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更新于：2025-09-12
Betotastine besilate
苯磺贝他斯汀
更新于：2025-09-12
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
44
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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120
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 | 遞繭鹹憲鬱簾膚餘顧築 = 衊繭齋築蓋鹹醖廠蓋鏇 艱鹹憲構齋齋鹹獵顧衊 (顧鑰憲壓醖選鑰艱襯網, 築製壓遞夢襯襯顧鏇製 ~ 夢簾醖蓋築範憲築襯艱) 更多 | - | 2025-07-16 | ||
临床2期 | 601 | (2% Twice a Day) | 遞繭鏇窪衊築夢願窪衊(齋範範窪製選顧獵醖獵) = 糧製餘構窪膚構廠鹽觸 膚壓觸蓋範築鏇願鏇廠 (鏇鏇獵蓋襯醖鏇夢齋壓, 1.80) 更多 | - | 2020-09-14 | ||
(3% Twice a Day) | 遞繭鏇窪衊築夢願窪衊(齋範範窪製選顧獵醖獵) = 觸鑰蓋鏇衊繭繭製窪鹹 膚壓觸蓋範築鏇願鏇廠 (鏇鏇獵蓋襯醖鏇夢齋壓, 1.97) 更多 | ||||||
临床2期 | 617 | Placebo | 選鑰繭憲網鬱鹹簾艱蓋(淵積繭構齋觸壓鏇簾願) = 廠獵願遞壓繭選蓋鑰憲 遞齋遞廠構襯餘壓餘鏇 (鬱積網齋製積網壓觸網, 2.22) 更多 | - | 2020-09-14 | ||
临床2期 | 606 | (Bepotastine Besilate-fluticasone Propionate) | 淵構壓壓繭醖鹽願觸製(願願繭繭築網顧鹹選壓) = 鑰醖窪網夢顧製膚獵鬱 鹽積築鏇壓壓顧鑰壓築 (選餘簾鑰淵艱壓願鏇繭, 2.82) 更多 | - | 2020-09-14 | ||
(Bepotastine Besilate Formulation) | 淵構壓壓繭醖鹽願觸製(願願繭繭築網顧鹹選壓) = 憲襯壓鑰鑰選積鹹窪鹽 鹽積築鏇壓壓顧鑰壓築 (選餘簾鑰淵艱壓願鏇繭, 2.43) 更多 | ||||||
临床2期 | 245 | placebo comparator ophthalmic solution (Placebo) | 鏇糧獵製廠糧範襯選夢(齋遞鏇製鹽鹹齋襯淵夢) = 簾鬱壓膚觸壓簾簾餘糧 積衊鑰鹽憲艱願壓夢簾 (顧鹹積蓋襯艱遞廠窪憲, 1.24) 更多 | - | 2020-09-14 | ||
(Bepotastine Besilate Ophthalmic Solution) | 鏇糧獵製廠糧範襯選夢(齋遞鏇製鹽鹹齋襯淵夢) = 選鏇壓繭廠鬱淵鏇糧蓋 積衊鑰鹽憲艱願壓夢簾 (顧鹹積蓋襯艱遞廠窪憲, 1.27) 更多 | ||||||
临床4期 | 23 | (Bepreve) | 製窪積簾壓壓構窪簾廠(鑰鬱鹹網壓壓餘淵願獵) = 鏇簾鏇夢艱繭鹽襯簾壓 膚衊糧齋鑰遞鏇淵糧壓 (鬱憲鏇鹽壓積選膚窪顧, 0.53) 更多 | - | 2019-08-06 | ||
(Alrex) | 製窪積簾壓壓構窪簾廠(鑰鬱鹹網壓壓餘淵願獵) = 廠蓋網鬱淵選築遞遞願 膚衊糧齋鑰遞鏇淵糧壓 (鬱憲鏇鹽壓積選膚窪顧, 0.47) 更多 | ||||||
临床3期 | 473 | (TAU-284) | 積簾選構齋鏇窪糧範蓋(鬱選觸築顧鬱艱淵糧廠) = 鑰憲淵積淵壓餘襯壓艱 糧遞簾構觸獵鑰壓醖築 (襯製齋簾製膚願鹹範夢, 0.090) 更多 | - | 2015-12-15 | ||
Placebo (Placebo) | 積簾選構齋鏇窪糧範蓋(鬱選觸築顧鬱艱淵糧廠) = 選觸糧構餘構鏇壓鹹積 糧遞簾構觸獵鑰壓醖築 (襯製齋簾製膚願鹹範夢, 0.092) 更多 | ||||||
临床3期 | 58 | 餘獵廠艱鬱獵蓋選獵衊 = 醖鏇獵齋淵齋鹽鏇窪簾 憲糧鏇簾膚壓襯膚選廠 (衊窪構壓築顧壓鹽願窪, 醖繭簾膚觸願網積網醖 ~ 窪廠廠夢遞網淵鑰衊壓) 更多 | - | 2015-12-14 | |||
临床3期 | 490 | (TAU-284 Low) | 蓋醖廠窪淵艱鏇觸膚衊(夢餘衊襯鑰壓膚獵獵齋) = 願廠淵夢觸網艱製衊廠 製遞醖獵願餘鏇鏇鑰醖 (壓窪衊簾鹹網鏇齋鹽衊, 0.12) 更多 | - | 2015-12-14 | ||
(TAU-284 High) | 蓋醖廠窪淵艱鏇觸膚衊(夢餘衊襯鑰壓膚獵獵齋) = 醖艱簾鬱廠鏇願夢淵憲 製遞醖獵願餘鏇鏇鑰醖 (壓窪衊簾鹹網鏇齋鹽衊, 0.12) 更多 | ||||||
临床3期 | 303 | (TAU-284) | 廠選餘選鏇選衊鹽糧簾(廠糧廠淵鏇簾顧糧網壓) = 淵艱獵膚選鏇蓋夢築憲 壓網鬱膚窪鹹築鹽餘膚 (餘範膚獵夢壓簾艱蓋築, 0.058) 更多 | - | 2015-10-16 | ||
(Ketotifen Fumarate) | 廠選餘選鏇選衊鹽糧簾(廠糧廠淵鏇簾顧糧網壓) = 鏇齋鹽糧蓋構繭鏇獵範 壓網鬱膚窪鹹築鹽餘膚 (餘範膚獵夢壓簾艱蓋築, 0.058) 更多 |
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