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

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

Drug Highest PhaseApproved

First Approval Date

GB (17 Sep 1997),

Chronic UrticariaRhinitis, Allergic

Regulation-

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Structure

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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159

Literatures (Medical) associated with Acrivastine

01 Oct 2023·Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association

Toxicological profiling of a de novo synthesized benzimidazole derivative with potent and selective proapoptotic potentials against breast cancer.

Article

Author: Shawky, Heba ; Shaker, Sylvia E ; Farrag, Ebtehal K ; Aziz, Wessam M ; Fayed, Dalia B

This study aimed to investigate the toxicological profile of 1-(6-(1H-benzo[d]imidazole-2-yl)-2-methylpyridin-3-yl) ethanone (BMPE), both in vitro and in vivo. The proapoptotic/necrotic and cell cycle arrest potentials of BMPE were assessed in MCF-7 cell line. The in vivo toxicology was assessed in female Balb/c mice by repeated dosing of 5, 25, and 50 mg/kg for 21 consecutive days, then different biochemical, inflammatory, and oxidative markers were assessed in sera/tissue homogenates of treated animals. The new derivative showed a potent selective cytotoxicity against malignant cell lines with IC₅₀ value 0.2 μM/mL, while the cytotoxic effect on normal Wi-38 cells was observed at IC₅₀ value 0.4 μM/mL; i.e. twofold the effective anticancer dose. BMPE exhibited an early DNA fragmentation-derived cell apoptosis observed at the G0/G1 checkpoint. In vivo, BMPE was biochemically/immunologically tolerable at a pharmacological dose range of 5-25 mg/kg, with no significant rates of mortality/morbidity and minimal-to-moderate histopathological alterations recorded. The new derivative represents an attractive therapeutic candidate for breast cancer, considering its noticeable modulatory effect on the oxidative-inflammatory axis that would relate to its potent antitumor effect.

01 Aug 2023·European Journal of Medicinal Chemistry

Optimization and evaluation of pyridinyl vinyl sulfones as Nrf2 activator for the antioxidant and anti-inflammatory effects

Article

Author: Kim, Jushin ; Kim, Byungeun ; Kim, Yoowon ; Lee, Elijah Hwejin ; Park, Sun Jun ; Choi, Ji Won ; Kim, Hyeon Jeong ; Park, Jong-Hyun ; Kim, Rium ; Kim, Jaehwan ; Park, Ki Duk

Many studies have reported that chalcone-based compounds exhibit biol. activities such as anticancer, antioxidant, anti-inflammatory and neuroprotective effects.Among the published chalcone derivatives, (E)-1-(3-methoxypyridin-2-yl)-3-(2-(trifluoromethyl)phenyl)prop-2-en-1-one (VEDA-1209), which is currently undergoing preclin. study, was selected as a starting compound for the development of new nuclear factor erythroid 2-related factor 2 (Nrf2) activators.Based on our previous knowledge, we attempted to redesign and synthesize VEDA-1209 derivatives by introducing the pyridine ring and sulfone moiety to ameliorate its Nrf2 efficacy and drug-like properties.Among the synthesized compounds, (E)-3-chloro-2-(2-((3-methoxypyridin-2-yl)sulfonyl)vinyl) pyridine (10e) was found to have approx. 16-folds higher Nrf2 activating effects than VEDA-1209 (10e: EC50 = 37.9 nM vs VEDA-1209: EC50 = 625 nM) in functional cell-based assay.In addition, 10e effectively improved drug-like properties such as CYP inhibition probability and metabolic stability.Finally, 10e demonstrated excellent antioxidant and anti-inflammatory effects in BV-2 microglial cells and significantly restored spatial memory deficits in lipopolysaccharide (LPS)-induced neuroinflammatory mouse models.

28 May 2023·IUCrData

(E)-5-(4-Methoxyphenyl)-N′-(2-oxoindolin-3-ylidene)-1-phenyl-1H-pyrazole-3-carbohydrazide

Article

Author: Farahat, Abdelbasset A ; Yousif, Emad ; Bekheit, Mohamed S ; Abdel-Wahab, Bakr F ; El-Hiti, Gamal A ; Kariuki, Benson M

The asymmetric unit of the title compound, C25H19N5O3, is composed of two independent molecules with slightly different conformations. The extended structure features N—H...O hydrogen bonds as well as π–π interactions.

100 Deals associated with Acrivastine

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