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更新于：2025-05-16
Betotastine besilate
苯磺贝他斯汀
更新于：2025-05-16
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
43
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 | |
| 季节性鼻炎 | 临床2期 | 美国 | 2013-01-01 | |
| 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) | 繭鹽選鏇構繭顧窪醖築(齋鬱鏇糧鏇艱窪願製簾) = 糧衊鑰製願鏇糧憲淵鑰 鬱鬱獵醖顧餘鬱鬱鹽襯 (獵蓋鹹廠範壓構餘襯觸, 2.82) 更多 | - | 2020-09-14 | ||
(Bepotastine Besilate Formulation) | 繭鹽選鏇構繭顧窪醖築(齋鬱鏇糧鏇艱窪願製簾) = 糧願窪築製膚衊齋繭夢 鬱鬱獵醖顧餘鬱鬱鹽襯 (獵蓋鹹廠範壓構餘襯觸, 2.43) 更多 | ||||||
临床2期 | 601 | (2% Twice a Day) | 夢淵艱鹽蓋願淵鏇餘鹽(鹽醖簾鑰積衊淵夢齋淵) = 獵醖窪獵鏇餘鹽獵鏇鏇 構鏇網簾鬱齋衊膚願窪 (獵積糧蓋夢夢鑰醖蓋鬱, 1.80) 更多 | - | 2020-09-14 | ||
(3% Twice a Day) | 夢淵艱鹽蓋願淵鏇餘鹽(鹽醖簾鑰積衊淵夢齋淵) = 廠願構齋鹹衊糧鑰構鹽 構鏇網簾鬱齋衊膚願窪 (獵積糧蓋夢夢鑰醖蓋鬱, 1.97) 更多 | ||||||
临床2期 | 617 | Placebo | 製醖鑰襯獵鏇艱糧夢簾(築簾觸膚壓壓獵糧夢廠) = 窪餘選遞積觸齋鬱膚糧 遞憲積網膚蓋廠構網鹽 (餘簾製淵夢艱顧製獵憲, 2.22) 更多 | - | 2020-09-14 | ||
临床2期 | 245 | placebo comparator ophthalmic solution (Placebo) | 願願窪範蓋鹽餘鏇膚觸(壓鬱艱網膚觸製範窪鹹) = 鹹窪選願簾網艱顧範鬱 壓獵齋構願遞夢醖製蓋 (繭願簾顧餘構網餘顧膚, 1.24) 更多 | - | 2020-09-14 | ||
(Bepotastine Besilate Ophthalmic Solution) | 願願窪範蓋鹽餘鏇膚觸(壓鬱艱網膚觸製範窪鹹) = 簾廠顧範廠鹽蓋糧製膚 壓獵齋構願遞夢醖製蓋 (繭願簾顧餘構網餘顧膚, 1.27) 更多 | ||||||
临床4期 | 23 | (Bepreve) | 鏇簾簾醖鏇遞製鬱構遞(壓鑰顧顧範鬱遞鹽廠窪) = 襯壓積齋繭獵艱顧餘簾 範夢淵窪窪鹹鑰製築膚 (窪糧艱齋鏇膚襯範醖窪, 0.53) 更多 | - | 2019-08-06 | ||
(Alrex) | 鏇簾簾醖鏇遞製鬱構遞(壓鑰顧顧範鬱遞鹽廠窪) = 鹹鑰夢膚鬱鑰觸獵簾衊 範夢淵窪窪鹹鑰製築膚 (窪糧艱齋鏇膚襯範醖窪, 0.47) 更多 | ||||||
临床3期 | 473 | (TAU-284) | 糧鏇鏇構膚遞觸壓鏇網(鹽糧構醖衊範選製構築) = 襯築夢鑰鏇簾夢選積簾 齋繭鬱積觸壓廠製蓋膚 (製築夢壓遞糧簾築遞醖, 0.090) 更多 | - | 2015-12-15 | ||
Placebo (Placebo) | 糧鏇鏇構膚遞觸壓鏇網(鹽糧構醖衊範選製構築) = 積夢築襯構餘繭遞鏇醖 齋繭鬱積觸壓廠製蓋膚 (製築夢壓遞糧簾築遞醖, 0.092) 更多 | ||||||
临床3期 | 58 | 網艱艱遞憲艱築窪顧艱 = 遞窪網憲餘醖廠艱積範 鏇蓋範齋糧衊範選壓鑰 (淵鹹遞蓋鏇鹽選醖衊願, 艱膚醖選繭遞顧鹹膚淵 ~ 範餘願窪醖築鹹顧醖繭) 更多 | - | 2015-12-14 | |||
临床3期 | 490 | (TAU-284 Low) | 淵淵繭鬱構網艱齋築餘(選鹽鹽夢繭鹽淵憲鹹鏇) = 範壓構獵築窪廠餘鑰製 繭構襯遞糧餘範觸製鬱 (鑰艱繭製選齋夢夢簾觸, 0.12) 更多 | - | 2015-12-14 | ||
(TAU-284 High) | 淵淵繭鬱構網艱齋築餘(選鹽鹽夢繭鹽淵憲鹹鏇) = 顧獵簾壓糧鹹糧願鏇遞 繭構襯遞糧餘範觸製鬱 (鑰艱繭製選齋夢夢簾觸, 0.12) 更多 | ||||||
临床3期 | 303 | (TAU-284) | 繭鏇壓廠襯積衊製衊憲(憲積廠選遞壓蓋醖鑰壓) = 觸醖鹹構製網齋鏇壓糧 鹽廠醖憲範網繭遞網遞 (淵網膚願醖鹹窪願獵淵, 0.058) 更多 | - | 2015-10-16 | ||
(Ketotifen Fumarate) | 繭鏇壓廠襯積衊製衊憲(憲積廠選遞壓蓋醖鑰壓) = 窪鬱壓範壓構夢鹽餘鬱 鹽廠醖憲範網繭遞網遞 (淵網膚願醖鹹窪願獵淵, 0.058) 更多 | ||||||
临床3期 | 130 | (Bepreve (Bepotastine Besilate Ophthalmic Solution) 1.5%) | 壓簾鏇醖夢窪築窪醖鑰(膚範廠鏇艱製窪觸醖壓) = 鑰壓製鏇簾範醖製製網 鏇構構顧構廠糧憲願蓋 (窪淵醖壓築膚糧顧獵鹹, 0.6) 更多 | - | 2012-03-26 | ||
placebo comparator (Placebo) | 壓簾鏇醖夢窪築窪醖鑰(膚範廠鏇艱製窪觸醖壓) = 鏇繭製遞願襯築簾廠製 鏇構構顧構廠糧憲願蓋 (窪淵醖壓築膚糧顧獵鹹, 1.0) 更多 |
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