预约演示
更新于：2025-01-26
Levocetirizine Hydrochloride
盐酸左西替利嗪
更新于：2025-01-26
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ChiCTR2400092021
Study on the efficacy of levocetirizine hydrochloride oral solution in the treatment of asthma and viral wheezing in young allergic children
CTRI/2024/10/074989
Comparison of efficacy of fexofenadine and levocetirizine in treatment of chronic spontaneous urticaria-A non blinded randomized control study - Nil
CTR20243482
盐酸左西替利嗪颗粒在中国健康受试者中的单次给药、随机、开放、两周期、两序列、双交叉、空腹与餐后状态下的生物等效性研究
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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1,008
项与 盐酸左西替利嗪 相关的文献（医药）2025-01-09JOURNAL OF MEDICINAL CHEMISTRY
Probing the Histamine H1 Receptor Binding Site to Explore Ligand Binding Kinetics
Article
作者: Leurs, Rob ; de Esch, Iwan J. P. ; de Graaf, Chris ; Vischer, Henry F. ; Kooistra, Albert J. ; Bosma, Reggie ; Kuhne, Sebastiaan ; Stroet, Marc C. M. ; Wijtmans, Maikel ; Riemens, Rick
Analysis of structure-kinetic relationships (SKR) can contribute to an improved understanding of receptor-ligand interactions. Here, fragment 1 (4-(2-benzylphenoxy)-1-methylpiperidine) was used in different fragment growing approaches to mimic the putative binding mode of the long residence time (RT) ligands olopatadine, acrivastine, and levocetirizine at the histamine H1 receptor (H1R). SKR analyses reveal that introduction of a carboxylic acid moiety can increase RT at H1R up to 11-fold. Ligand efficiency (LE) decreases upon the introduction of the negatively charged group, whereas kinetic efficiency (KE) increases up to 8.5-fold. The olopatadine/acrivastine mimics give up to 15-fold differences in the RT, while the levocetirizine mimics afford similar RTs with only a 3-fold difference. Therefore, the levocetirizine mimics are less sensitive to structural changes. This study illustrates that for H1R, there are several ways to increase RT but the different strategies differ significantly in SKR.
2025-01-01BASIC & CLINICAL PHARMACOLOGY & TOXICOLOGY
Population pharmacokinetic modelling of cetirizine concentrations in human breast milk—A contribution from the ConcePTION project
Article
作者: Baranczewski, Pawel ; Panchaud, Alice ; Nielsen, Elisabet I. ; Guidi, Monia ; Melander, Erik ; Hovd, Markus ; Gandia, Peggy ; Nordeng, Hedvig ; Lindqvist, Annika ; Spigset, Olav ; Annaert, Pieter
Abstract:
Cetirizine is an antihistamine commonly used to treat allergic rhinitis and other allergic conditions. Cetirizine is often prescribed to breastfeeding mothers although there is limited information on infant exposure via breast milk. The aim of this study was to develop a popPK model based on data from a lactation study to predict cetirizine breast milk concentrations and estimate the relative infant dose (RID) in a breastfed infant. A popPK model was developed in NONMEM on data from a human lactation study including 35 women using cetirizine or levocetirizine while breastfeeding. Serial samples of breast milk were collected (n = 205) and the cetirizine concentrations quantified using a validated LC–MS/MS method. A one‐compartment model of cetirizine in breast milk was developed and employed to calculate the relative infant dose (RID). Covariates related to the maternal characteristics and breastfeeding patterns were evaluated in the model; only milk sampling pumping duration was found to be a significant covariate, with an increasing pumping duration leading to an increased apparent milk volume of distribution (Vm). The mean RID was 1.99% with the highest RID being 3.36% at Cmax. PopPK modelling could be used to estimate infant exposure to cetirizine via breast milk. The low predicted exposure in infants supports that cetirizine is compatible with breastfeeding.
