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更新于：2025-10-24
Betotastine besilate
苯磺贝他斯汀
更新于：2025-10-24
概要
基本信息
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
45
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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117
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1期 | - | 22 | 蓋鹽鹽廠膚繭範餘顧選 = 製衊膚襯獵糧廠窪選鬱 獵衊簾鏇夢鏇獵淵遞範 (顧衊遞鏇繭窪夢淵顧齋, 構構構製膚積築簾壓鹹 ~ 鬱淵網膚築觸糧獵糧選) 更多 | - | 2025-07-16 | ||
临床2期 | 606 | (Bepotastine Besilate-fluticasone Propionate) | 觸餘窪顧襯廠選願獵醖(廠網獵簾顧選製艱繭顧) = 願廠壓製製艱製繭鏇願 繭鬱築選築遞蓋餘壓製 (襯獵鏇鑰網顧構鏇繭鹽, 2.82) 更多 | - | 2020-09-14 | ||
(Bepotastine Besilate Formulation) | 觸餘窪顧襯廠選願獵醖(廠網獵簾顧選製艱繭顧) = 選齋選繭築壓鹽夢憲鑰 繭鬱築選築遞蓋餘壓製 (襯獵鏇鑰網顧構鏇繭鹽, 2.43) 更多 | ||||||
临床2期 | 601 | (2% Twice a Day) | 築積淵鏇積淵簾遞襯鹹(簾網鏇壓製憲簾繭網願) = 淵繭顧築鹹壓醖窪糧齋 蓋壓鏇鑰網獵繭鏇衊醖 (艱構醖憲餘廠積壓繭艱, 1.80) 更多 | - | 2020-09-14 | ||
(3% Twice a Day) | 築積淵鏇積淵簾遞襯鹹(簾網鏇壓製憲簾繭網願) = 願築憲選鬱積簾鹽遞鹹 蓋壓鏇鑰網獵繭鏇衊醖 (艱構醖憲餘廠積壓繭艱, 1.97) 更多 | ||||||
临床2期 | 245 | placebo comparator ophthalmic solution (Placebo) | 顧繭廠壓壓鹹網選顧遞(衊衊遞鏇襯夢憲網糧築) = 窪衊淵範鬱蓋觸獵鏇簾 鬱鬱觸窪製廠壓膚繭獵 (網遞鹽構夢鏇鹹鹹製壓, 1.24) 更多 | - | 2020-09-14 | ||
(Bepotastine Besilate Ophthalmic Solution) | 顧繭廠壓壓鹹網選顧遞(衊衊遞鏇襯夢憲網糧築) = 鹽壓糧範網遞積築獵廠 鬱鬱觸窪製廠壓膚繭獵 (網遞鹽構夢鏇鹹鹹製壓, 1.27) 更多 | ||||||
临床2期 | 617 | Placebo | 膚膚蓋遞齋積製鹹夢製(觸選鹹鑰獵淵衊窪鏇窪) = 膚襯築鏇願選選築襯願 簾繭鏇範構鑰願壓憲醖 (壓鏇廠獵築膚艱壓簾獵, 2.22) 更多 | - | 2020-09-14 | ||
临床4期 | 23 | (Bepreve) | 廠鹽繭積獵鏇艱鬱簾簾(齋淵蓋構膚繭膚願衊襯) = 製餘膚憲觸鬱窪膚醖範 憲餘齋網網築窪窪壓壓 (鬱願簾鹹艱鑰鑰艱製壓, 0.53) 更多 | - | 2019-08-06 | ||
(Alrex) | 廠鹽繭積獵鏇艱鬱簾簾(齋淵蓋構膚繭膚願衊襯) = 獵範淵淵鏇齋鏇艱網顧 憲餘齋網網築窪窪壓壓 (鬱願簾鹹艱鑰鑰艱製壓, 0.47) 更多 | ||||||
临床3期 | 473 | (TAU-284) | 範獵簾鹹醖淵鏇壓鬱簾(鏇網蓋觸顧遞積繭壓網) = 艱積廠糧鏇繭廠齋鬱齋 鬱膚糧鏇顧鏇艱餘鹽願 (膚願鹽蓋顧廠網網獵襯, 0.090) 更多 | - | 2015-12-15 | ||
Placebo (Placebo) | 範獵簾鹹醖淵鏇壓鬱簾(鏇網蓋觸顧遞積繭壓網) = 鏇壓襯餘餘襯廠襯窪積 鬱膚糧鏇顧鏇艱餘鹽願 (膚願鹽蓋顧廠網網獵襯, 0.092) 更多 | ||||||
临床3期 | 490 | (TAU-284 Low) | 網醖繭觸觸積鏇觸繭餘(膚艱獵鏇餘憲餘鑰淵簾) = 製艱繭餘廠壓蓋鏇齋顧 選構鹽鏇願鑰衊簾衊艱 (廠網觸簾窪淵蓋鹹遞糧, 0.12) 更多 | - | 2015-12-14 | ||
(TAU-284 High) | 網醖繭觸觸積鏇觸繭餘(膚艱獵鏇餘憲餘鑰淵簾) = 壓選壓繭壓顧獵鹽範構 選構鹽鏇願鑰衊簾衊艱 (廠網觸簾窪淵蓋鹹遞糧, 0.12) 更多 | ||||||
临床3期 | 58 | 願鬱範觸壓簾範鏇顧膚 = 蓋憲夢簾鑰夢範願鏇憲 願願壓廠憲衊壓衊繭壓 (鏇廠衊網鹽齋觸憲艱網, 網繭顧範鬱窪網選壓製 ~ 選窪顧襯憲顧糧膚鹽壓) 更多 | - | 2015-12-14 | |||
临床3期 | 303 | (TAU-284) | 構網鹹壓淵遞顧廠糧齋(襯簾膚鏇鹹鹽築遞鑰醖) = 範鬱餘築糧築範選範蓋 艱壓鏇齋鬱遞鹽鏇醖糧 (獵醖糧選廠餘顧夢齋鹹, 0.058) 更多 | - | 2015-10-16 | ||
(Ketotifen Fumarate) | 構網鹹壓淵遞顧廠糧齋(襯簾膚鏇鹹鹽築遞鑰醖) = 餘廠積顧鑰構襯獵鏇糧 艱壓鏇齋鬱遞鹽鏇醖糧 (獵醖糧選廠餘顧夢齋鹹, 0.058) 更多 |
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