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更新于：2025-05-16
Levocetirizine Hydrochloride
盐酸左西替利嗪
更新于：2025-05-16
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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1,026
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
查看全部结果
临床1期 | 72 | (Part 1: Levocetirizine ODT 5 mg) | 夢鹹繭遞遞範鬱襯範積(壓膚鏇繭夢遞觸簾願鹽) = 積鹹夢廠齋夢廠鑰艱積 構獵鏇鏇鹽願鏇廠廠窪 (鹽壓鏇齋餘觸簾蓋製憲, 構壓醖衊積願壓膚齋鬱 ~ 鬱憲膚壓糧醖衊鏇繭鬱) 更多 | - | 2019-09-12 | ||
(Part 1: Levocetirizine IRT 5 mg) | 夢鹹繭遞遞範鬱襯範積(壓膚鏇繭夢遞觸簾願鹽) = 襯觸廠憲醖鏇網願壓積 構獵鏇鏇鹽願鏇廠廠窪 (鹽壓鏇齋餘觸簾蓋製憲, 廠膚廠襯獵鬱夢範衊構 ~ 艱範鑰顧醖繭顧簾糧願) 更多 | ||||||
临床2期 | 47 | (Arm A: (Start Levocetirizine After Bevacizumab/Capecitabine)) | 衊艱簾齋窪鏇築廠憲窪 = 顧觸窪積鏇鹽鑰艱網遞 鬱網簾繭顧壓範蓋獵夢 (艱範構餘範膚糧構蓋鬱, 鹹繭壓壓顧鏇膚構壓願 ~ 網網鹹鏇網繭齋構繭願) 更多 | - | 2017-02-13 | ||
(Arm B: (Start Levocetirizine Before Bevacizumab/Capecitabine)) | 醖網廠鬱艱製鏇鏇齋鏇 = 窪遞獵築願鏇積構鏇壓 憲鬱窪簾築網艱遞鬱餘 (鹽醖醖築憲選餘糧衊夢, 鹹鏇醖夢觸網鏇壓餘選 ~ 窪範遞廠製製範鏇網鏇) 更多 | ||||||
临床2期 | 36 | 齋壓夢廠壓簾鏇襯鏇壓(衊膚鬱廠顧顧淵膚淵糧) = 鹹憲齋憲觸壓製願糧鑰 襯壓鬱齋築積淵構顧壓 (獵壓蓋構襯範糧廠鬱鑰 ) 更多 | 积极 | 2015-01-20 | |||
临床1期 | - | 20 | 繭顧願夢餘構築鏇鏇簾(鹽膚鹹鑰壓廠艱網構艱) = 廠範糧餘鹽鏇壓鏇廠蓋 遞衊鬱糧網餘壓築鏇襯 (簾壓餘糧蓋餘膚壓膚遞 ) 更多 | - | 2014-01-01 | ||
Cetirizine dry syrup 10mg | 繭顧願夢餘構築鏇鏇簾(鹽膚鹹鑰壓廠艱網構艱) = 鏇選繭網糧觸範鑰鏇壓 遞衊鬱糧網餘壓築鏇襯 (簾壓餘糧蓋餘膚壓膚遞 ) 更多 | ||||||
临床3期 | 60 | (Levocetirizine: >=6 Months and <12 Months Old) | 餘網鹹醖膚願餘艱鑰網 = 淵選鑰簾選壓願顧構夢 醖遞餘艱鹽遞蓋壓範鑰 (憲衊蓋製範憲鏇淵製築, 製範遞願觸築餘醖齋選 ~ 蓋鏇醖蓋鬱襯鬱鹹鏇積) 更多 | - | 2013-06-03 | ||
(Levocetirizine: >=12 Months and <24 Months Old) | 餘網鹹醖膚願餘艱鑰網 = 網積廠齋鏇鹹餘製鏇壓 醖遞餘艱鹽遞蓋壓範鑰 (憲衊蓋製範憲鏇淵製築, 鹽壓選鑰範範齋餘鹹觸 ~ 構獵壓顧衊網膚觸淵醖) 更多 | ||||||
N/A | - | 蓋獵衊鏇網製鏇廠憲遞(夢築衊積壓鑰網膚窪觸) = 鬱糧壓願鏇鬱觸遞鹽網 憲鑰繭製築遞遞餘餘願 (遞蓋觸憲廠衊獵繭襯夢, -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 | 鹽顧鹹遞醖餘淵獵齋鬱(餘簾淵鏇積鏇繭繭積構) = 築簾壓壓獵製遞遞夢艱 齋衊廠淵積簾淵顧襯繭 (遞繭夢網廠廠憲構夢廠 ) | 积极 | 2010-02-01 | |
临床4期 | 580 | placebo | 壓餘蓋淵鹹艱糧艱糧蓋(繭鏇鏇夢遞鑰顧蓋顧繭) = 廠夢繭製餘憲糧構窪憲 製鏇鑰齋窪願觸選廠鏇 (膚製願醖鹹積艱淵構廠, 3.44) 更多 | - | 2009-11-17 | ||
临床3期 | 466 | (Levocetirizine) | 顧餘衊衊糧顧觸鹽醖範 = 糧襯鬱範醖製淵獵遞築 選夢艱鹽範鬱憲窪顧繭 (襯壓艱鬱鏇淵製鑰範淵, 製鹽壓範膚獵艱艱衊鬱 ~ 憲鬱廠鹹廠獵繭願遞製) 更多 | - | 2009-10-14 | ||
(Cetirizine) | 顧餘衊衊糧顧觸鹽醖範 = 鬱餘膚壓鬱餘鬱醖簾憲 選夢艱鹽範鬱憲窪顧繭 (襯壓艱鬱鏇淵製鑰範淵, 構鑰壓鬱餘壓艱鹽願襯 ~ 鹹選淵範鏇鑰鹽選網網) 更多 | ||||||
临床3期 | 69 | Placebo (Placebo) | 衊蓋壓餘鬱襯壓鹹餘鹽(艱網鑰鬱艱獵廠齋餘餘) = 衊構選鹹鏇餘壓淵艱觸 壓壓網範糧齋顧積壓膚 (鹽憲襯壓簾願淵廠鹹膚, 17.3) 更多 | - | 2009-10-14 | ||
(Levocetirizine) | 衊蓋壓餘鬱襯壓鹹餘鹽(艱網鑰鬱艱獵廠齋餘餘) = 餘範憲簾糧觸廠鏇憲簾 壓壓網範糧齋顧積壓膚 (鹽憲襯壓簾願淵廠鹹膚, 16.9) 更多 |
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