Delving into the Latest Updates on Acrivastine with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

acrivastina, Benadryl Allergy Relief

Target

H1 receptor

Action

antagonists

Mechanism

H1 receptor antagonists(Histamine H1 receptor antagonists)

Therapeutic Areas

Immune System DiseasesInfectious DiseasesOtorhinolaryngologic Diseases+ [2]

Active Indication

Chronic UrticariaRhinitis, Allergic

Inactive Indication

Allergic skin reactionDermatographic urticariaEczema+ [1]

Originator Organization

McNeil Products Ltd.

Active Organization

Brown & Burk UK Ltd.McNeil Products Ltd.

Inactive Organization

Wellcome Foundation Ltd

License Organization-

Drug Highest PhaseApproved

First Approval Date

United Kingdom (17 Sep 1997),

Chronic UrticariaRhinitis, Allergic

Regulation-

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Structure/Sequence

Molecular FormulaC22H24N2O2

InChIKeyPWACSDKDOHSSQD-IUTFFREVSA-N

CAS Registry87848-99-5

通过健康受试者在空腹和餐后状态下分别单次口服由重庆华邦制药有限公司的受试制剂（阿伐斯汀胶囊，规格8mg，欣西®）与McNeil Products Ltd的参比制剂（阿伐斯汀胶囊，规格8mg，Benadryl® Allergy Relief），进行人体相对生物利用度研究，评价受试制剂与参比制剂的生物等效性。

[Translation]

A relative bioavailability study was conducted in healthy subjects by taking a single oral dose of the test formulation (Avastin Capsules, 8 mg, Xinxi®) produced by Chongqing Huabang Pharmaceutical Co., Ltd. and the reference formulation (Avastin Capsules, 8 mg, Benadryl® Allergy Relief) produced by McNeil Products Ltd. in the fasting and fed states, respectively, to evaluate the bioequivalence of the test formulation and the reference formulation.

Start Date20 May 2019

Sponsor / Collaborator

Chongqing Huapont Pharmaceutical Co. Ltd.

ChiCTR-IPR-17011515

/ RecruitingPhase 4IIT

Efficacy and safety of Acrivastine combined with Clarityne in patients with chronic and intractable urticaria

Start Date01 May 2017

Sponsor / Collaborator-

100 Clinical Results associated with Acrivastine

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100 Translational Medicine associated with Acrivastine

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100 Patents (Medical) associated with Acrivastine

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270

Literatures (Medical) associated with Acrivastine

01 Jun 2025·Injury

Repurposing of activating transcription factor 3 (ATF3) activator molecules with potential wound-healing effects

Article

Author: De Jesus-González, Luis A ; Santos-Mena, Alan ; Trujillo-Paez, Valentin ; Jacobo-Delgado, Yolanda M ; Gonzalez-Curiel, Irma ; Felix-Arellano, Camelia ; Rivas-Santiago, Bruno

BACKGROUNDWound healing is a complex and regulated process that involves the coordinated action of key signaling pathways. Activating transcription factor 3 (ATF3) is a stress-inducible protein that has recently emerged as a critical modulator of cellular responses to injury, including those involved in wound healing.AIMThe aim of this study was to explore the repurposing of existing pharmacological agents to activate ATF3 and evaluate their potential to enhance wound healing factors.METHODSWe selected three compounds: retin-A, furosemide, and acrivastine based on their ability to modulate ATF3 expression and assessed their effects on wound healing processes in primary cell cultures. We evaluated wound healing-related genes such as LL-37, HBD-2, HBD-3, and VEGFA by qPCR, and a wound healing scratch assay using keratinocytes was conducted to evaluate cell migration.RESULTSInterestingly, retin-A induced the expression of key wound healing-related genes, including HBD-2, HBD-3, LL-37, and VEGF. Also, retin-A was the only compound showing wound healing effects, while furosemide and acrivastine did not exhibit any noticeable activity.CONCLUSIONOur research highlights the potential of retin-A as therapeutic agents to improve wound healing, particularly in chronic wound models.