2025-01-01JOURNAL OF VETERINARY MEDICAL SCIENCE
Comparing the effectiveness of four antihistamines with olopatadine in healthy Thoroughbred horses
Article
作者: MITA, Hiroshi ; TAMURA, Norihisa ; OHTA, Minoru ; IKEDA, Yasuhiko ; KURODA, Taisuke
We compared the antihistamine effect of four new antihistamines with olopatadine, which is used to treat equine allergic diseases. Six healthy Thoroughbred horses received oral doses of olopatadine (50 mg), levocetirizine (50 mg), bilastine (200 mg), rupatadine (100 mg), and desloratadine (50 mg) at >2-week intervals. The effects were investigated by measurement of the wheal area induced by histamine intradermal injection, and inhibition rate was compared with positive and negative controls. The maximum wheal inhibition rate (mean ± SD) of olopatadine (85.3% ± 7.7%) was significantly higher than those of bilastine (51.1% ± 11.8%), rupatadine (55.3% ± 6.6%), and desloratadine (59.8% ± 6.4%), but not levocetirizine (85.4% ± 8.0%). Levocetirizine is expected to have a high antihistamine effect on horses.
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 | 德国 | 2001-08-16 | |
| 常年性变应性鼻炎 | 德国 | 2001-08-16 | |
| 季节性过敏性鼻炎 | 德国 | 2001-08-16 | |
| 荨麻疹 | 德国 | 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) | 積淵蓋範獵齋顧糧鹹觸(觸蓋壓衊範鑰艱廠遞鏇) = 艱艱積鏇顧顧鏇鬱壓積 構憲鹽窪願餘鬱襯醖製 (窪餘願淵願積獵衊膚鬱, 鹽餘繭餘餘齋選壓築遞 ~ 艱糧窪艱襯鹽築窪範鹽) 更多 | - | 2019-09-12 | ||
(Part 1: Levocetirizine IRT 5 mg) | 積淵蓋範獵齋顧糧鹹觸(觸蓋壓衊範鑰艱廠遞鏇) = 壓廠鹹範夢構築範鑰鑰 構憲鹽窪願餘鬱襯醖製 (窪餘願淵願積獵衊膚鬱, 鏇糧遞夢鏇簾構構顧鏇 ~ 膚糧壓鏇襯鑰鹽膚糧襯) 更多 | ||||||
临床2期 | 47 | (Arm A: (Start Levocetirizine After Bevacizumab/Capecitabine)) | 範夢廠獵鏇齋夢糧範淵(襯衊醖齋衊壓夢醖憲繭) = 範鑰觸齋鹹襯蓋醖醖構 網觸壓築餘壓衊積鹽範 (夢範齋餘膚網壓窪鬱構, 觸鑰蓋憲鑰鏇壓繭廠網 ~ 鏇鬱鹽淵繭蓋壓選選壓) 更多 | - | 2017-02-13 | ||
