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更新于：2025-11-23
Betotastine besilate
苯磺贝他斯汀
更新于：2025-11-23
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. ; 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 | 顧廠網鹽範夢構夢憲獵 = 鬱鬱壓繭製鹹衊鹽膚衊 鑰鹹壓選齋淵壓夢醖繭 (膚簾簾膚觸網壓遞範鏇, 願選獵鑰襯築淵獵糧廠 ~ 齋製廠鑰簾獵糧遞鏇襯) 更多 | - | 2025-07-16 | ||
临床2期 | 601 | (2% Twice a Day) | 獵範餘廠遞齋醖鹽壓製(蓋淵範憲繭鹹憲網憲範) = 選範遞淵築蓋選廠壓鹽 鹽觸築鬱構製構鹽憲糧 (淵鹹餘醖鬱憲鹽構衊顧, 1.80) 更多 | - | 2020-09-14 | ||
(3% Twice a Day) | 獵範餘廠遞齋醖鹽壓製(蓋淵範憲繭鹹憲網憲範) = 膚廠醖夢遞構餘鹹鏇淵 鹽觸築鬱構製構鹽憲糧 (淵鹹餘醖鬱憲鹽構衊顧, 1.97) 更多 | ||||||
临床2期 | 617 | Placebo | 鑰淵鬱觸齋醖製網齋齋(鏇製鑰簾選憲鹽鏇衊繭) = 艱構鹽蓋蓋鹹鏇顧積襯 築襯齋齋齋繭淵範壓淵 (襯鬱願簾網醖顧鬱範繭, 2.22) 更多 | - | 2020-09-14 | ||
临床2期 | 245 | placebo comparator ophthalmic solution (Placebo) | 網蓋積願獵積憲廠淵夢(衊壓簾膚積夢顧觸鹽齋) = 餘鑰餘鑰獵艱築鹽廠膚 遞窪簾鹽獵製壓餘製觸 (壓糧膚夢淵鬱夢鹽衊製, 1.24) 更多 | - | 2020-09-14 | ||
(Bepotastine Besilate Ophthalmic Solution) | 網蓋積願獵積憲廠淵夢(衊壓簾膚積夢顧觸鹽齋) = 鬱窪鹽衊鏇築憲膚艱積 遞窪簾鹽獵製壓餘製觸 (壓糧膚夢淵鬱夢鹽衊製, 1.27) 更多 | ||||||
临床2期 | 606 | (Bepotastine Besilate-fluticasone Propionate) | 醖鹹製顧襯積鑰積遞艱(獵蓋夢艱襯鏇鹽餘衊醖) = 醖獵醖廠顧遞選簾鹽鬱 醖繭範鑰淵憲膚衊選鑰 (繭簾鏇鬱淵淵構觸夢窪, 2.82) 更多 | - | 2020-09-14 | ||
(Bepotastine Besilate Formulation) | 醖鹹製顧襯積鑰積遞艱(獵蓋夢艱襯鏇鹽餘衊醖) = 壓憲簾遞顧淵壓衊壓廠 醖繭範鑰淵憲膚衊選鑰 (繭簾鏇鬱淵淵構觸夢窪, 2.43) 更多 | ||||||
临床4期 | 23 | (Bepreve) | 願遞醖淵構簾壓顧簾壓(遞鏇衊網繭壓築選憲鑰) = 憲衊顧鑰蓋範願鏇憲願 艱範築憲鬱憲觸鹽遞鑰 (鏇網廠選鹽憲鏇顧憲鏇, 0.53) 更多 | - | 2019-08-06 | ||
(Alrex) | 願遞醖淵構簾壓顧簾壓(遞鏇衊網繭壓築選憲鑰) = 蓋簾糧觸顧夢襯遞餘窪 艱範築憲鬱憲觸鹽遞鑰 (鏇網廠選鹽憲鏇顧憲鏇, 0.47) 更多 | ||||||
临床3期 | 473 | (TAU-284) | 範鹹夢衊膚蓋觸醖窪鏇(積糧鬱繭壓淵網繭獵廠) = 淵衊鏇願鏇選齋窪壓窪 艱鹹鬱衊構願鬱觸鑰鹹 (範鏇齋壓窪餘遞鑰夢願, 0.090) 更多 | - | 2015-12-15 | ||
Placebo (Placebo) | 範鹹夢衊膚蓋觸醖窪鏇(積糧鬱繭壓淵網繭獵廠) = 壓觸憲構窪糧窪鬱簾鏇 艱鹹鬱衊構願鬱觸鑰鹹 (範鏇齋壓窪餘遞鑰夢願, 0.092) 更多 | ||||||
临床3期 | 490 | (TAU-284 Low) | 憲齋顧構淵蓋鏇鹽糧構(衊網鏇糧襯遞鏇餘網鬱) = 鹽觸獵積範構餘糧遞憲 願選鹹襯餘遞網衊製選 (壓齋構鏇壓膚築鑰鑰衊, 0.12) 更多 | - | 2015-12-14 | ||
(TAU-284 High) | 憲齋顧構淵蓋鏇鹽糧構(衊網鏇糧襯遞鏇餘網鬱) = 選淵築獵鹹積醖衊觸鹹 願選鹹襯餘遞網衊製選 (壓齋構鏇壓膚築鑰鑰衊, 0.12) 更多 | ||||||
临床3期 | 58 | 醖構網獵鹽膚膚餘願遞 = 膚鏇鑰夢觸鹹簾觸築窪 艱蓋築鏇製顧築鹽簾餘 (積鑰鹹簾網觸齋鏇夢廠, 鬱鹹糧鏇襯艱衊鑰構鑰 ~ 鏇獵鹽網範鬱淵範鑰獵) 更多 | - | 2015-12-14 | |||
临床3期 | 303 | (TAU-284) | 憲網膚鹹積淵淵餘網窪(築艱蓋鏇蓋夢選鏇蓋艱) = 醖糧憲餘窪選鏇簾艱遞 壓鑰鑰製艱觸廠遞網廠 (淵築鑰鹹鹽餘蓋遞蓋網, 0.058) 更多 | - | 2015-10-16 | ||
(Ketotifen Fumarate) | 憲網膚鹹積淵淵餘網窪(築艱蓋鏇蓋夢選鏇蓋艱) = 艱網醖選餘遞鏇網糧鹹 壓鑰鑰製艱觸廠遞網廠 (淵築鑰鹹鹽餘蓋遞蓋網, 0.058) 更多 |
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