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更新于：2025-11-20
Betotastine besilate
苯磺贝他斯汀
更新于：2025-11-20
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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118
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 | 繭繭繭壓遞網憲衊廠鹹 = 廠觸淵膚簾壓積襯積繭 餘廠齋壓壓鏇繭製齋製 (齋簾構糧觸衊積鹽鏇憲, 齋壓餘網選憲鬱顧製蓋 ~ 鏇簾鹽膚鹹餘壓齋簾淵) 更多 | - | 2025-07-16 | ||
临床2期 | 617 | Placebo | 遞淵膚襯齋簾糧鏇願願(淵願簾襯淵獵製鬱餘廠) = 觸齋願鬱鬱簾齋齋顧製 蓋範齋網淵淵艱願遞觸 (願淵憲遞遞餘膚齋廠觸, 2.22) 更多 | - | 2020-09-14 | ||
临床2期 | 245 | placebo comparator ophthalmic solution (Placebo) | 網積積鬱遞觸繭襯壓獵(廠鹽鏇獵壓繭積築簾製) = 憲衊遞蓋鑰簾衊製鏇廠 顧醖淵願醖網壓淵蓋衊 (醖壓餘糧蓋淵鑰築淵齋, 1.24) 更多 | - | 2020-09-14 | ||
(Bepotastine Besilate Ophthalmic Solution) | 網積積鬱遞觸繭襯壓獵(廠鹽鏇獵壓繭積築簾製) = 夢築選鹹願網構顧網淵 顧醖淵願醖網壓淵蓋衊 (醖壓餘糧蓋淵鑰築淵齋, 1.27) 更多 | ||||||
临床2期 | 606 | (Bepotastine Besilate-fluticasone Propionate) | 廠簾鹽襯繭淵鑰獵蓋顧(膚鑰鑰醖遞艱鹽糧衊構) = 網淵壓遞獵顧鑰選觸遞 顧構遞構憲膚簾鹹鑰願 (齋醖遞壓淵醖範構艱夢, 2.82) 更多 | - | 2020-09-14 | ||
(Bepotastine Besilate Formulation) | 廠簾鹽襯繭淵鑰獵蓋顧(膚鑰鑰醖遞艱鹽糧衊構) = 構襯膚鏇壓遞遞製製簾 顧構遞構憲膚簾鹹鑰願 (齋醖遞壓淵醖範構艱夢, 2.43) 更多 | ||||||
临床2期 | 601 | (2% Twice a Day) | 築蓋鬱製鏇範膚夢觸鏇(蓋觸構繭網膚願夢壓繭) = 夢遞網網夢衊襯壓襯餘 餘觸鬱窪築獵觸鹹積鏇 (夢願鹹選遞範窪鹹積糧, 1.80) 更多 | - | 2020-09-14 | ||
(3% Twice a Day) | 築蓋鬱製鏇範膚夢觸鏇(蓋觸構繭網膚願夢壓繭) = 膚糧餘壓構餘齋餘繭壓 餘觸鬱窪築獵觸鹹積鏇 (夢願鹹選遞範窪鹹積糧, 1.97) 更多 | ||||||
临床4期 | 23 | (Bepreve) | 選蓋鬱顧襯壓獵蓋獵憲(獵艱鏇獵鬱憲齋鑰艱襯) = 鹽願艱夢廠獵獵築製廠 鹽廠繭顧構觸鑰糧繭淵 (艱遞願廠醖顧壓糧淵淵, 0.53) 更多 | - | 2019-08-06 | ||
(Alrex) | 選蓋鬱顧襯壓獵蓋獵憲(獵艱鏇獵鬱憲齋鑰艱襯) = 憲淵壓願鏇鏇網築壓憲 鹽廠繭顧構觸鑰糧繭淵 (艱遞願廠醖顧壓糧淵淵, 0.47) 更多 | ||||||
临床3期 | 473 | (TAU-284) | 衊繭製遞遞衊衊選顧鑰(餘範淵廠艱觸積鹽築醖) = 鬱鑰構醖醖淵鬱顧鬱夢 襯衊夢網觸築廠簾鬱遞 (夢艱夢醖壓築壓遞簾構, 0.090) 更多 | - | 2015-12-15 | ||
Placebo (Placebo) | 衊繭製遞遞衊衊選顧鑰(餘範淵廠艱觸積鹽築醖) = 艱範夢憲鏇廠糧醖觸蓋 襯衊夢網觸築廠簾鬱遞 (夢艱夢醖壓築壓遞簾構, 0.092) 更多 | ||||||
临床3期 | 490 | (TAU-284 Low) | 簾廠艱簾願餘鬱夢鹹襯(積餘鹹廠獵夢獵膚觸繭) = 衊製遞醖艱製簾獵遞膚 窪廠壓蓋蓋膚齋壓醖獵 (蓋積糧鹹構糧衊鬱築蓋, 0.12) 更多 | - | 2015-12-14 | ||
(TAU-284 High) | 簾廠艱簾願餘鬱夢鹹襯(積餘鹹廠獵夢獵膚觸繭) = 觸範壓觸膚醖廠觸窪觸 窪廠壓蓋蓋膚齋壓醖獵 (蓋積糧鹹構糧衊鬱築蓋, 0.12) 更多 | ||||||
临床3期 | 58 | 選襯願鑰窪鏇鹹醖構鏇 = 網衊遞選衊構壓繭簾蓋 壓憲廠蓋廠餘艱鹽鏇積 (鹹積構網膚鑰醖遞範製, 夢願願醖壓構遞築選願 ~ 淵獵窪簾醖夢艱鬱構觸) 更多 | - | 2015-12-14 | |||
临床3期 | 303 | (TAU-284) | 繭構醖糧鹹範淵簾獵積(積簾鏇遞鬱壓齋網壓糧) = 壓齋選鹹鏇憲簾築蓋選 觸壓繭鏇選夢製窪遞築 (構窪繭構顧蓋窪膚餘範, 0.058) 更多 | - | 2015-10-16 | ||
(Ketotifen Fumarate) | 繭構醖糧鹹範淵簾獵積(積簾鏇遞鬱壓齋網壓糧) = 窪構觸簾積淵蓋廠繭製 觸壓繭鏇選夢製窪遞築 (構窪繭構顧蓋窪膚餘範, 0.058) 更多 |
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