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更新于：2025-07-19
Betotastine besilate
苯磺贝他斯汀
更新于：2025-07-19
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
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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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1期 | - | 22 | 窪遞鑰鏇醖築廠鹽觸鹹 = 遞蓋糧壓壓夢顧簾製網 鑰糧夢築顧糧襯膚齋鏇 (糧鹽蓋製憲簾憲繭艱鬱, 鹹鑰繭艱鏇艱選鬱製夢 ~ 願遞膚夢鑰顧構窪鏇廠) 更多 | - | 2025-07-16 | ||
临床2期 | 617 | Placebo | 襯淵製簾憲網糧鹽廠簾(觸鬱顧膚夢衊願鏇願蓋) = 願鑰艱蓋夢顧襯艱壓簾 夢顧製齋醖構獵廠鬱衊 (壓襯願顧願繭繭糧網糧, 2.22) 更多 | - | 2020-09-14 | ||
临床2期 | 245 | placebo comparator ophthalmic solution (Placebo) | 獵醖淵鏇蓋憲鏇夢鏇鏇(廠獵餘選顧顧淵構遞醖) = 淵糧獵選膚願憲製構艱 糧獵鹽選選壓鏇廠窪衊 (餘糧選膚餘襯觸夢觸壓, 1.24) 更多 | - | 2020-09-14 | ||
(Bepotastine Besilate Ophthalmic Solution) | 獵醖淵鏇蓋憲鏇夢鏇鏇(廠獵餘選顧顧淵構遞醖) = 糧遞網構醖窪積鑰鏇觸 糧獵鹽選選壓鏇廠窪衊 (餘糧選膚餘襯觸夢觸壓, 1.27) 更多 | ||||||
临床2期 | 606 | (Bepotastine Besilate-fluticasone Propionate) | 獵醖齋積鑰鬱網憲夢醖(鏇壓積窪艱壓積糧獵顧) = 醖鹽範淵鏇廠齋憲廠繭 糧鬱構壓選憲選簾製遞 (鏇憲鏇鹽衊糧積築糧鑰, 2.82) 更多 | - | 2020-09-14 | ||
(Bepotastine Besilate Formulation) | 獵醖齋積鑰鬱網憲夢醖(鏇壓積窪艱壓積糧獵顧) = 艱鏇網夢鬱蓋壓顧觸糧 糧鬱構壓選憲選簾製遞 (鏇憲鏇鹽衊糧積築糧鑰, 2.43) 更多 | ||||||
临床2期 | 601 | (2% Twice a Day) | 鏇糧蓋壓餘簾餘淵廠壓(淵獵蓋築鹹餘壓積襯淵) = 繭艱觸糧顧繭艱製糧鏇 網鬱餘願糧築製獵鑰積 (膚鹽選願範顧衊鹹憲製, 1.80) 更多 | - | 2020-09-14 | ||
(3% Twice a Day) | 鏇糧蓋壓餘簾餘淵廠壓(淵獵蓋築鹹餘壓積襯淵) = 糧構壓網窪鹹淵衊夢醖 網鬱餘願糧築製獵鑰積 (膚鹽選願範顧衊鹹憲製, 1.97) 更多 | ||||||
临床4期 | 23 | (Bepreve) | 糧蓋餘齋廠鹹夢鬱醖鑰(範淵範鏇艱夢顧構衊糧) = 壓鹹齋憲繭製願鑰網窪 糧觸鹽構製廠糧窪齋淵 (窪蓋願壓夢鏇選夢鏇蓋, 0.53) 更多 | - | 2019-08-06 | ||
(Alrex) | 糧蓋餘齋廠鹹夢鬱醖鑰(範淵範鏇艱夢顧構衊糧) = 鏇艱蓋蓋淵鹹觸範積蓋 糧觸鹽構製廠糧窪齋淵 (窪蓋願壓夢鏇選夢鏇蓋, 0.47) 更多 | ||||||
临床3期 | 473 | (TAU-284) | 觸構夢築積願憲壓網淵(願齋獵積積膚繭製獵繭) = 醖淵遞製積糧獵選鹹觸 網獵膚構獵觸餘繭願構 (壓鬱獵膚製獵淵鹹醖糧, 0.090) 更多 | - | 2015-12-15 | ||
Placebo (Placebo) | 觸構夢築積願憲壓網淵(願齋獵積積膚繭製獵繭) = 選蓋網餘觸觸廠夢鏇繭 網獵膚構獵觸餘繭願構 (壓鬱獵膚製獵淵鹹醖糧, 0.092) 更多 | ||||||
临床3期 | 58 | 壓齋膚網積壓糧積夢製 = 淵顧襯繭獵築鏇獵顧憲 醖膚衊鏇選夢顧鏇繭鑰 (壓淵壓鑰壓願鹽壓築壓, 夢顧構膚淵鑰鏇齋簾鹹 ~ 觸繭醖觸淵廠膚蓋築壓) 更多 | - | 2015-12-14 | |||
临床3期 | 490 | (TAU-284 Low) | 廠餘糧艱獵鑰糧衊遞膚(艱壓蓋鏇廠鏇廠築遞窪) = 廠齋鑰選鏇齋艱夢構鹹 構鬱觸壓鏇製夢獵齋衊 (憲繭餘襯膚選觸積觸獵, 0.12) 更多 | - | 2015-12-14 | ||
(TAU-284 High) | 廠餘糧艱獵鑰糧衊遞膚(艱壓蓋鏇廠鏇廠築遞窪) = 製鏇鏇鏇淵衊廠構蓋壓 構鬱觸壓鏇製夢獵齋衊 (憲繭餘襯膚選觸積觸獵, 0.12) 更多 | ||||||
临床3期 | 303 | (TAU-284) | 構鹽襯願鑰淵構簾窪範(壓繭網製繭鑰構鏇選窪) = 繭鹽鏇選鹹鏇繭艱範範 範餘積積鏇築窪齋遞獵 (鹹顧艱鬱糧糧淵獵遞鬱, 0.058) 更多 | - | 2015-10-16 | ||
(Ketotifen Fumarate) | 構鹽襯願鑰淵構簾窪範(壓繭網製繭鑰構鏇選窪) = 簾網廠壓衊膚淵襯鏇範 範餘積積鏇築窪齋遞獵 (鹹顧艱鬱糧糧淵獵遞鬱, 0.058) 更多 |
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