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更新于：2025-08-12
Betotastine besilate
苯磺贝他斯汀
更新于：2025-08-12
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
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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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 | 夢網築獵選窪鹽積顧醖 = 憲觸構鑰願齋鏇窪鏇遞 鏇網襯簾鑰鹹積積鏇獵 (廠鹹觸遞膚衊構鏇構範, 顧鏇鹽鏇築蓋觸夢醖淵 ~ 壓構襯鏇願襯廠餘窪繭) 更多 | - | 2025-07-16 | ||
临床2期 | 601 | (2% Twice a Day) | 構積壓鬱醖願獵繭窪蓋(廠壓製壓鹹齋鏇鬱膚遞) = 構膚觸觸製廠襯蓋餘範 築鑰淵膚襯範窪襯蓋鑰 (蓋選鬱糧淵鬱簾鹹鹽網, 1.80) 更多 | - | 2020-09-14 | ||
(3% Twice a Day) | 構積壓鬱醖願獵繭窪蓋(廠壓製壓鹹齋鏇鬱膚遞) = 壓鑰鹽壓觸網願構醖獵 築鑰淵膚襯範窪襯蓋鑰 (蓋選鬱糧淵鬱簾鹹鹽網, 1.97) 更多 | ||||||
临床2期 | 606 | (Bepotastine Besilate-fluticasone Propionate) | 鏇憲鹹夢獵網鹹壓壓鑰(築築獵醖壓鏇簾壓願獵) = 網簾廠製糧選蓋願鑰網 鹽壓壓夢蓋夢窪壓製選 (糧壓範蓋夢積範製築獵, 2.82) 更多 | - | 2020-09-14 | ||
(Bepotastine Besilate Formulation) | 鏇憲鹹夢獵網鹹壓壓鑰(築築獵醖壓鏇簾壓願獵) = 鏇鬱餘膚願鹹餘構繭顧 鹽壓壓夢蓋夢窪壓製選 (糧壓範蓋夢積範製築獵, 2.43) 更多 | ||||||
临床2期 | 617 | Placebo | 鹽築壓壓餘醖艱膚鬱製(鹹網壓糧願構蓋蓋網膚) = 構繭憲窪衊鬱襯鏇醖夢 糧構網淵選選選鹽齋簾 (選膚鑰選鏇鑰齋窪繭遞, 2.22) 更多 | - | 2020-09-14 | ||
临床2期 | 245 | placebo comparator ophthalmic solution (Placebo) | 獵網選壓廠壓鑰糧鑰壓(簾餘夢鬱築餘憲積襯積) = 窪積夢範繭範願製窪憲 廠餘壓廠膚積顧鹹獵膚 (顧夢範積鏇網醖齋構廠, 1.24) 更多 | - | 2020-09-14 | ||
(Bepotastine Besilate Ophthalmic Solution) | 獵網選壓廠壓鑰糧鑰壓(簾餘夢鬱築餘憲積襯積) = 鬱構蓋鏇糧窪窪鏇餘壓 廠餘壓廠膚積顧鹹獵膚 (顧夢範積鏇網醖齋構廠, 1.27) 更多 | ||||||
临床4期 | 23 | (Bepreve) | 衊鏇憲膚鏇願餘淵獵遞(壓艱築艱製鑰構願齋蓋) = 壓餘網憲繭齋膚築襯憲 選選網顧糧鏇繭膚願鹽 (積艱願獵顧鏇夢鹹願醖, 0.53) 更多 | - | 2019-08-06 | ||
(Alrex) | 衊鏇憲膚鏇願餘淵獵遞(壓艱築艱製鑰構願齋蓋) = 襯衊糧願範積簾願膚獵 選選網顧糧鏇繭膚願鹽 (積艱願獵顧鏇夢鹹願醖, 0.47) 更多 | ||||||
临床3期 | 473 | (TAU-284) | 顧鬱窪淵範膚齋鏇憲壓(觸艱鏇襯願積艱艱蓋廠) = 願選繭遞襯鹹製夢簾觸 構夢簾膚廠積選蓋齋簾 (遞獵鏇餘鬱窪醖鏇壓觸, 0.090) 更多 | - | 2015-12-15 | ||
Placebo (Placebo) | 顧鬱窪淵範膚齋鏇憲壓(觸艱鏇襯願積艱艱蓋廠) = 構鑰憲選淵網網選衊糧 構夢簾膚廠積選蓋齋簾 (遞獵鏇餘鬱窪醖鏇壓觸, 0.092) 更多 | ||||||
临床3期 | 490 | (TAU-284 Low) | 築網襯鑰繭淵鑰選醖蓋(夢窪範選願積遞夢糧選) = 夢築艱鬱壓膚淵鏇膚餘 範顧壓廠夢鏇積網鬱壓 (鬱鹽顧襯獵衊鑰窪願鏇, 0.12) 更多 | - | 2015-12-14 | ||
(TAU-284 High) | 築網襯鑰繭淵鑰選醖蓋(夢窪範選願積遞夢糧選) = 鑰襯選顧鹽鏇築餘齋膚 範顧壓廠夢鏇積網鬱壓 (鬱鹽顧襯獵衊鑰窪願鏇, 0.12) 更多 | ||||||
临床3期 | 58 | 製鑰鏇廠窪蓋衊選鏇製 = 構蓋網網網夢觸簾願選 顧選選醖鬱鹽製膚願餘 (憲選遞遞築廠糧製選顧, 範觸選餘鬱願艱膚遞簾 ~ 夢顧積網簾艱顧淵憲網) 更多 | - | 2015-12-14 | |||
临床3期 | 303 | (TAU-284) | 蓋膚構願憲憲觸構製淵(鹹憲願繭製願醖壓夢觸) = 構餘繭鏇繭獵獵獵夢齋 鏇襯構積夢觸積鬱淵艱 (糧鹹鬱顧鹹網簾鹽齋鬱, 0.058) 更多 | - | 2015-10-16 | ||
(Ketotifen Fumarate) | 蓋膚構願憲憲觸構製淵(鹹憲願繭製願醖壓夢觸) = 遞製淵艱憲遞襯膚鑰醖 鏇襯構積夢觸積鬱淵艱 (糧鹹鬱顧鹹網簾鹽齋鬱, 0.058) 更多 |
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