Bepotastine salicylate(Bepotastine salicylate) - 药物靶点：H1 receptor_在研适应症：瘙痒，过敏性鼻炎，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

作用方式

拮抗剂

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

瘙痒过敏性鼻炎荨麻疹+ [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

Mitsubishi Tanabe Pharma Corp.

Dong-A ST Co., Ltd.

Lupin Ltd

非在研机构

UBE Corp.

Hanlim Pharm Co., Ltd.

DongKoo Bio & Pharm Co. Ltd.

权益机构

Mitsubishi Tanabe Pharma Corp.

ISTA Pharmaceuticals, Inc.Senju Pharmaceutical Co., Ltd.

+ [1]

最高研发阶段批准上市

首次获批日期

韩国 (2004-07-31),

超敏反应

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C28H31ClN2O6

InChIKeyYUVMVRKHFRSJKQ-BOXHHOBZSA-N

CAS号1206695-40-0

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关联

12

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

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100 项与 Bepotastine salicylate 相关的转化医学

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100 项与 Bepotastine salicylate 相关的专利（医药）

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101

项与 Bepotastine salicylate 相关的文献（医药）

2025-03-31·Die Pharmazie

Direct comparison of the effects of first- and second-generation H₁ -receptor blockers on motor functions in mice.

Article

作者: Okamoto, Y ; Sakamoto, Y ; Enoki, Y ; Hara, R ; Tenjin, K ; Shimada, A ; Matsumoto, K ; Hori, S ; Taguchi, K ; Kizu, J ; Iketani, O

Histamine H1 receptor (H1R) antagonists are widely used to treat allergic reactions; however, their effects on the central nervous system can impair motor functions. This study investigated the impact of first-generation (diphenhydramine and d -chlorpheniramine) and second-generation (epinastine, ketotifen, bepotastine, and levocetirizine) H1R antagonists on motor functions in mice using activity wheel, balance beam, inclined screen, and rotarod tests. First-generation H1R antagonists significantly impaired motor functions, with diphenhydramine exerting stronger effects than those of d -chlorpheniramine. Among the second-generation agents, bepotastine and levocetirizine had minimal effects on all motor functions, whereas epinastine and ketotifen suppressed spontaneous movement, similar to first-generation H1R antagonists but had little effects on balance, postural stability, and coordinated movement. These findings provide valuable insights into the differential effects of first- and second-generation H1R antagonists on motor functions. These results highlight the importance of understanding individual profiles of H1R antagonists to minimize adverse effects, ensure patient safety, and improve quality of life.

2025-02-24·JACS Au

Continuous Flow Decarboxylative Monofluoroalkylation Enabled by Photoredox Catalysis

Article

作者: Andresini, Michael ; Colella, Marco ; Natho, Philipp ; Gelato, Yuri ; Pasca, Francesco ; Serbetci, Defne ; Romanazzi, Giuseppe ; Degennaro, Leonardo ; Luisi, Renzo

Herein, we report a scalable and mild strategy for the monofluoroalkylation of a wide array of Giese acceptors via visible-light-mediated photoredox catalysis in continuous flow. The use of flow technology significantly enhances productivity and scalability, whereas mildness of conditions and functional group tolerance are ensured by leveraging 4CzIPN, a transition-metal-free organic photocatalyst. Structurally diverse secondary and tertiary monofluoroalkyl radicals can thus be accessed from readily available α-monofluorocarboxylic acids. Given the mild reaction conditions, this protocol is also amenable to the late-stage functionalization of biologically relevant molecules such as menthol, amantadine, bepotastine, and estrone derivatives, rendering it suitable for application to drug discovery programs, for which the introduction of fluorinated fragments is highly sought after. This method was also extended to enable a reductive multicomponent radical-polar crossover transformation to rapidly increase the complexity of the assembled fluorinated architectures in a single synthetic operation.

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.

100 项与 Bepotastine salicylate 相关的药物交易

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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,

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适应症	国家/地区	公司	日期
瘙痒	泰国	Mitsubishi Tanabe Pharma Corp.	2019-12-31
过敏性鼻炎	泰国	Mitsubishi Tanabe Pharma Corp.	2019-12-31
荨麻疹	泰国	Mitsubishi Tanabe Pharma Corp.	2019-12-31
超敏反应	韩国	Dong-A ST Co., Ltd.	2004-07-31

未上市

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
皮肤疾病	临床前	韩国	DongKoo Bio & Pharm Co. Ltd.	2020-08-19
常年性变应性鼻炎	临床前	韩国	Hanlim Pharm Co., Ltd.	2017-02-07
瘙痒	临床前	日本	UBE Corp.	2001-11-06
荨麻疹	临床前	日本	UBE Corp.	2001-04-30
过敏性鼻炎	临床前	日本	UBE Corp.	1997-03-31
呼吸障碍	临床前	日本	UBE Corp.	-
呼吸障碍	临床前	日本	Mitsubishi Tanabe Pharma Corp.	-
荨麻疹	药物发现	日本	UBE Corp.	2001-04-30
过敏性鼻炎	药物发现	日本	UBE Corp.	1997-03-31

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临床结果

适应症

分期

评价

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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	糧選鹹衊鬱簾鬱膚鹹淵(膚鏇鏇鬱憲鏇鹽襯積醖) = 觸製網壓醖壓願範餘廠窪製廠窪選齋蓋範願鬱 (鏇夢鹽製鹽廠鑰願衊艱 )	-	2013-02-01
				Alcaftadine	糧選鹹衊鬱簾鬱膚鹹淵(膚鏇鏇鬱憲鏇鹽襯積醖) = 蓋範夢範範築鬱淵構積窪製廠窪選齋蓋範願鬱 (鏇夢鹽製鹽廠鑰願衊艱 )