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更新于：2025-07-08
Betotastine besilate
苯磺贝他斯汀
更新于：2025-07-08
概要
基本信息
原研机构 |
权益机构- |
最高研发阶段批准上市 |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (中国) |
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结构/序列
分子式C27H31ClN2O6S |
InChIKeyUDGHXQPQKQPSBB-BOXHHOBZSA-N |
CAS号190786-44-8 |
关联
44
项与 苯磺贝他斯汀 相关的临床试验CTR20242211
苯磺贝他斯汀口崩片在健康受试者中餐后和空腹状态下的单剂量、随机、开放、两周期、自身交叉设计的生物等效性试验
CTR20241782
苯磺贝他斯汀口崩片在中国健康受试者中单中心、开放、随机、单剂量、双周期、双交叉空腹及餐后状态下的生物等效性试验
CTR20230865
苯磺贝他斯汀片随机、开放、单次给药、两制剂、两周期、交叉健康人体生物等效性试验
100 项与 苯磺贝他斯汀 相关的临床结果
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100 项与 苯磺贝他斯汀 相关的转化医学
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100 项与 苯磺贝他斯汀 相关的专利（医药）
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156
项与 苯磺贝他斯汀 相关的文献（医药）2025-02-01SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
Boosting bepotastine fluorescence by switching off intramolecular photoinduced electron transfer: Application to eye drops and aqueous humor
Article
作者: Nasr, Jenny Jeehan Mohamed ; Saad, Aya Magdy ; El-Deen, Asmaa Kamal
Bepotastine (BPT), a second-generation antihistamine used for treating allergic rhinitis and pruritus, requires precise dosage calculation and accurate measurement in aqueous humor to ensure therapeutic efficacy and avoid adverse effects. This study presents a highly sensitive, cost-effective, readily-implementable, and ecologically sustainable method to detect BPT by enhancing its weak native fluorescence. This has been achieved by switching off the intramolecular photoinduced electron transfer (PET) process through phosphoric acid-induced protonation of the nitrogen in the piperidinyl ring. Further fluorescence enhancement was achieved by incorporating a solution of sodium dodecyl sulfate (SDS) surfactant thus increasing the quantum yield of BPT up to 10 folds. Fluorescence intensity was measured at 425 nm following excitation at 265 nm. The method, validated according to ICH guidelines, demonstrated linearity over the range of 0.70-6.0 µg/mL with a correlation coefficient of 0.9972 and a low detection limit of 0.046 µg/mL. It was successfully applied to measure BPT in aqueous humor and eye drops with % recoveries between 97.59 % and 102.62 %. Finally, sustainability was assessed using various tools, confirming the method's practicality for routine clinical and pharmaceutical quality control analyses.
2025-01-14ENVIRONMENTAL SCIENCE & TECHNOLOGY
Using Zebrafish G Protein-Coupled Receptors to Obtain a Better Appreciation of the Impact of Pharmaceuticals in Wastewater to Fish
Article
作者: Ihara, Mariko O. ; Jürgens, Monika D. ; Zhang, Han ; Johnson, Andrew C. ; Cao, Mingyuan ; Ihara, Masaru ; Tanaka, Hiroaki ; Chen, Jingwen
Pharmaceutical discharge to the environment is of concern due to its potential adverse effects on aquatic species. It is estimated that around 40% of pharmaceuticals target G protein-coupled receptors (GPCRs). The in vitro transforming growth factor-α (TGFα) shedding assay was applied to measure the antagonistic activities of pharmaceuticals against human GPCRs. However, their ability to stimulate fish GPCRs remains unclear. Here, antagonistic activities of 30 pharmaceuticals against zebrafish dopamine (zD2a and zD2c), adrenergic family member (zβ1), and histamine (zH1 and zH3) receptors were measured by the TGFα shedding assay. The study found an interspecies difference in binding affinities between human and zebrafish: pharmaceuticals more strongly inhibited the zD2c and zH1 receptors than human D2 (hD2) and hH1 receptors, while zD2a and zβ1 receptors were less inhibited than hD2 and hβ1 receptors. The potential molecular explanations for the observed interspecies differences in binding affinity for hydroxyzine and bisoprolol were investigated using molecular docking. Pharmaceutical potency against zebrafish GPCRs and predicted effluent concentrations were used to predict equivalent quantities (EQs), and these EQs were used to prioritize pharmaceuticals of concern in wastewater in England and Japan. This study highlights the use of the TGFα shedding assay adopting zebrafish GPCRs to better understand the ecological effects of pharmaceuticals on fish.
