Delving into the Latest Updates on Flurbiprofen Sodium with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Flurbiprofen sodium (USP), 氟吡洛芬钠

+ [3]

Target

COX-2

Action

inhibitors

Mechanism

COX-2 inhibitors(Cyclooxygenase-2 inhibitors)

Therapeutic Areas

Immune System DiseasesInfectious DiseasesNervous System Diseases+ [2]

Active Indication

Ankylosing SpondylitisOsteoarthritisPain+ [1]

Inactive Indication

MiosisOsteoarthritis, Knee

Originator Organization

Allergan UC

Active Organization

Shanghai Zhongxi Sunve Pharmaceutical Co., Ltd.

Inactive Organization

Allergan, Inc.

Beijing Tide Pharmaceutical Co., Ltd.Mikasa Seiyaku Co. Ltd.

Drug Highest PhaseApproved

First Approval Date

United States (31 Dec 1986),

Miosis

Regulation-

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Structure/Sequence

Molecular FormulaC15H13FO2

InChIKeySYTBZMRGLBWNTM-UHFFFAOYSA-N

CAS Registry5104-49-4

View All Structures (2)

[Translation] A single-center, open, randomized, single-dose, two-period, two-sequence, crossover bioequivalence study was conducted to evaluate the bioequivalence of the test preparation, flurbiprofen gel patch (specification: 40 mg) and the reference preparation (Zepsilon®) (specification: 40 mg) in healthy adult subjects under topical conditions.

主要目的：研究外用条件下单次给予受试制剂氟比洛芬凝胶贴膏（规格：40 mg，乐明药业（苏州）有限公司）与参比制剂氟比洛芬凝胶贴膏（泽普思®，规格：40 mg；日本三笠制药株式会社）在健康受试者体内的药代动力学特征，评价外用条件下给予两种制剂的生物等效性。次要目的：1、研究受试制剂氟比洛芬凝胶贴膏（规格：40 mg）和参比制剂氟比洛芬凝胶贴膏（泽普思®）（规格：40 mg）在健康受试者中的安全性。 2、研究受试制剂氟比洛芬凝胶贴膏（规格：40 mg）和参比制剂氟比洛芬凝胶贴膏（泽普思®）（规格：40 mg）在健康受试者中的黏附性。

[Translation]

Primary objective: To study the pharmacokinetic characteristics of the test preparation flurbiprofen gel patch (specification: 40 mg, Leming Pharmaceutical (Suzhou) Co., Ltd.) and the reference preparation flurbiprofen gel patch (Zepce®, specification: 40 mg; Mikasa Pharmaceutical Co., Ltd., Japan) in healthy subjects after a single administration under topical conditions, and to evaluate the bioequivalence of the two preparations under topical conditions. Secondary objectives: 1. To study the safety of the test preparation flurbiprofen gel patch (specification: 40 mg) and the reference preparation flurbiprofen gel patch (Zepce®) (specification: 40 mg) in healthy subjects. 2. To study the adhesion of the test preparation flurbiprofen gel patch (specification: 40 mg) and the reference preparation flurbiprofen gel patch (Zepce®) (specification: 40 mg) in healthy subjects.

Start Date10 Nov 2021

Sponsor / Collaborator

Lindmik Pharmaceutical (Suzhou) Co., Ltd.

100 Clinical Results associated with Flurbiprofen Sodium

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100 Translational Medicine associated with Flurbiprofen Sodium

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100 Patents (Medical) associated with Flurbiprofen Sodium

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4,274

Literatures (Medical) associated with Flurbiprofen Sodium

01 Apr 2025·Journal of Molecular Structure

Design, synthesis, and computational docking techniques of novel 1,2,3‒triazole‒tetrazole hybrids as potential leads in the development of anticancer agents

Author: Allaka, Tejeswara Rao ; Vudari, Balaraju ; Vellaiyan, Venkatesan ; Nagarajaiah, Honnappa ; Chepuri, Kalyani ; Bhoomandla, Srinu

