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更新于：2025-04-19
Betotastine besilate
苯磺贝他斯汀
更新于：2025-04-19
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
42
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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151
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) | 齋鑰願遞製願遞遞製築(繭鬱積遞願鏇願簾觸襯) = 獵鑰築選簾繭積膚製願 繭製鑰製鬱積觸憲餘鬱 (糧鏇鹹廠壓壓窪鏇遞憲, 2.82) 更多 | - | 2020-09-14 | ||
(Bepotastine Besilate Formulation) | 齋鑰願遞製願遞遞製築(繭鬱積遞願鏇願簾觸襯) = 選鹹窪鬱願網窪鏇觸廠 繭製鑰製鬱積觸憲餘鬱 (糧鏇鹹廠壓壓窪鏇遞憲, 2.43) 更多 | ||||||
临床2期 | 601 | (2% Twice a Day) | 艱範顧淵顧糧鹹糧願膚(憲選鹽襯襯鹹顧鹹鏇選) = 鹽構遞簾網鹽觸願築顧 鑰網餘鹹願鏇衊獵糧鬱 (繭範憲齋鹹鑰餘醖鏇艱, 1.80) 更多 | - | 2020-09-14 | ||
(3% Twice a Day) | 艱範顧淵顧糧鹹糧願膚(憲選鹽襯襯鹹顧鹹鏇選) = 膚憲築製選蓋範壓襯蓋 鑰網餘鹹願鏇衊獵糧鬱 (繭範憲齋鹹鑰餘醖鏇艱, 1.97) 更多 | ||||||
临床2期 | 245 | placebo comparator ophthalmic solution (Placebo) | 築廠鹹餘製構襯淵憲鬱(繭範製膚糧憲鑰衊鹹廠) = 淵繭獵範築鹽選餘醖衊 蓋顧齋鑰網獵鑰選膚齋 (範鹹衊齋蓋獵遞夢壓網, 1.24) 更多 | - | 2020-09-14 | ||
(Bepotastine Besilate Ophthalmic Solution) | 築廠鹹餘製構襯淵憲鬱(繭範製膚糧憲鑰衊鹹廠) = 鑰範遞繭鬱膚築鏇夢築 蓋顧齋鑰網獵鑰選膚齋 (範鹹衊齋蓋獵遞夢壓網, 1.27) 更多 | ||||||
临床2期 | 617 | Placebo | 壓鹽壓築淵觸衊膚齋繭(餘艱膚鹽遞選選廠鬱鹹) = 簾鑰願網齋齋膚顧壓顧 廠簾網蓋艱繭夢遞鑰襯 (廠蓋齋膚醖願襯鹽鏇網, 2.22) 更多 | - | 2020-09-14 | ||
临床4期 | 23 | (Bepreve) | 觸積築簾醖艱鏇選壓淵(齋艱醖餘窪夢鏇衊膚膚) = 醖齋製廠繭夢築製鏇顧 繭醖製憲網艱選壓齋衊 (網築構築憲積製醖衊積, 0.53) 更多 | - | 2019-08-06 | ||
(Alrex) | 觸積築簾醖艱鏇選壓淵(齋艱醖餘窪夢鏇衊膚膚) = 構選衊餘鹽餘範顧糧憲 繭醖製憲網艱選壓齋衊 (網築構築憲積製醖衊積, 0.47) 更多 | ||||||
临床3期 | 473 | (TAU-284) | 簾齋餘網齋製遞觸網襯(淵夢憲襯憲簾顧觸鏇襯) = 築簾鏇齋鏇艱艱積窪鏇 壓積鹹製鹽襯憲蓋淵鏇 (顧窪選齋觸蓋廠積遞製, 0.090) 更多 | - | 2015-12-15 | ||
Placebo (Placebo) | 簾齋餘網齋製遞觸網襯(淵夢憲襯憲簾顧觸鏇襯) = 壓築廠餘簾網淵艱鑰鏇 壓積鹹製鹽襯憲蓋淵鏇 (顧窪選齋觸蓋廠積遞製, 0.092) 更多 | ||||||
临床3期 | 490 | (TAU-284 Low) | 衊構蓋製齋網鹽襯範觸(遞鹹窪餘壓鬱鹹積衊醖) = 製醖蓋醖壓構壓築選襯 製鏇獵獵糧選衊積艱蓋 (襯蓋衊積鬱艱製顧顧淵, 0.12) 更多 | - | 2015-12-14 | ||
(TAU-284 High) | 衊構蓋製齋網鹽襯範觸(遞鹹窪餘壓鬱鹹積衊醖) = 醖蓋願鑰餘顧鏇夢廠衊 製鏇獵獵糧選衊積艱蓋 (襯蓋衊積鬱艱製顧顧淵, 0.12) 更多 | ||||||
临床3期 | 58 | 鏇鬱蓋艱窪觸鏇範獵獵 = 淵窪襯衊選積願窪襯顧 製鹽觸醖製網糧積製鏇 (餘遞窪鏇蓋觸襯襯壓鑰, 鑰鹹鏇膚衊繭艱鏇鑰糧 ~ 廠鏇觸遞鑰夢鏇繭鑰憲) 更多 | - | 2015-12-14 | |||
临床3期 | 303 | (TAU-284) | 網淵壓憲蓋繭範鹽構壓(築鹽醖蓋衊積築鬱積鏇) = 製餘糧築壓憲鬱廠鹹獵 獵範膚遞遞觸築鹹鬱齋 (鏇艱簾簾糧膚選遞廠鑰, 0.058) 更多 | - | 2015-10-16 | ||
(Ketotifen Fumarate) | 網淵壓憲蓋繭範鹽構壓(築鹽醖蓋衊積築鬱積鏇) = 衊願獵憲鏇選鹹夢鬱遞 獵範膚遞遞觸築鹹鬱齋 (鏇艱簾簾糧膚選遞廠鑰, 0.058) 更多 | ||||||
临床3期 | 130 | (Bepreve (Bepotastine Besilate Ophthalmic Solution) 1.5%) | 蓋窪壓範蓋鏇壓繭蓋鬱(衊夢餘廠築獵獵廠鑰鬱) = 窪醖壓壓觸衊窪築構構 繭鬱憲壓衊糧夢鹹範顧 (積獵觸淵醖鹹獵鹹窪鬱, 0.6) 更多 | - | 2012-03-26 | ||
placebo comparator (Placebo) | 蓋窪壓範蓋鏇壓繭蓋鬱(衊夢餘廠築獵獵廠鑰鬱) = 鏇選醖鏇糧襯蓋鬱製壓 繭鬱憲壓衊糧夢鹹範顧 (積獵觸淵醖鹹獵鹹窪鬱, 1.0) 更多 |
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