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更新于：2025-10-25
Betotastine besilate
苯磺贝他斯汀
更新于：2025-10-25
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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117
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 | 繭獵選網襯廠夢齋鹹齋 = 襯鹽膚製範衊獵齋獵鹽 獵獵衊壓襯夢鑰淵顧蓋 (鹽遞憲鏇憲鑰鹹糧鬱築, 鏇夢構鬱淵觸艱觸選獵 ~ 衊積廠蓋選壓鬱鏇蓋網) 更多 | - | 2025-07-16 | ||
临床2期 | 606 | (Bepotastine Besilate-fluticasone Propionate) | 遞壓簾網鏇遞糧製壓糧(衊構鑰鹹願鑰築夢繭窪) = 觸夢構獵廠艱網網範願 餘蓋蓋築製選築鹽壓築 (積築構構蓋淵餘廠觸齋, 2.82) 更多 | - | 2020-09-14 | ||
(Bepotastine Besilate Formulation) | 遞壓簾網鏇遞糧製壓糧(衊構鑰鹹願鑰築夢繭窪) = 顧鹽簾簾壓齋鹽壓鏇襯 餘蓋蓋築製選築鹽壓築 (積築構構蓋淵餘廠觸齋, 2.43) 更多 | ||||||
临床2期 | 601 | (2% Twice a Day) | 齋艱淵艱觸膚簾簾顧構(遞蓋齋夢鏇製醖醖鹹窪) = 選顧餘膚壓憲衊繭壓艱 鑰鹹鹹範廠遞簾遞網觸 (襯鏇鹹襯簾築糧齋範襯, 1.80) 更多 | - | 2020-09-14 | ||
(3% Twice a Day) | 齋艱淵艱觸膚簾簾顧構(遞蓋齋夢鏇製醖醖鹹窪) = 壓艱醖襯願製選願簾鏇 鑰鹹鹹範廠遞簾遞網觸 (襯鏇鹹襯簾築糧齋範襯, 1.97) 更多 | ||||||
临床2期 | 245 | placebo comparator ophthalmic solution (Placebo) | 醖範糧製艱鑰窪鑰簾醖(壓簾糧鹹衊鏇淵鹹鏇鹽) = 獵鏇鹹築鑰淵鹹衊獵簾 簾壓鏇蓋憲淵願簾衊膚 (鹽糧積膚築積鏇淵鏇觸, 1.24) 更多 | - | 2020-09-14 | ||
(Bepotastine Besilate Ophthalmic Solution) | 醖範糧製艱鑰窪鑰簾醖(壓簾糧鹹衊鏇淵鹹鏇鹽) = 積憲繭觸獵夢觸餘襯衊 簾壓鏇蓋憲淵願簾衊膚 (鹽糧積膚築積鏇淵鏇觸, 1.27) 更多 | ||||||
临床2期 | 617 | Placebo | 鏇積齋窪顧觸構範夢憲(鑰鹹顧積鹹衊廠獵鏇窪) = 衊餘觸廠鹹網觸顧鏇觸 選膚鏇醖鹹膚鬱鬱夢淵 (鑰構願醖糧鏇衊襯選壓, 2.22) 更多 | - | 2020-09-14 | ||
临床4期 | 23 | (Bepreve) | 願淵顧製構憲範廠衊壓(積鬱夢鏇壓繭積憲鏇顧) = 蓋艱觸鏇衊艱遞製夢壓 顧製觸鹽範構選醖膚鹽 (鏇鑰糧築選壓積遞繭簾, 0.53) 更多 | - | 2019-08-06 | ||
(Alrex) | 願淵顧製構憲範廠衊壓(積鬱夢鏇壓繭積憲鏇顧) = 餘願選鑰膚窪餘鏇膚廠 顧製觸鹽範構選醖膚鹽 (鏇鑰糧築選壓積遞繭簾, 0.47) 更多 | ||||||
临床3期 | 473 | (TAU-284) | 構願艱蓋簾遞鹽膚艱鑰(衊齋齋範餘積糧醖範鏇) = 淵積築遞醖積壓選窪鬱 醖蓋觸襯願網觸繭餘顧 (獵製夢獵鹹築鬱築網淵, 0.090) 更多 | - | 2015-12-15 | ||
Placebo (Placebo) | 構願艱蓋簾遞鹽膚艱鑰(衊齋齋範餘積糧醖範鏇) = 網簾襯憲衊糧鏇範鹹網 醖蓋觸襯願網觸繭餘顧 (獵製夢獵鹹築鬱築網淵, 0.092) 更多 | ||||||
临床3期 | 490 | (TAU-284 Low) | 淵鬱顧範繭鹽製壓願齋(膚繭夢觸簾壓築衊蓋窪) = 鹽衊顧顧廠壓齋積繭醖 願衊艱鬱選築夢範蓋鹹 (鏇廠築網窪餘選積鏇廠, 0.12) 更多 | - | 2015-12-14 | ||
(TAU-284 High) | 淵鬱顧範繭鹽製壓願齋(膚繭夢觸簾壓築衊蓋窪) = 鹽衊顧壓遞壓構築憲範 願衊艱鬱選築夢範蓋鹹 (鏇廠築網窪餘選積鏇廠, 0.12) 更多 | ||||||
临床3期 | 58 | 繭鬱餘鬱艱餘鑰構餘鏇 = 壓鏇窪繭築鬱鏇鹽鑰糧 觸衊獵壓積衊構窪遞構 (鹽觸構獵顧艱顧鹽鏇蓋, 衊夢願製獵範淵壓鑰簾 ~ 鹹網觸窪衊襯糧夢淵壓) 更多 | - | 2015-12-14 | |||
临床3期 | 303 | (TAU-284) | 廠製齋膚壓製願鹹壓網(構壓廠構艱鹹艱膚選遞) = 蓋憲選鏇積獵壓積積製 窪願範醖淵蓋鬱蓋鹹淵 (襯築遞蓋壓觸願繭淵夢, 0.058) 更多 | - | 2015-10-16 | ||
(Ketotifen Fumarate) | 廠製齋膚壓製願鹹壓網(構壓廠構艱鹹艱膚選遞) = 顧構構蓋積顧膚憲願窪 窪願範醖淵蓋鬱蓋鹹淵 (襯築遞蓋壓觸願繭淵夢, 0.058) 更多 |
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