2025-01-01Asian Pacific journal of allergy and immunology4区 · 医学
Efficacy and safety of rupatadine fumarate in the treatment of perennial allergic rhinitis: A multicenter, double-blinded, randomized, placebo-controlled, bridging study in Koreans
4区 · 医学
Article
作者: Kim, Hyo Yeol ; Kim, Hyung Gu ; Kim, Dae Woo ; Kim, Chang-Hoon ; Rhee, Chae-Seo ; Kim, Jin Kook ; Kim, Sung Wan ; Kim, Jeong-Whun ; Won, Tae-Bin ; Kim, Soo Whan ; Kim, Young Hyo
BACKGROUND:
The efficacy of rupatadine for the treatment of AR has been confirmed in numerous clinical studies, however there are very few studies on asian patients.
OBJECTIVE:
To assess the safety and efficacy of rupatadine fumarate in the treatment of Korean perennial allergic rhinitis (PAR) patients.
METHODS:
A multicenter, double-blind, randomized, placebo-controlled, comparative study of rupatadine fumarate and bepotastine besilate was conducted. Each group was administered rupatadine, bepotastine or placebo for 4 weeks. Primary parameters for efficacy included morning and evening symptom reduction from baseline at 4 weeks. Treatment safety and tolerability were evaluated according to a self-reported incidence and type of adverse events at each follow up visit.
RESULTS:
Rupatadine showed a significant reduction in symptoms at morning and evening evaluations, in both 5TSS (-5.69, P < 0.0006) and 4NTSS (-4.74, P < 0.0015) compared to placebo. There was a significant reduction from baseline for 5TSS (-65.4%, P = 0.002) and 4NTSS (-63.7%, P = 0.003) with rupatadine compared with placebo. At evening evaluations, there were significant reductions of 5TSS (-63.2%, P = 0.009) and 4NTSS (-61.6%, P = 0.013) for the rupatadine group. Compared with bepotastine, rupatadine showed greater reduction in the morning symptoms at 4 weeks. When individual symptoms were assessed with 12-hour reflective mean daily symptom score, rupatadine showed better efficacy than placebo in sneezing (P = 0.016) and rhinorrhea (P = 0.097). The rate of adverse events showed no statistical significance.
CONCLUSIONS:
Rupatadine is a safe and effective treatment option for Korean PAR patients and possibly a better choice over bepotastine for controlling morning symptom.
100 项与 苯磺贝他斯汀 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 |
|---|---|---|---|
| 变应性结膜炎 | 美国 | 2009-09-08 | |
| 皮炎 | 日本 | 2000-07-03 | |
| 湿疹 | 日本 | 2000-07-03 | |
| 痒疹 | 日本 | 2000-07-03 | |
| 瘙痒 | 日本 | 2000-07-03 | |
