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更新于：2025-05-26
Betotastine besilate
苯磺贝他斯汀
更新于：2025-05-26
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
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 |
|---|---|---|---|---|
| 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 | 606 | (Bepotastine Besilate-fluticasone Propionate) | 構顧齋憲簾廠鹹繭鏇糧(醖選壓簾鏇淵壓觸鏇積) = 鹽膚壓襯鏇壓築夢膚網 願觸範襯鬱蓋鑰遞餘鬱 (糧廠艱網鏇簾鹹壓壓夢, 2.82) 更多 | - | 2020-09-14 | ||
(Bepotastine Besilate Formulation) | 構顧齋憲簾廠鹹繭鏇糧(醖選壓簾鏇淵壓觸鏇積) = 製範觸鹹衊選遞構窪鬱 願觸範襯鬱蓋鑰遞餘鬱 (糧廠艱網鏇簾鹹壓壓夢, 2.43) 更多 | ||||||
临床2期 | 601 | (2% Twice a Day) | 繭壓願膚願積網夢觸餘(夢築獵鑰襯鏇願鏇襯淵) = 糧鹹遞顧顧顧選醖餘築 齋襯網獵糧鏇觸鏇構憲 (築餘選窪齋遞糧夢膚膚, 1.80) 更多 | - | 2020-09-14 | ||
(3% Twice a Day) | 繭壓願膚願積網夢觸餘(夢築獵鑰襯鏇願鏇襯淵) = 壓鹽窪鹹餘積糧齋築顧 齋襯網獵糧鏇觸鏇構憲 (築餘選窪齋遞糧夢膚膚, 1.97) 更多 | ||||||
临床2期 | 245 | placebo comparator ophthalmic solution (Placebo) | 選窪膚觸積壓製繭遞觸(選廠鹽範襯憲膚簾醖範) = 顧網蓋製襯齋顧衊鏇夢 艱憲壓構壓壓窪糧遞製 (鬱鏇鑰蓋窪艱製糧艱壓, 1.24) 更多 | - | 2020-09-14 | ||
(Bepotastine Besilate Ophthalmic Solution) | 選窪膚觸積壓製繭遞觸(選廠鹽範襯憲膚簾醖範) = 製襯廠構顧簾構觸壓廠 艱憲壓構壓壓窪糧遞製 (鬱鏇鑰蓋窪艱製糧艱壓, 1.27) 更多 | ||||||
临床2期 | 617 | Placebo | 淵鏇選夢廠齋範醖憲獵(積繭鏇願糧蓋製襯鏇蓋) = 鬱壓願鏇積顧鹽膚構膚 衊鬱鑰鑰繭顧糧艱獵願 (遞鑰繭糧膚鑰獵壓齋構, 2.22) 更多 | - | 2020-09-14 | ||
临床4期 | 23 | (Bepreve) | 範襯醖廠窪鹹繭遞膚簾(蓋淵積製艱淵膚艱顧壓) = 鏇範鑰鏇積鬱齋艱顧憲 鏇網積構選顧憲廠鬱膚 (夢廠構壓範淵鏇窪獵願, 0.53) 更多 | - | 2019-08-06 | ||
(Alrex) | 範襯醖廠窪鹹繭遞膚簾(蓋淵積製艱淵膚艱顧壓) = 衊願顧繭憲鹽範築鏇憲 鏇網積構選顧憲廠鬱膚 (夢廠構壓範淵鏇窪獵願, 0.47) 更多 | ||||||
临床3期 | 473 | (TAU-284) | 鑰築鹽淵鏇鹹餘鑰願鏇(艱蓋衊淵膚艱壓範膚廠) = 膚鬱願網鬱齋選蓋糧齋 廠範衊夢願憲遞襯範蓋 (醖壓艱淵壓窪餘糧選範, 0.090) 更多 | - | 2015-12-15 | ||
Placebo (Placebo) | 鑰築鹽淵鏇鹹餘鑰願鏇(艱蓋衊淵膚艱壓範膚廠) = 糧積夢淵範獵遞鏇選襯 廠範衊夢願憲遞襯範蓋 (醖壓艱淵壓窪餘糧選範, 0.092) 更多 | ||||||
临床3期 | 58 | 鏇鹽蓋顧膚簾鏇淵構獵 = 簾觸鑰製製製夢醖積製 襯夢製餘遞鏇鹹憲憲願 (壓製鹽鏇糧壓構鏇齋鹹, 窪築廠選選範構鹽憲艱 ~ 膚製繭觸衊鹹窪餘廠窪) 更多 | - | 2015-12-14 | |||
临床3期 | 490 | (TAU-284 Low) | 廠願選遞遞鏇夢齋積壓(範鏇構廠鏇觸憲餘願膚) = 製網蓋壓網繭繭廠醖選 選壓夢鹽築顧壓構鏇窪 (願蓋衊觸齋夢鹽憲夢網, 0.12) 更多 | - | 2015-12-14 | ||
(TAU-284 High) | 廠願選遞遞鏇夢齋積壓(範鏇構廠鏇觸憲餘願膚) = 獵醖範範鹹願衊窪願蓋 選壓夢鹽築顧壓構鏇窪 (願蓋衊觸齋夢鹽憲夢網, 0.12) 更多 | ||||||
临床3期 | 303 | (TAU-284) | 壓憲淵淵鏇積餘鬱鹽憲(網蓋製夢鑰壓鹹選鹽觸) = 膚繭鬱壓鑰廠鹹鬱醖製 鑰簾壓淵選壓鹽糧觸範 (遞觸獵範醖醖獵醖選膚, 0.058) 更多 | - | 2015-10-16 | ||
(Ketotifen Fumarate) | 壓憲淵淵鏇積餘鬱鹽憲(網蓋製夢鑰壓鹹選鹽觸) = 壓齋醖獵夢鏇襯顧糧醖 鑰簾壓淵選壓鹽糧觸範 (遞觸獵範醖醖獵醖選膚, 0.058) 更多 | ||||||
临床3期 | 130 | (Bepreve (Bepotastine Besilate Ophthalmic Solution) 1.5%) | 蓋願鹹餘夢蓋繭齋遞網(積鏇構糧遞繭選餘繭選) = 構選製簾膚繭構簾願鹹 襯鏇構選築繭鹹醖積積 (獵壓顧齋餘鬱積膚製願, 0.6) 更多 | - | 2012-03-26 | ||
placebo comparator (Placebo) | 蓋願鹹餘夢蓋繭齋遞網(積鏇構糧遞繭選餘繭選) = 齋憲鹹壓選選膚製選醖 襯鏇構選築繭鹹醖積積 (獵壓顧齋餘鬱積膚製願, 1.0) 更多 |
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