
| 特应性皮炎 | 临床3期 | - | 2002-03-20 | |
| 咳嗽 | 临床2期 | - | 2001-12-01 | |
| 瘙痒（皮肤发痒） | 临床1期 | 中国 | 2017-09-12 | |
| 季节性常年性变应性鼻炎 | 临床1期 | 日本 | 2012-05-02 | |
| 禁食 | 临床1期 | 印度 | 2007-12-01 |
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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1期 | 72 | (Part 1: Levocetirizine ODT 5 mg) | 鬱選鬱選壓選憲鹽遞鬱(構蓋壓壓獵選餘齋襯觸) = 齋積鬱鏇壓窪鏇醖膚構 廠艱糧構顧夢蓋觸醖積 (鹽獵願顧簾襯餘顧構廠, 簾淵築糧遞網憲廠觸窪 ~ 繭鏇齋淵糧醖鏇糧積餘) 更多 | - | 2019-09-12 | ||
(Part 1: Levocetirizine IRT 5 mg) | 鬱選鬱選壓選憲鹽遞鬱(構蓋壓壓獵選餘齋襯觸) = 艱網選願積網壓蓋製鏇 廠艱糧構顧夢蓋觸醖積 (鹽獵願顧簾襯餘顧構廠, 襯衊齋範積製鹽簾選窪 ~ 選壓糧選齋鹽鏇艱顧憲) 更多 | ||||||
临床2期 | 47 | (Arm A: (Start Levocetirizine After Bevacizumab/Capecitabine)) | 製製夢構範夢夢餘餘願 = 憲窪鹽構夢淵簾鹽齋蓋 築鑰遞廠網築製憲衊網 (醖繭膚淵廠齋糧繭艱衊, 鏇衊觸鬱鏇築顧夢鑰願 ~ 網積壓構廠願憲獵鏇顧) 更多 | - | 2017-02-13 | ||
(Arm B: (Start Levocetirizine Before Bevacizumab/Capecitabine)) | 繭網蓋獵選鏇積願觸鏇 = 夢膚築構鹽築淵膚餘網 廠製獵選淵膚醖糧齋觸 (衊淵構顧鬱築鬱淵鏇膚, 壓衊窪鑰襯餘鑰鹽製鏇 ~ 糧鑰衊積鏇夢鏇獵構艱) 更多 | ||||||
临床2期 | 36 | 糧廠願壓顧餘選膚獵簾(積夢齋網積構顧壓壓鏇) = 齋襯餘遞網築襯選鹹鑰 廠夢觸襯膚觸襯衊築鹹 (憲憲廠顧廠憲襯衊壓獵 ) 更多 | 积极 | 2015-01-20 | |||
临床1期 | - | 20 | 獵願選齋餘廠積願觸觸(蓋選網餘構壓膚窪積壓) = 襯鹽鑰齋餘窪範積鹽膚 窪製淵願蓋淵鹹觸鑰蓋 (壓構衊膚構鬱餘築顧遞 ) 更多 | - | 2014-01-01 | ||
Cetirizine dry syrup 10mg | 獵願選齋餘廠積願觸觸(蓋選網餘構壓膚窪積壓) = 獵壓衊範鹽願鏇壓選築 窪製淵願蓋淵鹹觸鑰蓋 (壓構衊膚構鬱餘築顧遞 ) 更多 | ||||||
临床3期 | 60 | (Levocetirizine: >=6 Months and <12 Months Old) | 獵衊鬱壓遞遞襯憲壓蓋 = 築鑰獵顧蓋夢鑰網憲構 築淵蓋鏇獵簾壓構淵範 (鑰鬱繭廠糧壓簾選範憲, 構衊艱鑰膚網糧鏇製顧 ~ 餘構衊衊遞繭鹽鬱獵齋) 更多 | - | 2013-06-03 | ||
(Levocetirizine: >=12 Months and <24 Months Old) | 獵衊鬱壓遞遞襯憲壓蓋 = 繭製顧窪壓衊繭餘願製 築淵蓋鏇獵簾壓構淵範 (鑰鬱繭廠糧壓簾選範憲, 製壓顧積齋遞築糧廠糧 ~ 鬱鏇窪夢憲選壓鑰築鑰) 更多 | ||||||
N/A | - | 餘簾遞鹽鑰憲艱製糧衊(範構齋鹹鑰艱夢鹹構範) = 鬱簾顧壓願醖憲範簾艱 餘夢憲鬱鹽網糧獵觸憲 (願壓醖憲鏇範衊選鹹願, -8.1% ~ -7.9%) 更多 | 积极 | 2011-02-01 | |||
N/A | 常年性变应性鼻炎 nNO | nEos | 31 | Oral Levocetirizine (LC) 5mg | 獵糧獵壓窪餘鏇蓋窪願(壓獵淵餘簾鹹遞窪遞蓋) = 窪衊膚襯鬱顧衊鏇觸網 膚襯糧壓艱繭餘鑰餘襯 (願鑰鬱淵製壓鹹鑰壓憲 ) | 积极 | 2010-02-01 | |
临床4期 | 580 | placebo | 醖網製襯獵鏇齋蓋齋壓(淵遞糧繭遞鹽蓋膚簾餘) = 鬱鹽鏇膚積艱齋製壓築 遞窪獵簾夢構齋簾餘淵 (鹹糧糧觸廠網觸選膚積, 3.44) 更多 | - | 2009-11-17 | ||
临床3期 | 466 | (Levocetirizine) | 獵獵餘膚餘廠艱簾獵獵 = 艱糧夢構網鹹繭艱餘願 醖窪淵鹹網簾積糧網糧 (壓繭鹽積鹽鏇糧鏇齋鑰, 淵夢糧繭構齋憲齋構選 ~ 鏇壓觸製醖網憲廠蓋艱) 更多 | - | 2009-10-14 | ||
(Cetirizine) | 獵獵餘膚餘廠艱簾獵獵 = 鏇窪餘獵憲獵壓繭糧醖 醖窪淵鹹網簾積糧網糧 (壓繭鹽積鹽鏇糧鏇齋鑰, 蓋憲襯繭醖網鑰膚製廠 ~ 遞壓願範蓋鏇衊艱觸鹽) 更多 | ||||||
临床3期 | 69 | Placebo (Placebo) | 觸願衊憲艱積壓獵壓襯(範遞鹽築鹽淵壓壓醖鹹) = 壓夢糧淵獵鬱鹹願艱觸 構獵網糧憲鬱願顧簾鑰 (築窪願顧膚餘築鹽窪願, 17.3) 更多 | - | 2009-10-14 | ||
(Levocetirizine) | 觸願衊憲艱積壓獵壓襯(範遞鹽築鹽淵壓壓醖鹹) = 網築選構艱製範糧窪獵 構獵網糧憲鬱願顧簾鑰 (築窪願顧膚餘築鹽窪願, 16.9) 更多 |
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