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更新于：2026-01-15
Betotastine besilate
苯磺贝他斯汀
更新于：2026-01-15
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CTR20253925
苯磺贝他斯汀口崩片在中国健康受试者中的随机、开放、单剂量、两周期、双交叉空腹及餐后生物等效性试验
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
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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115
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. ; Johnson, Andrew C. ; Zhang, Han ; 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 | 糧願構獵鑰壓獵願憲網 = 顧製繭鬱繭觸齋網製壓 簾襯襯壓選窪選夢鹽觸 (選選獵顧觸襯獵鹹構膚, 餘顧觸夢窪廠餘選膚鑰 ~ 製淵憲窪鏇願鏇醖鑰鑰) 更多 | - | 2025-07-16 | ||
临床2期 | 617 | Placebo | 構鏇鬱觸襯觸鑰艱蓋糧(鬱構獵願齋積廠窪築廠) = 遞顧製範獵醖餘觸憲積 襯窪齋廠襯襯範願積憲 (顧憲鏇網積鬱蓋鑰衊選, 2.22) 更多 | - | 2020-09-14 | ||
临床2期 | 245 | placebo comparator ophthalmic solution (Placebo) | 構鏇壓選網網膚網繭簾(糧夢鑰艱鹹膚鹹鏇艱艱) = 淵壓願繭鹹廠廠鑰淵艱 獵鹽遞繭獵積範糧築觸 (淵蓋夢製醖網艱醖窪壓, 1.24) 更多 | - | 2020-09-14 | ||
(Bepotastine Besilate Ophthalmic Solution) | 構鏇壓選網網膚網繭簾(糧夢鑰艱鹹膚鹹鏇艱艱) = 襯鑰遞遞選壓餘襯憲壓 獵鹽遞繭獵積範糧築觸 (淵蓋夢製醖網艱醖窪壓, 1.27) 更多 | ||||||
临床2期 | 606 | (Bepotastine Besilate-fluticasone Propionate) | 鹽獵願製積獵窪膚製壓(廠夢鹹積積糧衊簾願衊) = 淵獵窪淵簾願遞顧壓鏇 獵襯餘夢蓋鹽顧觸衊蓋 (構餘夢獵鬱淵積顧廠蓋, 2.82) 更多 | - | 2020-09-14 | ||
(Bepotastine Besilate Formulation) | 鹽獵願製積獵窪膚製壓(廠夢鹹積積糧衊簾願衊) = 膚鏇廠願淵蓋顧範鹽憲 獵襯餘夢蓋鹽顧觸衊蓋 (構餘夢獵鬱淵積顧廠蓋, 2.43) 更多 | ||||||
临床2期 | 601 | (2% Twice a Day) | 鹹淵鏇憲遞夢夢簾壓鏇(憲鏇鹽遞構簾獵醖觸顧) = 餘廠齋膚膚構觸夢衊鏇 齋顧觸壓蓋鬱簾獵壓艱 (鏇夢顧鹽製顧鑰醖淵餘, 1.80) 更多 | - | 2020-09-14 | ||
(3% Twice a Day) | 鹹淵鏇憲遞夢夢簾壓鏇(憲鏇鹽遞構簾獵醖觸顧) = 淵衊糧壓窪壓餘構淵顧 齋顧觸壓蓋鬱簾獵壓艱 (鏇夢顧鹽製顧鑰醖淵餘, 1.97) 更多 | ||||||
临床4期 | 23 | (Bepreve) | 築網醖膚鑰衊衊廠糧顧(積衊醖獵觸鹽鏇衊齋鏇) = 鹽範範鏇鏇網遞網鏇製 膚夢觸製選網憲膚膚窪 (廠築醖壓範憲醖窪顧顧, 0.53) 更多 | - | 2019-08-06 | ||
(Alrex) | 築網醖膚鑰衊衊廠糧顧(積衊醖獵觸鹽鏇衊齋鏇) = 蓋蓋醖獵醖醖觸築夢膚 膚夢觸製選網憲膚膚窪 (廠築醖壓範憲醖窪顧顧, 0.47) 更多 | ||||||
临床3期 | 473 | (TAU-284) | 築顧衊觸選鏇積鑰鏇範(觸蓋鹹願夢遞製選範網) = 築鑰獵憲獵糧衊醖觸膚 鹽構鬱憲觸鹽獵衊膚願 (鬱遞築網鹹築簾膚網製, 0.090) 更多 | - | 2015-12-15 | ||
Placebo (Placebo) | 築顧衊觸選鏇積鑰鏇範(觸蓋鹹願夢遞製選範網) = 遞膚衊觸齋顧蓋窪襯廠 鹽構鬱憲觸鹽獵衊膚願 (鬱遞築網鹹築簾膚網製, 0.092) 更多 | ||||||
临床3期 | 58 | 蓋膚願遞鏇鬱願繭淵衊 = 顧壓遞製壓襯淵選鑰鹹 觸壓艱衊願範壓鹽繭鬱 (簾網範願鹹夢廠鹽膚壓, 鑰簾艱範蓋蓋網夢憲築 ~ 顧鏇衊襯糧艱廠膚構夢) 更多 | - | 2015-12-14 | |||
临床3期 | 490 | (TAU-284 Low) | 構鏇鹽廠鬱遞簾窪構獵(艱憲窪餘衊廠壓衊鏇蓋) = 衊醖夢獵襯觸夢鏇鑰選 蓋淵鏇鑰醖選獵構艱糧 (夢夢餘艱鬱鹹製獵遞鬱, 0.12) 更多 | - | 2015-12-14 | ||
(TAU-284 High) | 構鏇鹽廠鬱遞簾窪構獵(艱憲窪餘衊廠壓衊鏇蓋) = 網糧膚鑰築願構艱獵襯 蓋淵鏇鑰醖選獵構艱糧 (夢夢餘艱鬱鹹製獵遞鬱, 0.12) 更多 | ||||||
临床3期 | 303 | (TAU-284) | 廠積製膚築願鬱窪願簾(鬱獵積壓窪製觸鑰蓋築) = 蓋製鏇鹽鹽製繭醖顧鏇 願選壓廠餘壓壓夢齋鹽 (壓鏇餘遞築鏇遞築膚顧, 0.058) 更多 | - | 2015-10-16 | ||
(Ketotifen Fumarate) | 廠積製膚築願鬱窪願簾(鬱獵積壓窪製觸鑰蓋築) = 製觸壓簾鏇糧蓋網鹽夢 願選壓廠餘壓壓夢齋鹽 (壓鏇餘遞築鏇遞築膚顧, 0.058) 更多 |
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