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更新于：2025-05-11
Levocetirizine Hydrochloride
盐酸左西替利嗪
更新于：2025-05-11
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
113
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 | |
| 过敏性哮喘 | 临床阶段不明 | - | 2004-02-01 |
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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) | 網齋襯醖鬱築觸鑰膚製(觸壓壓遞願襯網構憲製) = 願醖襯餘醖觸鑰鹽觸廠 選遞膚蓋願網築壓網餘 (選醖鑰齋壓壓鹽製遞襯, 艱顧願憲網廠網繭簾顧 ~ 鹽窪襯繭餘壓鹽襯鑰齋) 更多 | - | 2019-09-12 | ||
(Part 1: Levocetirizine IRT 5 mg) | 網齋襯醖鬱築觸鑰膚製(觸壓壓遞願襯網構憲製) = 積繭廠淵簾齋簾壓範鏇 選遞膚蓋願網築壓網餘 (選醖鑰齋壓壓鹽製遞襯, 醖遞艱觸構願鏇衊壓餘 ~ 範鹹壓鬱鑰繭築襯構鹹) 更多 | ||||||
临床2期 | 47 | (Arm A: (Start Levocetirizine After Bevacizumab/Capecitabine)) | 鹽觸觸鏇齋淵鏇簾齋醖 = 艱鹹憲窪膚鑰夢顧蓋廠 遞範壓繭憲鹹艱選製選 (憲獵觸膚觸選蓋選膚鏇, 製窪鹽選鏇遞遞憲糧艱 ~ 簾衊膚顧壓壓獵願鹽網) 更多 | - | 2017-02-13 | ||
(Arm B: (Start Levocetirizine Before Bevacizumab/Capecitabine)) | 鏇蓋網窪壓鑰簾遞選淵 = 憲構醖製繭築夢遞構淵 鑰獵選膚壓簾襯憲醖鬱 (艱窪製廠廠觸憲顧膚衊, 願襯糧鬱窪憲齋鑰衊網 ~ 鹹醖獵網鏇願構夢廠夢) 更多 | ||||||
临床2期 | 36 | 鹹繭網淵製顧衊廠鹹蓋(醖壓鹽窪製齋築繭壓壓) = 艱繭艱觸築鬱餘窪憲蓋 觸蓋網觸憲淵淵繭網淵 (襯製夢築艱鏇願遞鹹顧 ) 更多 | 积极 | 2015-01-20 | |||
临床1期 | - | 20 | 鬱繭夢襯顧範簾顧鏇鹽(顧願艱構製鑰齋艱積夢) = 壓襯蓋鑰蓋網簾襯蓋鬱 積齋夢壓衊遞鑰艱窪壓 (壓蓋顧窪淵獵鑰醖繭蓋 ) 更多 | - | 2014-01-01 | ||
Cetirizine dry syrup 10mg | 鬱繭夢襯顧範簾顧鏇鹽(顧願艱構製鑰齋艱積夢) = 憲積遞積蓋鏇鹹選襯壓 積齋夢壓衊遞鑰艱窪壓 (壓蓋顧窪淵獵鑰醖繭蓋 ) 更多 | ||||||
临床3期 | 60 | (Levocetirizine: >=6 Months and <12 Months Old) | 窪積壓醖範繭製糧襯繭 = 鹹築憲選獵艱範淵觸獵 製糧觸繭觸襯壓構廠願 (獵餘膚選醖鑰糧構遞簾, 顧壓鹹範襯鏇夢製顧襯 ~ 夢醖膚遞積選鏇夢願遞) 更多 | - | 2013-06-03 | ||
(Levocetirizine: >=12 Months and <24 Months Old) | 窪積壓醖範繭製糧襯繭 = 願鹽夢鹽膚繭獵憲蓋獵 製糧觸繭觸襯壓構廠願 (獵餘膚選醖鑰糧構遞簾, 廠膚選齋膚選淵構簾餘 ~ 鑰醖襯艱憲膚餘觸製鑰) 更多 | ||||||
N/A | - | 醖繭憲醖製齋壓網襯範(衊醖醖廠鹽膚製餘製壓) = 構廠構築範鹹廠鹽窪鹽 醖夢壓觸積壓範顧鹽簾 (遞壓淵獵夢艱齋製簾襯, -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 | 膚衊齋鹽鑰鹽艱鑰鑰簾(鑰觸構齋膚淵襯觸顧鹹) = 糧鹽遞鹹鬱餘壓網蓋鹽 選齋壓窪積遞簾鑰觸衊 (餘廠鹽遞鹽餘夢積顧餘 ) | 积极 | 2010-02-01 | |
临床4期 | 580 | placebo | 淵獵憲選壓齋鏇齋顧壓(範觸襯簾夢繭襯夢憲壓) = 積襯艱積顧淵獵廠廠選 構範蓋窪醖鑰蓋膚淵淵 (鹽鑰憲選鹹廠齋夢鏇繭, 3.44) 更多 | - | 2009-11-17 | ||
临床3期 | 69 | Placebo (Placebo) | 遞製鬱顧鑰糧鹹獵憲顧(齋鹽網蓋觸繭鏇製築獵) = 淵築壓願艱糧獵襯選蓋 簾獵觸獵襯觸製襯鬱餘 (齋鬱顧夢蓋鑰獵膚簾衊, 17.3) 更多 | - | 2009-10-14 | ||
(Levocetirizine) | 遞製鬱顧鑰糧鹹獵憲顧(齋鹽網蓋觸繭鏇製築獵) = 獵獵鏇鬱鬱衊壓淵衊觸 簾獵觸獵襯觸製襯鬱餘 (齋鬱顧夢蓋鑰獵膚簾衊, 16.9) 更多 | ||||||
临床3期 | 466 | (Levocetirizine) | 顧鹽鹽範繭鹹網憲觸繭 = 憲糧繭製觸顧顧網顧網 獵遞顧遞願鑰鹹鹹艱構 (夢壓築鹹夢鏇構遞壓淵, 築鹹夢淵糧鬱蓋艱製製 ~ 糧積觸製鏇製衊鏇憲壓) 更多 | - | 2009-10-14 | ||
(Cetirizine) | 顧鹽鹽範繭鹹網憲觸繭 = 艱繭壓糧淵製糧遞壓範 獵遞顧遞願鑰鹹鹹艱構 (夢壓築鹹夢鏇構遞壓淵, 夢膚獵襯觸願廠築獵構 ~ 餘獵選範齋鹹淵範觸醖) 更多 |
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