Delving into the Latest Updates on Bepotastine salicylate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

BELION, Bepotastine, Bepotastine sustained-release

+ [4]

Target

H1 receptor

Mechanism

H1 receptor antagonists(Histamine H1 receptor antagonists)

Therapeutic Areas

Immune System DiseasesInfectious DiseasesOtorhinolaryngologic Diseases+ [2]

Active Indication

HypersensitivityPruritusUrticaria+ [1]

Inactive Indication

Respiration DisordersRhinitis, Allergic, Perennial

Originator Organization

Hanlim Pharm Co., Ltd.

Active Organization

UBE Corp.

Mitsubishi Tanabe Pharma Corp.

Lupin Ltd

+ [1]

Inactive Organization

Hanlim Pharm Co., Ltd.

DongKoo Bio & Pharm Co. Ltd.

Drug Highest PhaseApproved

First Approval Date

JP (27 Oct 2000),

Rhinitis, Allergic

Regulation-

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Structure/Sequence

Molecular FormulaC28H31ClN2O6

InChIKeyYUVMVRKHFRSJKQ-BOXHHOBZSA-N

CAS Registry1206695-40-0

View All Structures (2)

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.

01 Jan 2025·Asian Pacific Journal of Allergy and ImmunologyQ4 · MEDICINE

Efficacy and safety of rupatadine fumarate in the treatment of perennial allergic rhinitis: A multicenter, double-blinded, randomized, placebo-controlled, bridging study in Koreans

Q4 · MEDICINE

Article

Author: 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.

31 Dec 2024·Emerging Microbes & Infections

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

Article

Author: 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 Deals associated with Bepotastine salicylate

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External Link

KEGG	Wiki	ATC	Drug Bank
-	-	R06	DB04890

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Hypersensitivity	KR	Dong-A ST Co., Ltd.	31 Jul 2004
Pruritus	JP	UBE Corp.	30 Jan 2002
Urticaria	JP	UBE Corp.	30 Jan 2002
Rhinitis, Allergic	JP	UBE Corp.	27 Oct 2000

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Skin Diseases	Phase 2	KR	DongKoo Bio & Pharm Co. Ltd.	19 Aug 2020
Urticaria	Phase 2	SG	Mitsubishi Tanabe Pharma Corp.	31 Mar 2019
Pruritus	Phase 2	KR	Hanlim Pharm Co., Ltd.	17 May 2017
Rhinitis, Allergic, Perennial	Phase 2	KR	Hanlim Pharm Co., Ltd.	07 Feb 2017
Respiration Disorders	Phase 2	JP	Mitsubishi Tanabe Pharma Corp.	-
Respiration Disorders	Phase 2	JP	UBE Corp.	-
Rhinitis, Allergic	Discovery	SG	Mitsubishi Tanabe Pharma Corp.	31 Mar 2019
Urticaria	Discovery	SG	Mitsubishi Tanabe Pharma Corp.	31 Mar 2019

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


AAAAI2013	Not Applicable	-	-	Olopatadine	pgkolvlfnx(uxdrwlvhjb) = taknhxumic hyfenycdte (tkgahwxntj )	-	01 Feb 2013
				Alcaftadine	pgkolvlfnx(uxdrwlvhjb) = wbwjwcoilo hyfenycdte (tkgahwxntj )