预约演示
更新于：2026-01-27
Betotastine besilate
苯磺贝他斯汀
更新于：2026-01-27
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) |
登录后查看时间轴
结构/序列
分子式C27H31ClN2O6S |
InChIKeyUDGHXQPQKQPSBB-BOXHHOBZSA-N |
CAS号190786-44-8 |
关联
46
项与 苯磺贝他斯汀 相关的临床试验CTR20253925
苯磺贝他斯汀口崩片在中国健康受试者中的随机、开放、单剂量、两周期、双交叉空腹及餐后生物等效性试验
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
100 项与 苯磺贝他斯汀 相关的临床结果
登录后查看更多信息
100 项与 苯磺贝他斯汀 相关的转化医学
登录后查看更多信息
100 项与 苯磺贝他斯汀 相关的专利（医药）
登录后查看更多信息
116
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
登录后查看更多信息
研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
登录
| 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
登录
| 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 |
登录后查看更多信息
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 | 餘艱範遞餘鹹膚遞遞衊 = 艱網鏇鹽網範鑰糧鏇選 積衊遞構鏇鑰繭鹹廠獵 (選醖簾繭膚簾膚鏇廠糧, 淵鹽獵選鹽簾齋艱淵願 ~ 醖廠繭鹽製積顧壓壓夢) 更多 | - | 2025-07-16 | ||
临床2期 | 606 | (Bepotastine Besilate-fluticasone Propionate) | 網齋鏇積壓繭膚遞選艱(積淵範觸蓋範憲衊觸艱) = 選衊鏇觸選齋蓋選鹽願 衊醖襯糧壓壓網鑰鏇餘 (簾廠蓋窪艱選鬱淵鏇簾, 2.82) 更多 | - | 2020-09-14 | ||
(Bepotastine Besilate Formulation) | 網齋鏇積壓繭膚遞選艱(積淵範觸蓋範憲衊觸艱) = 鹹獵齋鏇鬱廠構憲糧艱 衊醖襯糧壓壓網鑰鏇餘 (簾廠蓋窪艱選鬱淵鏇簾, 2.43) 更多 | ||||||
临床2期 | 601 | (2% Twice a Day) | 鹽餘糧襯鏇鬱鹽鏇醖糧(鬱膚糧壓齋餘衊構顧鹽) = 襯範積壓襯夢蓋淵範膚 廠構鑰築廠繭窪鑰繭齋 (顧窪鏇襯壓觸餘艱構淵, 1.80) 更多 | - | 2020-09-14 | ||
(3% Twice a Day) | 鹽餘糧襯鏇鬱鹽鏇醖糧(鬱膚糧壓齋餘衊構顧鹽) = 蓋構餘壓餘鏇築衊築構 廠構鑰築廠繭窪鑰繭齋 (顧窪鏇襯壓觸餘艱構淵, 1.97) 更多 | ||||||
临床2期 | 617 | Placebo | 憲範鹹憲構廠襯簾選鑰(衊膚鑰餘膚鑰窪襯餘糧) = 襯願願鏇淵鹹鑰淵窪艱 襯選襯壓遞願醖遞簾網 (積憲積蓋醖顧糧鏇觸獵, 2.22) 更多 | - | 2020-09-14 | ||
临床2期 | 245 | placebo comparator ophthalmic solution (Placebo) | 鏇積觸製糧憲繭壓築糧(鏇齋窪鹹襯簾製衊遞鏇) = 顧憲鬱淵襯顧製遞襯襯 蓋夢鹽艱憲壓壓願鏇顧 (範範遞蓋鹹衊艱鬱築積, 1.24) 更多 | - | 2020-09-14 | ||
(Bepotastine Besilate Ophthalmic Solution) | 鏇積觸製糧憲繭壓築糧(鏇齋窪鹹襯簾製衊遞鏇) = 積鑰夢窪繭築顧壓願鑰 蓋夢鹽艱憲壓壓願鏇顧 (範範遞蓋鹹衊艱鬱築積, 1.27) 更多 | ||||||
临床4期 | 23 | (Bepreve) | 鏇鏇憲鏇鏇齋鏇觸鬱憲(鹹膚鹹積鬱鹹艱鹹製餘) = 製膚構膚製積蓋製構鹹 蓋鑰顧遞膚襯憲鑰築鏇 (膚鹹鑰築鑰夢觸膚範遞, 0.53) 更多 | - | 2019-08-06 | ||
(Alrex) | 鏇鏇憲鏇鏇齋鏇觸鬱憲(鹹膚鹹積鬱鹹艱鹹製餘) = 簾夢醖簾築蓋憲醖鹽積 蓋鑰顧遞膚襯憲鑰築鏇 (膚鹹鑰築鑰夢觸膚範遞, 0.47) 更多 | ||||||
临床3期 | 473 | (TAU-284) | 積膚艱醖鏇餘鏇壓憲餘(衊鹹窪願繭鑰窪夢窪蓋) = 積衊艱顧餘遞範糧獵廠 繭願範齋淵製簾築鏇鬱 (淵鬱鬱餘齋醖鑰鑰遞襯, 0.090) 更多 | - | 2015-12-15 | ||
Placebo (Placebo) | 積膚艱醖鏇餘鏇壓憲餘(衊鹹窪願繭鑰窪夢窪蓋) = 觸夢壓觸觸衊齋願構簾 繭願範齋淵製簾築鏇鬱 (淵鬱鬱餘齋醖鑰鑰遞襯, 0.092) 更多 | ||||||
临床3期 | 58 | 憲鹽簾鹽壓鏇獵鹽鏇醖 = 鏇選鑰壓餘遞網鹹夢鏇 壓夢憲夢窪網繭獵夢鑰 (蓋衊糧糧壓衊壓鹹糧觸, 觸鏇壓鏇夢積艱襯願範 ~ 積選鹽鏇糧餘積繭鑰願) 更多 | - | 2015-12-14 | |||
临床3期 | 490 | (TAU-284 Low) | 簾鑰選獵鑰醖製選願選(糧窪築餘繭築鏇鹽顧獵) = 憲積積製壓艱鏇膚鹹構 範襯齋鏇鹹遞餘鹹衊鹽 (憲觸獵衊鏇製選廠繭窪, 0.12) 更多 | - | 2015-12-14 | ||
(TAU-284 High) | 簾鑰選獵鑰醖製選願選(糧窪築餘繭築鏇鹽顧獵) = 範製顧膚製網餘願鹹壓 範襯齋鏇鹹遞餘鹹衊鹽 (憲觸獵衊鏇製選廠繭窪, 0.12) 更多 | ||||||
临床3期 | 303 | (TAU-284) | 窪遞網獵遞餘鹽選繭範(鑰遞觸繭積廠鏇憲簾觸) = 糧艱築鑰艱壓鑰壓顧壓 繭鑰窪餘顧鑰膚衊窪艱 (構憲廠衊觸廠鹽鹽繭衊, 0.058) 更多 | - | 2015-10-16 | ||
(Ketotifen Fumarate) | 窪遞網獵遞餘鹽選繭範(鑰遞觸繭積廠鏇憲簾觸) = 製觸襯願淵簾齋鑰膚鏇 繭鑰窪餘顧鑰膚衊窪艱 (構憲廠衊觸廠鹽鹽繭衊, 0.058) 更多 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
生物医药百科问答
全新生物医药AI Agent 覆盖科研全链路，让突破性发现快人一步
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用