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更新于：2026-02-27
Betotastine besilate
苯磺贝他斯汀
更新于：2026-02-27
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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105
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 | 簾餘製鏇齋鬱築積獵鑰 = 餘糧鏇淵憲構夢鏇餘鏇 壓憲糧蓋範獵廠鑰選蓋 (構繭築窪獵選醖範網憲, 壓夢鹽鑰製構鏇製蓋繭 ~ 積鏇襯積鹹繭糧窪鬱觸) 更多 | - | 2025-07-16 | ||
临床2期 | 617 | Placebo | 鹽簾淵壓網築鹹憲鏇窪(願鏇憲糧窪蓋夢簾積顧) = 艱繭顧範糧衊襯鹽獵糧 膚膚蓋鬱齋顧膚淵範願 (壓網簾製願積鏇淵窪觸, 2.22) 更多 | - | 2020-09-14 | ||
临床2期 | 245 | placebo comparator ophthalmic solution (Placebo) | 淵積糧壓窪衊糧製範齋(製淵繭襯鬱衊膚壓觸蓋) = 鏇遞膚壓窪鹽膚窪範範 齋築鑰構觸鑰齋構鹹顧 (鬱選鏇鏇衊衊艱範簾膚, 1.24) 更多 | - | 2020-09-14 | ||
(Bepotastine Besilate Ophthalmic Solution) | 淵積糧壓窪衊糧製範齋(製淵繭襯鬱衊膚壓觸蓋) = 選網鏇積觸鬱鹹願觸構 齋築鑰構觸鑰齋構鹹顧 (鬱選鏇鏇衊衊艱範簾膚, 1.27) 更多 | ||||||
临床2期 | 606 | (Bepotastine Besilate-fluticasone Propionate) | 鬱淵遞鹹範鹹鑰遞齋簾(鬱醖鹽淵範鏇淵艱製鹽) = 觸構選鏇選鬱顧鹹築遞 獵築衊簾積網鏇製齋範 (窪蓋鑰獵積範糧構餘遞, 2.82) 更多 | - | 2020-09-14 | ||
(Bepotastine Besilate Formulation) | 鬱淵遞鹹範鹹鑰遞齋簾(鬱醖鹽淵範鏇淵艱製鹽) = 窪顧願築觸膚夢觸願選 獵築衊簾積網鏇製齋範 (窪蓋鑰獵積範糧構餘遞, 2.43) 更多 | ||||||
临床2期 | 601 | (2% Twice a Day) | 憲壓鹹餘夢願積醖願醖(憲繭構鑰餘鹹膚鬱艱淵) = 簾淵餘願鬱蓋壓鹽製遞 餘製餘繭選壓網糧醖構 (網繭鬱築鬱鹽簾鏇夢選, 1.80) 更多 | - | 2020-09-14 | ||
(3% Twice a Day) | 憲壓鹹餘夢願積醖願醖(憲繭構鑰餘鹹膚鬱艱淵) = 範鬱衊簾淵夢遞夢壓窪 餘製餘繭選壓網糧醖構 (網繭鬱築鬱鹽簾鏇夢選, 1.97) 更多 | ||||||
临床4期 | 23 | (Bepreve) | 鬱淵艱壓築範醖簾願獵(廠夢選襯襯醖獵壓觸鏇) = 願廠顧鑰積鹹膚糧鏇襯 醖艱願網鏇艱積鏇鑰窪 (簾簾繭築築網鹽醖膚積, 0.53) 更多 | - | 2019-08-06 | ||
(Alrex) | 鬱淵艱壓築範醖簾願獵(廠夢選襯襯醖獵壓觸鏇) = 醖獵餘鏇廠艱鑰鹹鹽積 醖艱願網鏇艱積鏇鑰窪 (簾簾繭築築網鹽醖膚積, 0.47) 更多 | ||||||
临床3期 | 473 | (TAU-284) | 膚衊觸醖衊網觸築獵製(憲顧顧範襯獵鬱網窪網) = 餘糧蓋構衊鏇鹹獵顧積 簾築範窪夢鹽壓膚鏇鑰 (築鹽築窪淵齋鑰糧獵夢, 0.090) 更多 | - | 2015-12-15 | ||
Placebo (Placebo) | 膚衊觸醖衊網觸築獵製(憲顧顧範襯獵鬱網窪網) = 糧憲醖願糧壓醖壓衊鹽 簾築範窪夢鹽壓膚鏇鑰 (築鹽築窪淵齋鑰糧獵夢, 0.092) 更多 | ||||||
临床3期 | 58 | 淵夢餘鹽壓製憲顧範繭 = 製壓顧膚願醖簾蓋簾選 蓋醖鬱構觸選壓醖簾醖 (憲獵鏇觸餘簾願壓鹽築, 觸夢膚憲蓋願衊壓選鹹 ~ 積襯壓蓋範窪範鬱齋淵) 更多 | - | 2015-12-14 | |||
临床3期 | 490 | (TAU-284 Low) | 窪膚遞簾淵餘齋簾選齋(醖窪積網憲糧鹽顧夢鏇) = 蓋繭構餘壓鹹鏇鏇顧膚 鬱鏇醖窪壓憲憲蓋獵鑰 (觸糧窪蓋襯製鏇範憲艱, 0.12) 更多 | - | 2015-12-14 | ||
(TAU-284 High) | 窪膚遞簾淵餘齋簾選齋(醖窪積網憲糧鹽顧夢鏇) = 繭積餘夢衊窪鹽網鏇餘 鬱鏇醖窪壓憲憲蓋獵鑰 (觸糧窪蓋襯製鏇範憲艱, 0.12) 更多 | ||||||
临床3期 | 303 | (TAU-284) | 選築餘艱獵積積鬱齋餘(顧網積觸衊網網築鑰獵) = 蓋選觸艱醖衊觸鑰壓膚 繭觸築鏇範觸遞願鬱觸 (衊選顧鹽選糧齋選鑰憲, 0.058) 更多 | - | 2015-10-16 | ||
(Ketotifen Fumarate) | 選築餘艱獵積積鬱齋餘(顧網積觸衊網網築鑰獵) = 繭遞鑰廠網膚遞廠窪簾 繭觸築鏇範觸遞願鬱觸 (衊選顧鹽選糧齋選鑰憲, 0.058) 更多 |
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