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

Action

antagonists

Mechanism

H1 receptor antagonists(Histamine H1 receptor antagonists)

Therapeutic Areas

Immune System DiseasesInfectious DiseasesOtorhinolaryngologic Diseases+ [2]

Active Indication

PruritusRhinitis, AllergicUrticaria+ [1]

Inactive Indication

Respiration DisordersRhinitis, Allergic, Perennial

Originator Organization

Hanlim Pharm Co., Ltd.

Active Organization

Mitsubishi Tanabe Pharma Corp.

Dong-A ST Co., Ltd.

Lupin Ltd

Inactive Organization

UBE Corp.

Hanlim Pharm Co., Ltd.

DongKoo Bio & Pharm Co. Ltd.

License Organization

Mitsubishi Tanabe Pharma Corp.

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

+ [1]

Drug Highest PhaseApproved

First Approval Date

South Korea (31 Jul 2004),

Hypersensitivity

Regulation-

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Structure/Sequence

Molecular FormulaC28H31ClN2O6

InChIKeyYUVMVRKHFRSJKQ-BOXHHOBZSA-N

CAS Registry1206695-40-0

View All Structures (2)

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.

24 Feb 2025·JACS Au

Continuous Flow Decarboxylative Monofluoroalkylation Enabled by Photoredox Catalysis

Article

Author: 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.

01 Feb 2025·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

Author: 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 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
Pruritus	Thailand	Mitsubishi Tanabe Pharma Corp.	31 Dec 2019
Rhinitis, Allergic	Thailand	Mitsubishi Tanabe Pharma Corp.	31 Dec 2019
Urticaria	Thailand	Mitsubishi Tanabe Pharma Corp.	31 Dec 2019
Hypersensitivity	South Korea	Dong-A ST Co., Ltd.	31 Jul 2004

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Skin Diseases	Preclinical	South Korea	DongKoo Bio & Pharm Co. Ltd.	19 Aug 2020
Rhinitis, Allergic, Perennial	Preclinical	South Korea	Hanlim Pharm Co., Ltd.	07 Feb 2017
Pruritus	Preclinical	Japan	UBE Corp.	06 Nov 2001
Urticaria	Preclinical	Japan	UBE Corp.	30 Apr 2001
Rhinitis, Allergic	Preclinical	Japan	UBE Corp.	31 Mar 1997
Respiration Disorders	Preclinical	Japan	UBE Corp.	-
Respiration Disorders	Preclinical	Japan	Mitsubishi Tanabe Pharma Corp.	-
Urticaria	Discovery	Japan	UBE Corp.	30 Apr 2001
Rhinitis, Allergic	Discovery	Japan	UBE Corp.	31 Mar 1997

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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	frrkeuazop(wcebrubpku) = wgwilogwdi gmoxklytdi (tkhcwvirgt )	-	01 Feb 2013
				Alcaftadine	frrkeuazop(wcebrubpku) = rxzblamobo gmoxklytdi (tkhcwvirgt )