09 Jan 2025·Journal of Medicinal Chemistry

Probing the Histamine H₁ Receptor Binding Site to Explore Ligand Binding Kinetics

Article

Author: Kooistra, Albert J. ; Vischer, Henry F. ; Kuhne, Sebastiaan ; de Esch, Iwan J. P. ; Leurs, Rob ; Riemens, Rick ; Stroet, Marc C. M. ; de Graaf, Chris ; Wijtmans, Maikel ; Bosma, Reggie

Analysis of structure-kinetic relationships (SKR) can contribute to an improved understanding of receptor-ligand interactions. Here, fragment 1 (4-(2-benzylphenoxy)-1-methylpiperidine) was used in different fragment growing approaches to mimic the putative binding mode of the long residence time (RT) ligands olopatadine, acrivastine, and levocetirizine at the histamine H₁ receptor (H₁R). SKR analyses reveal that introduction of a carboxylic acid moiety can increase RT at H₁R up to 11-fold. Ligand efficiency (LE) decreases upon the introduction of the negatively charged group, whereas kinetic efficiency (KE) increases up to 8.5-fold. The olopatadine/acrivastine mimics give up to 15-fold differences in the RT, while the levocetirizine mimics afford similar RTs with only a 3-fold difference. Therefore, the levocetirizine mimics are less sensitive to structural changes. This study illustrates that for H₁R, there are several ways to increase RT but the different strategies differ significantly in SKR.

14 Aug 2024·mBio

The histamine receptor H1 acts as an alternative receptor for SARS-CoV-2

Article

Author: Yu, Fei ; Pan, Ting ; Liu, Han ; Liu, Guangyan ; Tu, Tianyong ; Liang, Taizhen ; Liu, Ruxin ; Li, Xinyu ; Liu, Sen ; Zhang, Zhenglai ; Xiao, Shiqi ; Liu, Xiaoqing ; Li, Peiwen ; Ma, Xiancai ; Lv, Xi ; Zhang, Hui ; Zhu, Yiqiang ; Ou, Hailan ; Wei, Xuepeng ; Chen, Tao ; Hu, Meilin

ABSTRACTNumerous host factors, in addition to human angiotensin-converting enzyme 2 (hACE2), have been identified as coreceptors of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), demonstrating broad viral tropism and diversified druggable potential. We and others have found that antihistamine drugs, particularly histamine receptor H1 (HRH1) antagonists, potently inhibit SARS-CoV-2 infection. In this study, we provided compelling evidence that HRH1 acts as an alternative receptor for SARS-CoV-2 by directly binding to the viral spike protein. HRH1 also synergistically enhanced hACE2-dependent viral entry by interacting with hACE2. Antihistamine drugs effectively prevent viral infection by competitively binding to HRH1, thereby disrupting the interaction between the spike protein and its receptor. Multiple inhibition assays revealed that antihistamine drugs broadly inhibited the infection of various SARS-CoV-2 mutants with an average IC50 of 2.4 µM. The prophylactic function of these drugs was further confirmed by authentic SARS-CoV-2 infection assays and humanized mouse challenge experiments, demonstrating the therapeutic potential of antihistamine drugs for combating coronavirus disease 19.IMPORTANCEIn addition to human angiotensin-converting enzyme 2, severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) can utilize alternative cofactors to facilitate viral entry. In this study, we discovered that histamine receptor H1 (HRH1) not only functions as an independent receptor for SARS-CoV-2 but also synergistically enhances ACE2-dependent viral entry by directly interacting with ACE2. Further studies have demonstrated that HRH1 facilitates the entry of SARS-CoV-2 by directly binding to the N-terminal domain of the spike protein. Conversely, antihistamine drugs, primarily HRH1 antagonists, can competitively bind to HRH1 and thereby prevent viral entry. These findings revealed that the administration of repurposable antihistamine drugs could be a therapeutic intervention to combat coronavirus disease 19.

100 Deals associated with Acrivastine

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