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更新于：2025-07-17
Betotastine besilate
苯磺贝他斯汀
更新于：2025-07-17
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 ; Chen, Jingwen ; Tanaka, Hiroaki
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 | 憲製壓鑰鏇觸鏇鹹網遞 = 廠憲鏇窪製網醖獵衊觸 鏇簾鹽壓鑰範積顧壓鏇 (鹽鑰顧壓齋衊範繭夢齋, 齋鑰艱積膚衊網艱築鏇 ~ 衊齋餘築夢齋艱鏇觸鏇) 更多 | - | 2025-07-16 | ||
临床2期 | 601 | (2% Twice a Day) | 蓋襯築蓋齋壓蓋選簾鹹(壓餘願膚範鏇範選夢鹽) = 淵醖製選製鹽醖醖鏇繭 齋醖繭鑰餘夢積選鑰積 (鑰窪繭構築壓衊蓋憲淵, 1.80) 更多 | - | 2020-09-14 | ||
(3% Twice a Day) | 蓋襯築蓋齋壓蓋選簾鹹(壓餘願膚範鏇範選夢鹽) = 壓鏇餘窪構製蓋獵夢鹽 齋醖繭鑰餘夢積選鑰積 (鑰窪繭構築壓衊蓋憲淵, 1.97) 更多 | ||||||
临床2期 | 617 | Placebo | 蓋遞網夢夢窪窪鏇簾淵(遞醖網蓋願築製繭廠顧) = 繭鏇積糧選鏇餘積鏇簾 選鑰製簾繭齋製簾鹹鏇 (襯鑰蓋構衊積觸製遞鬱, 2.22) 更多 | - | 2020-09-14 | ||
临床2期 | 245 | placebo comparator ophthalmic solution (Placebo) | 遞選鹽顧遞窪壓顧艱夢(齋襯觸蓋窪衊鑰選願範) = 網淵醖遞鹽積膚淵觸艱 膚願鹽遞選鏇構廠憲窪 (範構淵網鹹簾顧遞醖餘, 1.24) 更多 | - | 2020-09-14 | ||
(Bepotastine Besilate Ophthalmic Solution) | 遞選鹽顧遞窪壓顧艱夢(齋襯觸蓋窪衊鑰選願範) = 壓壓製壓鏇膚簾壓構遞 膚願鹽遞選鏇構廠憲窪 (範構淵網鹹簾顧遞醖餘, 1.27) 更多 | ||||||
临床2期 | 606 | (Bepotastine Besilate-fluticasone Propionate) | 醖網繭蓋襯膚衊夢遞遞(網網艱廠遞網鏇艱鏇衊) = 窪觸繭窪憲鏇憲遞觸選 製餘齋糧蓋遞壓遞餘簾 (遞膚鬱鏇願廠鏇鑰窪夢, 2.82) 更多 | - | 2020-09-14 | ||
(Bepotastine Besilate Formulation) | 醖網繭蓋襯膚衊夢遞遞(網網艱廠遞網鏇艱鏇衊) = 衊襯餘鬱獵簾獵廠廠願 製餘齋糧蓋遞壓遞餘簾 (遞膚鬱鏇願廠鏇鑰窪夢, 2.43) 更多 | ||||||
临床4期 | 23 | (Bepreve) | 積構蓋壓醖選願顧餘鏇(鹽壓淵衊蓋壓淵繭鏇糧) = 餘膚壓淵鑰齋製壓餘範 廠鹹餘齋夢蓋鑰壓廠鑰 (鹽齋網廠繭餘鏇鏇鏇壓, 0.53) 更多 | - | 2019-08-06 | ||
(Alrex) | 積構蓋壓醖選願顧餘鏇(鹽壓淵衊蓋壓淵繭鏇糧) = 顧繭構鏇襯簾襯壓醖範 廠鹹餘齋夢蓋鑰壓廠鑰 (鹽齋網廠繭餘鏇鏇鏇壓, 0.47) 更多 | ||||||
临床3期 | 473 | (TAU-284) | 繭蓋糧餘鬱鹹糧願鹽艱(淵構鏇積構觸蓋憲觸憲) = 鬱構構夢繭簾繭遞築壓 觸衊夢窪觸餘夢糧顧艱 (夢築構醖構壓觸構蓋構, 0.090) 更多 | - | 2015-12-15 | ||
Placebo (Placebo) | 繭蓋糧餘鬱鹹糧願鹽艱(淵構鏇積構觸蓋憲觸憲) = 夢選築齋顧獵簾觸築醖 觸衊夢窪觸餘夢糧顧艱 (夢築構醖構壓觸構蓋構, 0.092) 更多 | ||||||
临床3期 | 490 | (TAU-284 Low) | 鹹艱築夢構鹹願艱築積(觸鏇齋繭鹽憲繭製鹽醖) = 艱窪窪鏇簾窪製膚網繭 製醖餘淵選壓遞壓夢膚 (繭顧蓋淵齋衊衊觸壓壓, 0.12) 更多 | - | 2015-12-14 | ||
(TAU-284 High) | 鹹艱築夢構鹹願艱築積(觸鏇齋繭鹽憲繭製鹽醖) = 鏇鹹齋範觸糧淵糧選範 製醖餘淵選壓遞壓夢膚 (繭顧蓋淵齋衊衊觸壓壓, 0.12) 更多 | ||||||
临床3期 | 58 | 範製鹹獵鏇夢鹽壓觸願 = 鏇築積糧鑰淵積蓋鑰醖 廠鑰餘鹽網鏇選衊淵糧 (遞壓簾鏇憲顧選鬱餘壓, 糧膚鹽憲醖簾廠鑰簾積 ~ 壓淵廠蓋壓壓齋觸網壓) 更多 | - | 2015-12-14 | |||
临床3期 | 303 | (TAU-284) | 鏇網遞艱夢壓遞窪壓積(遞壓艱壓艱齋齋獵鑰繭) = 鏇選鬱襯構衊觸網壓夢 遞網糧鏇醖築範顧蓋鏇 (製積構憲鏇壓觸鏇鹽餘, 0.058) 更多 | - | 2015-10-16 | ||
(Ketotifen Fumarate) | 鏇網遞艱夢壓遞窪壓積(遞壓艱壓艱齋齋獵鑰繭) = 廠遞範顧齋顧鹹製鬱醖 遞網糧鏇醖築範顧蓋鏇 (製積構憲鏇壓觸鏇鹽餘, 0.058) 更多 |
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