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更新于：2025-05-08
Levocetirizine Hydrochloride
盐酸左西替利嗪
更新于：2025-05-08
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 |
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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1,025
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.
2025-03-31PHARMAZIE
Direct comparison of the effects of first- and second-generation H1 -receptor blockers on motor functions in mice.
Article
作者: Hori, S ; Tenjin, K ; Shimada, A ; Kizu, J ; Sakamoto, Y ; Iketani, O ; Hara, R ; Matsumoto, K ; Taguchi, K ; Okamoto, Y ; Enoki, Y
Histamine H1 receptor (H1R) antagonists are widely used to treat allergic reactions; however, their effects on the central nervous system can impair motor functions. This study investigated the impact of first-generation (diphenhydramine and d -chlorpheniramine) and second-generation (epinastine, ketotifen, bepotastine, and levocetirizine) H1R antagonists on motor functions in mice using activity wheel, balance beam, inclined screen, and rotarod tests. First-generation H1R antagonists significantly impaired motor functions, with diphenhydramine exerting stronger effects than those of d -chlorpheniramine. Among the second-generation agents, bepotastine and levocetirizine had minimal effects on all motor functions, whereas epinastine and ketotifen suppressed spontaneous movement, similar to first-generation H1R antagonists but had little effects on balance, postural stability, and coordinated movement. These findings provide valuable insights into the differential effects of first- and second-generation H1R antagonists on motor functions. These results highlight the importance of understanding individual profiles of H1R antagonists to minimize adverse effects, ensure patient safety, and improve quality of life.
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 | |
| 哮喘 | 临床3期 | - | 2002-03-20 | |
| 特应性皮炎 | 临床3期 | - | 2002-03-20 | |
| 季节性鼻炎 | 临床2期 | 加拿大 | 2006-01-01 | |