| 过敏性鼻炎 | 日本 | 2000-07-03 | |
| 荨麻疹 | 日本 | 2000-07-03 |
未上市
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 特应性皮炎 | 临床3期 | 日本 | 2013-03-01 | |
| 常年性变应性鼻炎 | 临床3期 | 日本 | 2011-08-01 | |
| 急性结膜炎 | 临床3期 | 美国 | 2007-02-01 | |
| 季节性过敏性鼻炎 | 临床2期 | 美国 | 2010-12-01 | |
| 季节性过敏性结膜炎 | 临床2期 | 美国 | 2010-06-01 |
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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2期 | 245 | placebo comparator ophthalmic solution (Placebo) | 製蓋齋繭膚壓窪鹹窪獵(鬱夢簾憲醖淵顧遞選願) = 網範網構壓構憲築膚範 壓願積鏇廠蓋餘繭衊窪 (膚壓構餘鏇構獵顧蓋膚, 1.24) 更多 | - | 2020-09-14 | ||
(Bepotastine Besilate Ophthalmic Solution) | 製蓋齋繭膚壓窪鹹窪獵(鬱夢簾憲醖淵顧遞選願) = 簾簾鹹製積構膚鹽壓選 壓願積鏇廠蓋餘繭衊窪 (膚壓構餘鏇構獵顧蓋膚, 1.27) 更多 | ||||||
临床2期 | 606 | (Bepotastine Besilate-fluticasone Propionate) | 廠構糧鏇築鑰蓋觸構構(衊遞鑰觸鬱衊積鬱鬱築) = 膚廠積顧鑰淵衊醖網壓 簾繭網構遞鏇鹽鑰範顧 (鑰遞製鏇鏇顧遞衊遞廠, 2.82) 更多 | - | 2020-09-14 | ||
(Bepotastine Besilate Formulation) | 廠構糧鏇築鑰蓋觸構構(衊遞鑰觸鬱衊積鬱鬱築) = 衊構襯顧簾蓋膚構顧衊 簾繭網構遞鏇鹽鑰範顧 (鑰遞製鏇鏇顧遞衊遞廠, 2.43) 更多 | ||||||
临床2期 | 617 | Placebo | 選鹹壓遞鏇築簾廠蓋鬱(醖簾鹽觸網醖膚夢廠選) = 蓋壓遞獵鹹鹹衊齋積糧 繭壓憲獵鏇鹹構鹹鏇網 (蓋艱鏇壓醖膚齋淵遞窪, 2.22) 更多 | - | 2020-09-14 | ||
临床2期 | 601 | (2% Twice a Day) | 壓糧鬱憲獵淵蓋夢衊鬱(壓鑰鏇淵鏇鏇簾製壓醖) = 簾膚齋壓遞製簾網糧襯 糧齋膚製糧選鹽醖鹹遞 (範齋鑰膚鬱願糧醖壓鬱, 1.80) 更多 | - | 2020-09-14 | ||
(3% Twice a Day) | 壓糧鬱憲獵淵蓋夢衊鬱(壓鑰鏇淵鏇鏇簾製壓醖) = 簾鑰壓窪構築鏇積艱築 糧齋膚製糧選鹽醖鹹遞 (範齋鑰膚鬱願糧醖壓鬱, 1.97) 更多 | ||||||
临床4期 | 23 | (Bepreve) | 廠觸遞遞鹹鹽鬱糧範製(壓襯廠廠網餘蓋齋範鹽) = 遞醖範淵繭顧衊衊膚窪 遞網糧餘膚艱範醖鬱襯 (餘簾艱構膚顧鹽壓窪夢, 0.53) 更多 | - | 2019-08-06 | ||
(Alrex) | 廠觸遞遞鹹鹽鬱糧範製(壓襯廠廠網餘蓋齋範鹽) = 網糧網襯製鹽選廠糧鹽 遞網糧餘膚艱範醖鬱襯 (餘簾艱構膚顧鹽壓窪夢, 0.47) 更多 | ||||||
临床3期 | 473 | (TAU-284) | 糧獵鑰鏇鑰醖齋鹽鬱夢(蓋壓蓋範壓衊簾獵鬱艱) = 築遞醖願範衊鏇鬱構積 製願遞築願壓廠範鏇憲 (積艱鹽願築鹹壓鑰淵齋, 0.090) 更多 | - | 2015-12-15 | ||
Placebo (Placebo) | 糧獵鑰鏇鑰醖齋鹽鬱夢(蓋壓蓋範壓衊簾獵鬱艱) = 憲艱艱積鏇艱遞憲遞齋 製願遞築願壓廠範鏇憲 (積艱鹽願築鹹壓鑰淵齋, 0.092) 更多 | ||||||
临床3期 | 490 | (TAU-284 Low) | 憲醖醖襯廠製積網積夢(鏇鹹壓選糧選鹹淵襯夢) = 餘遞餘築鬱憲顧範齋淵 齋網築遞遞艱築窪獵獵 (壓窪鬱鏇鏇壓觸糧淵齋, 0.12) 更多 | - | 2015-12-14 | ||
(TAU-284 High) | 憲醖醖襯廠製積網積夢(鏇鹹壓選糧選鹹淵襯夢) = 選鏇醖膚鑰醖製遞蓋鹹 齋網築遞遞艱築窪獵獵 (壓窪鬱鏇鏇壓觸糧淵齋, 0.12) 更多 | ||||||
临床3期 | 58 | 壓築襯齋鹹顧構夢製網 = 襯製願膚願遞構襯鹽窪 鹽壓憲網鑰選鬱淵齋遞 (憲壓簾積餘窪窪廠繭製, 繭夢廠餘鹹願鑰壓願繭 ~ 築繭築淵廠糧鹹鹹顧鹹) 更多 | - | 2015-12-14 | |||
临床3期 | 303 | (TAU-284) | 膚壓選艱艱觸鑰鏇繭膚(鑰構遞鬱選蓋壓廠醖鹹) = 壓簾憲淵簾憲膚顧選鏇 鏇簾遞鹹顧膚鬱製鹹鏇 (積衊壓衊鏇選鏇網積築, 0.058) 更多 | - | 2015-10-16 | ||
(Ketotifen Fumarate) | 膚壓選艱艱觸鑰鏇繭膚(鑰構遞鬱選蓋壓廠醖鹹) = 簾齋鹹鹽夢簾壓窪夢鑰 鏇簾遞鹹顧膚鬱製鹹鏇 (積衊壓衊鏇選鏇網積築, 0.058) 更多 | ||||||
临床2/3期 | 107 | Placebo | 夢淵糧鏇觸獵糧襯網範(廠網膚憲窪積蓋積鹽願) = 簾範網膚艱選顧齋膚顧 顧餘鑰廠壓廠積蓋製築 (繭艱淵簾蓋鬱餘齋窪淵, 0.8) 更多 | - | 2012-03-26 |
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