New flurbiprofen linked 1,2,3-triazole and tetrazole scaffolds have been designed and synthesized using a Cu(I)-catalyzed azide-alkyne cycloaddition (CuAAC).All the synthesized compounds were examined for the growth inhibition of HepG2, HuH7, MCF-7, and T-47D tumor cells and binding with focusing on the human cytochrome P 450 2C9 active site was investigated using mol. modeling.There was a strong correlation between the data from the docking studies and the biol. screening results.The cell lines that responded to the novel compound′s effects the best were HepG2 and MCF-7.Compound 5j was the most efficacious derivative among the four cancer cells (HepG2, HuH7, MCF-7, and T-47D) having IC₅₀ values of 1.89 ± 0.103, 2.86 ± 0.167, 1.66 ± 0.056, and 3.55 ± 0.045 μM, resp. and it had greater activity than doxorubicin.In addition, an in silico docking anal. was carried out to confirm the results of the experimentThe results highlight the potential of our triazole-bridged tetrazoles when combined with flurbiprofen (PDB: 1R9O) to enter the active site of human cytochrome P 450 2C9.The proposed binding mode of ligand 5 g was shown three hydrogen bonding via tetrazole with Glu427 (N24...OE1), triazole with Ala280 (N17...O) and fluoro group with Arg80 (F28...NH2) residues their internuclear distances are 2.89 Å, 2.71 Å, and 3.19 Å resp.Furthermore, the ADMET profile was assessed for each mol., and the findings of the in vitro and in silico investigations indicate that the triazoles incorporating tetrazole provide important new information for the creation of innovative anti-cancer treatments.

01 Apr 2025·Separation and Purification Technology

Using artificial neural networks to elucidate retention interactions on stationary phases with amine moieties dedicated to supercritical fluid chromatography

Author: Nováková, Lucie ; Plachka, Katerina ; Svec, Frantisek ; Plachká, Kateřina ; Pilařová, Veronika ; Gazarkova, Tatana ; Novakova, Lucie ; Švec, František ; Gazárková, Taťána ; Pilarova, Veronika ; Garrigues, Jean-Christophe

The retention mechanisms of small mols. on a wide range of stationary phases using different mobile phase compositions are one of the most discussed topics in current state-of-the-art supercritical fluid chromatog. (SFC).Although various theories have been published on retention behavior, prediction, and stability over time, an in-depth insight into the mechanisms is still lacking.Our study focused on the description of the retention mechanisms on columns with amine moieties, i.e., 2-ethylpyridine, 2-picolylamine, 1-aminoanthracene, and diethylamine, dedicated to SFC, using three different compositions of organic modifier, i.e., methanol, methanol + 10 mmol/L NH₃, and methanol + 2% H₂O, in CO₂.An extensive set of analytes characterized by more than 200 mol. descriptors was used.The importance of the effect of each mol. descriptor on the retention behavior was determined by artificial neural networks.Thus, the descriptors increasing and/or decreasing retention on individual columns using different mobile phase compositions were defined.The data collected over one year of column use were statistically evaluated to describe the retention behavior of small mols. on the tested stationary phases using three organic modifiers and to describe the changes in retention behavior over time.As the development of the SFC method can be laborious and time-consuming, this publication offers a detailed description of the interactions taking place between the analyte and the SFC stationary phase.Understanding these fundamental processes will enable faster development of SFC methods using quality-by-design principles.

14 Feb 2025·Organic Letters

Nickel/Photo-Cocatalyzed Cross-Coupling of Enol Silyl Ethers with α-Trifluoromethyl Bromides to Access β-CF₃-Substituted Ketones

Author: Jiang, Yan ; Pan, Fei ; Liao, Youzhi ; Zhao, Yi

Herein, we introduce a nickel-photocatalyzed cross-coupling reaction between enol silyl ethers and CF3-substituted alkyl bromides.This method provides a streamlined approach for synthesizing a wide array of structurally diverse β-CF3-substituted ketones, achieving favorable yields under mild conditions.The practicality of this methodol. is further underscored by its successful application in the late-stage functionalization of various pharmaceuticals and natural products.

100 Deals associated with Flurbiprofen Sodium

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External Link

KEGG	Wiki	ATC	Drug Bank
D02290	Flurbiprofen Sodium	M01AE09 M02AA19 R02AX01 S01BC04	-

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Ankylosing Spondylitis	China	Shanghai Zhongxi Sunve Pharmaceutical Co., Ltd.	01 Jan 1998
Osteoarthritis	China	Shanghai Zhongxi Sunve Pharmaceutical Co., Ltd.	01 Jan 1998
Pain	China	Shanghai Zhongxi Sunve Pharmaceutical Co., Ltd.	01 Jan 1998
Rheumatoid Arthritis	China	Shanghai Zhongxi Sunve Pharmaceutical Co., Ltd.	01 Jan 1998

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Osteoarthritis, Knee	Preclinical	China	Mikasa Seiyaku Co. Ltd.	31 Mar 2020
Osteoarthritis, Knee	Preclinical	China	Beijing Tide Pharmaceutical Co., Ltd.	31 Mar 2020