Bepotastine salicylate(Bepotastine salicylate) - 药物靶点：H1 receptor_在研适应症：超敏反应，瘙痒，荨麻疹_专利_临床

概要

基本信息

药物类型

小分子化药

别名

BELION、Bepotastine、Bepotastine sustained-release

+ [4]

靶点

H1 receptor

作用机制

H1 receptor拮抗剂(组胺H1受体拮抗剂)

治疗领域

免疫系统疾病感染耳鼻咽喉疾病+ [2]

在研适应症

超敏反应瘙痒荨麻疹+ [1]

非在研适应症

呼吸障碍常年性变应性鼻炎

原研机构

Hanlim Pharm Co., Ltd.

在研机构

UBE Corp.

Mitsubishi Tanabe Pharma Corp.

Lupin Ltd

+ [1]

非在研机构

Hanlim Pharm Co., Ltd.

DongKoo Bio & Pharm Co. Ltd.

最高研发阶段批准上市

首次获批日期

日本 (2000-10-27),

过敏性鼻炎

最高研发阶段(中国)-

特殊审评-

登录后查看时间轴

结构/序列

分子式C28H31ClN2O6

InChIKeyYUVMVRKHFRSJKQ-BOXHHOBZSA-N

CAS号1206695-40-0

查看全部结构式(2)

关联

13

项与 Bepotastine salicylate 相关的临床试验

CTRI/2022/11/047129

/ Not yet recruiting临床4期IIT

Double blinded randomized Controlled Study Comparing the Efficacy and Tolerance of levocetrizine, Bilastine and Bepotastine in Patients with Urticaria.

开始日期2022-11-10

申办/合作机构-

NCT04877678

/ Completed临床4期IIT

Effects of Second-generation Antihistamine Bepotastine on Cough Outcomes in Cough Patients With Allergic Rhinitis: A Randomized, Double-blind, Placebo Controlled Study

This is a phase 4 study to evaluate the the efficacy of second generation antihistamine on cough outcomes in cough patients with allergic rhinitis.

开始日期2021-10-01

申办/合作机构

Asan Medical Center

KCT0006104

/ Completed临床1期

An open-label, randomized, single-dose, 2-sequence, 2-period, cross-over phase 1 study under fed state to evaluate the safety and pharmacokinetics of DKB19003” in healthy adult volunteers

开始日期2021-04-05

申办/合作机构

DongKoo Bio & Pharm Co. Ltd.

100 项与 Bepotastine salicylate 相关的临床结果

登录后查看更多信息

100 项与 Bepotastine salicylate 相关的转化医学

登录后查看更多信息

100 项与 Bepotastine salicylate 相关的专利（医药）

登录后查看更多信息

58

项与 Bepotastine salicylate 相关的文献（医药）

2025-02-01·Spectrochimica 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 ; El-Deen, Asmaa Kamal ; Saad, Aya Magdy

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.

2025-01-01·Asian 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, Dae Woo ; Kim, Jeong-Whun ; Rhee, Chae-Seo ; Kim, Sung Wan ; Kim, Soo Whan ; Kim, Chang-Hoon ; Kim, Hyung Gu ; Kim, Jin Kook ; Kim, Hyo Yeol ; Won, Tae-Bin ; Kim, Young Hyo

BACKGROUNDThe efficacy of rupatadine for the treatment of AR has been confirmed in numerous clinical studies, however there are very few studies on asian patients.OBJECTIVETo assess the safety and efficacy of rupatadine fumarate in the treatment of Korean perennial allergic rhinitis (PAR) patients.METHODSA 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.RESULTSRupatadine 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.CONCLUSIONSRupatadine is a safe and effective treatment option for Korean PAR patients and possibly a better choice over bepotastine for controlling morning symptom.

2024-12-31·Emerging Microbes & Infections

Inhibition of RAN attenuates influenza a virus replication and nucleoprotein nuclear export

Article

作者: Li, Yaqin ; Cao, Lei ; Sun, Xiaomei ; Huang, Kun ; Zhao, Ya ; Hui, Xianfeng ; Mao, Haiying ; Lin, Xian ; Zhao, Lianzhong ; Jin, Meilin ; Zhang, Yumei ; Cheng, Chuxing ; Wang, Ting ; Xu, Ting ; She, Ziwei

Nuclear export of the viral ribonucleoprotein (vRNP) is a critical step in the influenza A virus (IAV) life cycle and may be an effective target for the development of anti-IAV drugs. The host factor ras-related nuclear protein (RAN) is known to participate in the life cycle of several viruses, but its role in influenza virus replication remains unknown. In the present study, we aimed to determine the function of RAN in influenza virus replication using different cell lines and subtype strains. We found that RAN is essential for the nuclear export of vRNP, as it enhances the binding affinity of XPO1 toward the viral nuclear export protein NS2. Depletion of RAN constrained the vRNP complex in the nucleus and attenuated the replication of various subtypes of influenza virus. Using in silico compound screening, we identified that bepotastine could dissociate the RAN-XPO1-vRNP trimeric complex and exhibit potent antiviral activity against influenza virus both in vitro and in vivo. This study demonstrates the important role of RAN in IAV replication and suggests its potential use as an antiviral target.

100 项与 Bepotastine salicylate 相关的药物交易

登录后查看更多信息

外链

KEGG	Wiki	ATC	Drug Bank
-	-	R06	DB04890

研发状态

批准上市

10 条最早获批的记录,

登录

后查看更多信息

适应症	国家/地区	公司	日期
超敏反应	韩国	Dong-A ST Co., Ltd.	2004-07-31
瘙痒	日本	UBE Corp.	2002-01-30
荨麻疹	日本	UBE Corp.	2002-01-30
过敏性鼻炎	日本	UBE Corp.	2000-10-27

未上市

10 条进展最快的记录,

登录

后查看更多信息

适应症	最高研发状态	国家/地区	公司	日期
皮肤疾病	临床2期	韩国	DongKoo Bio & Pharm Co. Ltd.	2020-08-19
荨麻疹	临床2期	新加坡	Mitsubishi Tanabe Pharma Corp.	2019-03-31
瘙痒	临床2期	韩国	Hanlim Pharm Co., Ltd.	2017-05-17
常年性变应性鼻炎	临床2期	韩国	Hanlim Pharm Co., Ltd.	2017-02-07
呼吸障碍	临床2期	日本	Mitsubishi Tanabe Pharma Corp.	-
呼吸障碍	临床2期	日本	UBE Corp.	-
过敏性鼻炎	药物发现	新加坡	Mitsubishi Tanabe Pharma Corp.	2019-03-31
荨麻疹	药物发现	新加坡	Mitsubishi Tanabe Pharma Corp.	2019-03-31

登录后查看更多信息

临床结果

适应症

分期

评价

查看全部结果

研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


AAAAI2013	N/A	-	-	Olopatadine	願網膚觸獵繭憲範選蓋(鹹廠簾願艱網構憲壓壓) = 鏇觸積獵糧夢糧鬱築繭糧艱顧構築淵艱醖蓋膚 (夢膚窪窪製繭衊鹹憲廠 )	-	2013-02-01
				Alcaftadine	願網膚觸獵繭憲範選蓋(鹹廠簾願艱網構憲壓壓) = 廠糧獵範憲憲艱願遞齋糧艱顧構築淵艱醖蓋膚 (夢膚窪窪製繭衊鹹憲廠 )