Delving into the Latest Updates on Ibuprofen Piconol with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Ibuprofen piconol (JP17/USAN), イブプロフェンピコノール, ピメプロフェン

+ [6]

Target

COX-1 x COX-2

Action

inhibitors

Mechanism

COX-1 inhibitors(Cyclooxygenase-1 inhibitors), COX-2 inhibitors(Cyclooxygenase-2 inhibitors)

Therapeutic Areas

Immune System DiseasesInfectious DiseasesCongenital Disorders+ [1]

Active Indication

Acne VulgarisAcute eczemaChronic eczema+ [5]

Inactive Indication-

Originator Organization

Torii Pharmaceutical Co., Ltd.

Active Organization

Hisamitsu Pharmaceutical Co., Inc.

Torii Pharmaceutical Co., Ltd.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

Japan (17 Mar 1984),

Acute eczemaChronic eczemaDermatitis, Atopic+ [4]

Regulation-

Login to view timeline

Structure/Sequence

Molecular FormulaC19H23NO2

InChIKeyACEWLPOYLGNNHV-UHFFFAOYSA-N

CAS Registry64622-45-3

本试验为正式试验，旨在研究局部涂抹汕头经济特区鮀滨制药厂研制、生产的布洛芬吡甲酯乳膏（T：10 g﹕0.5 g）的药代动力学特征；以鳥居薬品株式会社生产的布洛芬吡甲酯乳膏（STADERM®，R：10 g﹕0.5 g）为参比制剂，评价受试制剂与参比制剂在布洛芬/布洛芬吡甲酯上的药动学参数（Cmax、AUC0-t、AUC0-∞）的差异性，并评价受试制剂的安全性。

[Translation]

This test is a formal test, aiming to study the pharmacokinetic characteristics of topical application of ibuprofen methylpyridin cream (T: 10 g﹕0.5 g) developed and produced by Tuobin Pharmaceutical Factory in Shantou Special Economic Zone; Ibuprofen methylpyridine cream (STADERM®, R: 10 g﹕0.5 g) produced by Co., Ltd. is a reference preparation. The test preparation and the reference preparation are evaluated on ibuprofen/ibuprofen methylpyridine. Differences in pharmacokinetic parameters (Cmax, AUC0-t, AUC0-∞), and evaluate the safety of the test preparations.

Start Date-

Sponsor / Collaborator

Shandong Bestcomm Pharmaceutical Co., Ltd.

CTR20182207

/ Not yet recruitingNot Applicable

布洛芬吡甲酯软膏单中心、随机、开放、单剂量、平行试验设计人体药代动力学比较研究

[Translation] Comparative study on the pharmacokinetics of ibuprofen methylpyrifos ointment in humans using a single-center, randomized, open-label, single-dose, parallel trial design

本试验为正式试验，旨在研究局部涂抹汕头经济特区鮀滨制药厂研制、生产的布洛芬吡甲酯软膏（T：10 g﹕0.5 g）的药代动力学特征；以鳥居薬品株式会社生产的布洛芬吡甲酯软膏（STADERM®，R：10 g﹕0.5 g）为参比制剂，评价受试制剂与参比制剂在布洛芬/布洛芬吡甲酯上的药动学参数（Cmax、AUC0-t、AUC0-∞）的差异性，并评价受试制剂的安全性。

[Translation]

This test is a formal test, aiming to study the pharmacokinetic characteristics of topical application of ibuprofen methyl methyl ointment (T: 10 g: 0.5 g) developed and produced by Tuobin Pharmaceutical Factory in Shantou Special Economic Zone; Torii Ointment Co., Ltd. Ibuprofen methylpyridine ointment (STADERM®, R: 10 g﹕0.5 g) produced by the company is a reference preparation. The pharmacodynamics of the test preparation and the reference preparation on ibuprofen/ibuprofen methylpyridine are evaluated. The differences in chemical parameters (Cmax, AUC0-t, AUC0-∞) were evaluated, and the safety of the test preparations was evaluated.

Start Date-

Sponsor / Collaborator

Shandong Bestcomm Pharmaceutical Co., Ltd.

100 Clinical Results associated with Ibuprofen Piconol

Login to view more data

100 Translational Medicine associated with Ibuprofen Piconol

Login to view more data

100 Patents (Medical) associated with Ibuprofen Piconol

Login to view more data

46

Literatures (Medical) associated with Ibuprofen Piconol

05 Jan 2025·Journal of Computational Chemistry

CGPDTA: An Explainable Transfer Learning‐Based Predictor With Molecule Substructure Graph for Drug‐Target Binding Affinity

Article

Author: Shen, Jun ; Zhang, Simeng ; Chen, Yadong ; Ning, Xiangzhen ; Zhang, Yanmin ; Liu, Yingxu ; Han, Weijie ; Xu, Chengcheng ; Liu, Haichun ; Fan, Qing