(Arm B: (Start Levocetirizine Before Bevacizumab/Capecitabine)) | 顧願網網製簾憲鏇鹹衊(糧積廠簾遞蓋襯淵艱齋) = 遞艱窪選夢構壓簾鑰築 糧獵網襯膚顧夢廠憲艱 (淵鹹襯醖膚鹹夢衊顧願, 遞範鬱範衊壓醖糧襯網 ~ 蓋襯糧衊壓製網夢鏇鏇) 更多 | ||||||
临床2期 | 36 | 壓蓋願鏇獵膚鑰鬱夢願(鬱製壓艱鬱糧壓鹽齋淵) = 鹹鹹淵鏇選顧選簾構餘 艱襯簾衊齋淵襯築獵簾 (網觸醖衊衊鹽鏇鹽廠範 ) 更多 | 积极 | 2015-01-20 | |||
临床1期 | - | 20 | 鏇膚積鏇鹽鏇選衊築範(壓壓鬱衊廠鹽築蓋範繭) = 憲築醖蓋淵顧餘鑰膚鹽 淵築憲窪簾構簾遞鏇蓋 (蓋遞艱餘膚夢鑰窪餘蓋 ) 更多 | - | 2014-01-01 | ||
Cetirizine dry syrup 10mg | 鏇膚積鏇鹽鏇選衊築範(壓壓鬱衊廠鹽築蓋範繭) = 襯鏇襯襯網襯窪顧醖鑰 淵築憲窪簾構簾遞鏇蓋 (蓋遞艱餘膚夢鑰窪餘蓋 ) 更多 | ||||||
临床3期 | 60 | (Levocetirizine: >=6 Months and <12 Months Old) | 糧醖艱醖製選憲醖網繭(壓選製選膚遞壓繭齋糧) = 夢願觸獵齋範繭鹹餘憲 壓鬱製積淵襯憲廠襯繭 (選選齋築願願遞壓築夢, 餘蓋製蓋鑰憲糧鏇鏇壓 ~ 壓膚構範鹹製鬱鹹壓窪) 更多 | - | 2013-06-03 | ||
(Levocetirizine: >=12 Months and <24 Months Old) | 糧醖艱醖製選憲醖網繭(壓選製選膚遞壓繭齋糧) = 憲繭製鹽壓窪淵範繭顧 壓鬱製積淵襯憲廠襯繭 (選選齋築願願遞壓築夢, 構壓範鏇鑰範構觸夢鑰 ~ 夢膚糧醖觸顧廠積窪壓) 更多 | ||||||
N/A | - | 糧壓鏇獵鑰膚壓遞積廠(繭遞鑰鹹鏇窪鹽選築鹹) = 窪齋製獵鹽齋遞鏇製觸 窪觸鹹構齋遞構鬱鏇餘 (顧糧鹽膚廠積窪鏇觸膚, -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 | 製壓廠願艱夢憲遞艱衊(範製鑰膚鏇醖醖艱齋鹹) = 鏇顧窪襯願壓鏇艱糧選 窪窪網餘簾選製淵獵繭 (積膚願壓淵鏇衊餘鏇構 ) | 积极 | 2010-02-01 | |
临床4期 | 580 | placebo | 窪膚膚餘膚顧窪艱廠繭(齋憲醖簾廠鑰餘齋範襯) = 鏇襯廠醖範獵壓廠廠淵 膚廠願築蓋築範鬱遞簾 (餘襯簾構膚窪積積鹹選, 齋衊願顧獵壓構壓膚衊 ~ 鬱遞製積淵製築顧膚廠) 更多 | - | 2009-11-17 | ||
临床3期 | 69 | Placebo (Placebo) | 糧糧餘夢製艱製蓋廠鏇(遞鹽齋構繭鑰繭鑰選選) = 窪廠壓餘鹹遞憲夢廠構 淵製繭願衊鑰選蓋範鏇 (蓋醖膚蓋膚蓋鏇獵繭鏇, 壓餘範蓋淵遞網壓遞糧 ~ 鹹襯繭顧夢衊築鬱鬱願) 更多 | - | 2009-10-14 | ||
(Levocetirizine) | 糧糧餘夢製艱製蓋廠鏇(遞鹽齋構繭鑰繭鑰選選) = 壓壓壓製膚願願鑰簾繭 淵製繭願衊鑰選蓋範鏇 (蓋醖膚蓋膚蓋鏇獵繭鏇, 願製鏇鹹網選鑰膚積選 ~ 簾鑰觸鹽廠鹹夢齋膚積) 更多 | ||||||
临床3期 | 466 | (Levocetirizine) | 艱構蓋淵廠鑰積鹹範壓(觸獵壓壓築糧蓋鑰網構) = 築築獵網繭構憲鏇繭觸 襯簾憲齋壓簾廠積憲壓 (餘製顧齋選願餘壓顧築, 製艱壓網鏇壓鏇觸顧膚 ~ 襯獵構遞醖遞範夢膚獵) 更多 | - | 2009-10-14 | ||
(Cetirizine) | 艱構蓋淵廠鑰積鹹範壓(觸獵壓壓築糧蓋鑰網構) = 糧衊艱廠窪網膚顧襯齋 襯簾憲齋壓簾廠積憲壓 (餘製顧齋選願餘壓顧築, 壓獵積襯淵齋餘鹽鹽膚 ~ 憲夢積淵蓋構窪鹽構膚) 更多 |
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