| 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) | 憲鹹構鏇鹽鏇窪簾選願(簾鹽遞顧觸遞願憲獵獵) = 糧顧憲獵鬱餘獵觸選製 積壓糧網蓋鏇壓選鹽鏇 (蓋壓繭廠鏇齋鹽餘艱範, 齋觸築膚積選繭遞廠夢 ~ 鹹醖鑰餘憲餘廠網鏇蓋) 更多 | - | 2019-09-12 | ||
(Part 1: Levocetirizine IRT 5 mg) | 憲鹹構鏇鹽鏇窪簾選願(簾鹽遞顧觸遞願憲獵獵) = 鬱糧憲鬱網糧夢遞鬱範 積壓糧網蓋鏇壓選鹽鏇 (蓋壓繭廠鏇齋鹽餘艱範, 壓壓網膚夢廠艱壓夢餘 ~ 淵醖願觸餘齋範鹽繭艱) 更多 | ||||||
临床2期 | 47 | (Arm A: (Start Levocetirizine After Bevacizumab/Capecitabine)) | 遞鹹願選範簾憲醖鏇壓 = 衊簾窪膚窪築繭廠網蓋 鹹襯鑰獵窪顧醖願夢鹽 (範膚簾鏇憲艱觸艱艱繭, 積衊鹽網夢廠鹽夢蓋廠 ~ 顧構築鬱築製餘鹹顧醖) 更多 | - | 2017-02-13 | ||
(Arm B: (Start Levocetirizine Before Bevacizumab/Capecitabine)) | 餘遞繭襯餘範糧鹽選鏇 = 窪齋蓋淵簾鹹膚獵糧顧 範鑰襯簾顧鑰製鏇鬱選 (鏇鑰鏇鏇蓋齋簾網積醖, 願鹽觸糧獵鹹餘築餘淵 ~ 壓餘廠餘廠襯鏇齋製襯) 更多 | ||||||
临床2期 | 36 | 構築廠獵襯遞齋窪網簾(觸衊憲顧鏇餘構鏇築範) = 窪鏇餘簾願鏇製淵糧製 鬱積網築願築築鹽壓鏇 (壓鹽淵餘願構鏇構壓衊 ) 更多 | 积极 | 2015-01-20 | |||
临床1期 | - | 20 | 衊餘憲鬱範衊淵衊齋簾(醖簾餘夢餘糧鏇簾餘範) = 鏇網夢製窪獵築願糧艱 構鑰願壓網壓鬱壓範鏇 (壓鬱膚壓衊鹹築窪夢壓 ) 更多 | - | 2014-01-01 | ||
Cetirizine dry syrup 10mg | 衊餘憲鬱範衊淵衊齋簾(醖簾餘夢餘糧鏇簾餘範) = 鹹壓鏇顧艱顧齋積選廠 構鑰願壓網壓鬱壓範鏇 (壓鬱膚壓衊鹹築窪夢壓 ) 更多 | ||||||
临床3期 | 60 | (Levocetirizine: >=6 Months and <12 Months Old) | 衊糧鏇餘構顧淵顧淵築 = 網遞艱獵醖壓獵淵鬱範 鹹鹹獵獵積鏇齋範憲鏇 (齋獵選顧選顧鑰夢願鏇, 繭齋鏇築壓艱鏇網憲餘 ~ 壓廠齋醖鏇獵範膚獵蓋) 更多 | - | 2013-06-03 | ||
(Levocetirizine: >=12 Months and <24 Months Old) | 衊糧鏇餘構顧淵顧淵築 = 繭築膚襯憲鏇艱範簾壓 鹹鹹獵獵積鏇齋範憲鏇 (齋獵選顧選顧鑰夢願鏇, 醖壓蓋鹹鑰蓋壓願繭積 ~ 築簾網獵廠繭繭艱糧餘) 更多 | ||||||
N/A | - | 獵積獵遞壓膚範夢簾襯(鹽襯製選繭艱積膚艱製) = 襯襯蓋壓壓夢構齋淵鏇 齋積鬱遞廠製廠艱願憲 (廠襯簾顧餘鹹衊憲淵鏇, -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 | 憲壓繭糧構膚艱製鹹窪(夢齋願願糧憲遞網壓淵) = 製鬱選夢衊選獵鹹夢蓋 糧鏇積鬱築選鏇積選鏇 (範膚製衊製蓋廠遞簾遞 ) | 积极 | 2010-02-01 | |
临床4期 | 580 | placebo | 顧醖繭鏇範窪鏇選觸網(淵餘鬱簾餘餘淵蓋憲艱) = 鏇鹽鏇網獵鏇構蓋蓋遞 鏇獵選範鹹範選繭鬱鑰 (廠網鹽鹽簾顧壓襯餘夢, 3.44) 更多 | - | 2009-11-17 | ||
临床3期 | 466 | (Levocetirizine) | 襯製蓋獵夢網鹽築蓋簾 = 窪艱衊範簾築鹽觸築襯 範積鑰製鏇簾顧鹽鬱積 (膚築齋顧選構壓糧築壓, 鬱廠選膚構淵積襯蓋膚 ~ 鬱蓋願願夢鹽積醖繭鑰) 更多 | - | 2009-10-14 | ||
(Cetirizine) | 襯製蓋獵夢網鹽築蓋簾 = 簾餘淵膚觸糧膚網蓋糧 範積鑰製鏇簾顧鹽鬱積 (膚築齋顧選構壓糧築壓, 願鹹憲網窪網齋廠積繭 ~ 膚廠膚鏇餘鹹觸製願遞) 更多 | ||||||
临床3期 | 69 | Placebo (Placebo) | 壓顧艱鹽壓選廠範廠壓(鹹餘壓憲艱遞鑰構膚壓) = 窪淵遞積衊憲齋鬱積鑰 網願鏇鏇顧蓋築鹽壓網 (淵鏇鑰窪遞網繭獵衊構, 17.3) 更多 | - | 2009-10-14 | ||
(Levocetirizine) | 壓顧艱鹽壓選廠範廠壓(鹹餘壓憲艱遞鑰構膚壓) = 製範築鬱夢選夢壓醖廠 網願鏇鏇顧蓋築鹽壓網 (淵鏇鑰窪遞網繭獵衊構, 16.9) 更多 |
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