ABSTRACTIdentifying interactions between drugs and targets is crucial for drug discovery and development. Nevertheless, the determination of drug‐target binding affinities (DTAs) through traditional experimental methods is a time‐consuming process. Conventional approaches to predicting drug‐target interactions (DTIs) frequently prove inadequate due to an insufficient representation of drugs and targets, resulting in ineffective feature capture and questionable interpretability of results. To address these challenges, we introduce CGPDTA, a novel deep learning framework empowered by transfer learning, designed explicitly for the accurate prediction of DTAs. CGPDTA leverages the complementarity of drug–drug and protein–protein interaction knowledge through advanced drug and protein language models. It further enhances predictive capability and interpretability by incorporating molecular substructure graphs and protein pocket sequences to represent local features of drugs and targets effectively. Our findings demonstrate that CGPDTA not only outperforms existing methods in accuracy but also provides meaningful insights into the predictive process, marking a significant advancement in the field of drug discovery.

01 Mar 2023·Journal of Biological Chemistry

Early-phase drug discovery of β-III-spectrin actin-binding modulators for treatment of spinocerebellar ataxia type 5

Article

Author: Avery, Adam W ; Keller, Amanda R ; Rebbeck, Robyn T ; Carter, Anna L ; Hays, Thomas S ; Atang, Alexandra E ; Denha, Sarah A ; Svensson, Bengt ; Thomas, David D ; Guhathakurta, Piyali

β-III-Spectrin is a key cytoskeletal protein that localizes to the soma and dendrites of cerebellar Purkinje cells and is required for dendritic arborization and signaling. A spinocerebellar ataxia type 5 L253P mutation in the cytoskeletal protein β-III-spectrin causes high-affinity actin binding. Previously we reported a cell-based fluorescence assay for identification of small-molecule actin-binding modulators of the L253P mutant β-III-spectrin. Here we describe a complementary, in vitro, fluorescence resonance energy transfer (FRET) assay that uses purified L253P β-III-spectrin actin-binding domain (ABD) and F-actin. To validate the assay for high-throughput compatibility, we first confirmed that our 50% FRET signal was responsive to swinholide A, an actin-severing compound, and that this yielded excellent assay quality with a Z' value > 0.77. Second, we screened a 2684-compound library of US Food and Drug Administration-approved drugs. Importantly, the screening identified numerous compounds that decreased FRET between fluorescently labeled L253P ABD and F-actin. The activity and target of multiple Hit compounds were confirmed in orthologous cosedimentation actin-binding assays. Through future medicinal chemistry, the Hit compounds can potentially be developed into a spinocerebellar ataxia type 5-specific therapeutic. Furthermore, our validated FRET-based in vitro high-throughput screening platform is poised for screening large compound libraries for β-III-spectrin ABD modulators.

01 Feb 2023·Angewandte Chemie International Edition

C3‐Cyanation of Pyridines: Constraints on Electrophiles and Determinants of Regioselectivity

Article

Author: Tang, Zi‐Lu ; Wang, Xiao‐Chen ; Zhou, Qingyang ; Luo, Heng ; Zhang, Ming ; Xu, Xiufang

AbstractMethods for C−H cyanation of pyridines are rare. Here, we report a method for C3‐selective cyanation of pyridines by a tandem process with the reaction of an in situ generated dihydropyridine with a cyano electrophile as the key step. The method is suitable for late‐stage functionalization of pyridine drugs. The low reduction potential of the electrophile and effective transfer of the nitrile group were found to be essential for the success of this method. We studied the reaction mechanism in detail by means of control experiments and theoretical calculations and found that a combination of electronic and steric factors determined the regioselectivity of reactions involving C2‐substituted pyridines.

100 Deals associated with Ibuprofen Piconol

Login to view more data

External Link

KEGG	Wiki	ATC	Drug Bank
D01122	-	M02AA13 R02AX02 M01AE01 G02CC01 C01EB16	-

R&D Status

10 top approved records.

Login

to view more data

Indication	Country/Location	Organization	Date
Acne Vulgaris	Japan	Torii Pharmaceutical Co., Ltd.	13 Feb 1986
Acute eczema	Japan	Torii Pharmaceutical Co., Ltd.	17 Mar 1984
Chronic eczema	Japan	Torii Pharmaceutical Co., Ltd.	17 Mar 1984
Dermatitis, Atopic	Japan	Torii Pharmaceutical Co., Ltd.	17 Mar 1984
Dermatitis, Contact	Japan	Torii Pharmaceutical Co., Ltd.	17 Mar 1984
Dermatitis, Perioral	Japan	Torii Pharmaceutical Co., Ltd.	17 Mar 1984
Herpes Zoster	Japan	Torii Pharmaceutical Co., Ltd.	17 Mar 1984
Rosacea-like dermatitis	Japan	Torii Pharmaceutical Co., Ltd.	17 Mar 1984