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

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.

31 Dec 2024·Emerging Microbes & Infections

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

Article

Author: Li, Yaqin ; Cao, Lei ; Hui, Xianfeng ; Sun, Xiaomei ; Huang, Kun ; Zhao, Ya ; 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.

01 Aug 2024·Hospital Pharmacy

Cost-effectiveness Analysis of Second-Generation Antihistamine 1 Receptor Blockers and Japanese Kampo Shoseiryuto for Treating Perennial Allergic Rhinitis in Outpatient Settings in Japan

Article

Author: Kashiwabara, Masami ; Egawa, Kei ; Nakagawa, Naoto ; Sasaki, Ayaka

Objectives: Perennial allergic rhinitis (PAR) is common in Japan. Second-generation antihistamines (SGAs) are commonly used for its treatment; however, it remains unclear which SGA is the most cost-effective. Additionally, the pharmacoeconomics of Japanese Kampo shoseiryuto (which was traditionally prescribed to treat PAR in Japan) remains poorly understood. In this study, we aimed to investigate the effectiveness of various SGAs and shoseiryuto for the treatment of PAR in Japanese outpatients, from the healthcare payer’s perspective. Methods: The most cost- and clinically effective SGAs were determined from a list of 6 SGAs (bepotastine, 10 mg; cetirizine, 10 mg; ebastine, 10 mg; epinastine, 20 mg; loratadine, 10 mg; and olopatadine, 5 mg) together with shoseiryuto, using the overall improvement rate through a model-based analysis. The time horizon was 28 days. Costs were determined based on the Medical Fee Index in 2020. Deterministic and probabilistic sensitivity analyses were conducted to address the uncertainty of the base-case results. Results: Overall, bepotastine (10 mg) and ebastine (10 mg) were cost-effective. Shoseiryuto was less cost-effective than ebastine (10 mg) (dominated). Ebastine (10 mg) was the most cost-effective option based on deterministic and probabilistic sensitivity analyses. Conclusions: Ebastine (10 mg) was the most cost-effective treatment strategy for PAR among the agents evaluated in this study. This insight could aid in establishing an appropriate formulary for treating PAR in hospitals and communities.

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
Rhinitis, Allergic	Preclinical	SG	Mitsubishi Tanabe Pharma Corp.	31 Mar 2019
Urticaria	Preclinical	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	onwvldidra(ihetkofmdk) = grhcftujzh djuwintcwb (arodnfexjp )	-	01 Feb 2013
				Alcaftadine	onwvldidra(ihetkofmdk) = vaviyaldah djuwintcwb (arodnfexjp )