Delving into the Latest Updates on Oxaprozin with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Oxaproxin, Oxaprozin (JP17/USP/INN)

+ [12]

Target

COX

Mechanism

COX inhibitors(Cyclooxygenases inhibitors)

Therapeutic Areas

Immune System DiseasesInfectious DiseasesNervous System Diseases+ [4]

Active Indication

Ankylosing SpondylitisCervicobrachial syndromePain+ [9]

Inactive Indication-

Originator Organization

Pfizer Inc.

Active Organization

Pfizer Inc.

Sunflower Pharmaceutical Group Co., Ltd.

Taisho Pharmaceutical Co., Ltd.

+ [1]

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

JP (22 Aug 1985),

BursitisGoutLow Back Pain+ [3]

Regulation-

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Structure

Molecular FormulaC18H15NO3

InChIKeyOFPXSFXSNFPTHF-UHFFFAOYSA-N

CAS Registry21256-18-8

This is an open-label, 2-period add-on study to assess the drug-drug interaction between FYU-981 and oxaprozin. The purpose of this study is to investigate the pharmacokinetics of each period in a single administration of FYU-981 and concomitant administration of FYU-981 with oxaprozin at steady -state in healthy volunteers.

Start Date02 Nov 2017

Sponsor / Collaborator

Mochida Pharmaceutical Co., Ltd.

[+1]

CTR20131751 / Completed

奥沙普秦肠溶胶囊人体生物等效性试验

[Translation] Bioequivalence study of oxaprozin enteric-coated capsules in humans

对22名健康男性自愿受试者按随机交叉自身对照的方法，口服西安大唐制药集团有限公司研制的奥沙普秦肠溶胶囊与湖北百科亨迪药业有限公司生产的奥沙普秦肠溶胶囊，通过对两种制剂口服后的血药浓度测定，计算药动学参数，并进行吸收速度与吸收程度的比较，评价两种制剂的生物等效性，为生产与临床合理使用本品提供参考。

[Translation]

A total of 22 healthy male volunteers were randomly cross-controlled and orally administered oxaprozin enteric-coated capsules developed by Xi'an Datang Pharmaceutical Group Co., Ltd. and oxaprozin enteric-coated capsules produced by Hubei Baike Hendi Pharmaceutical Co., Ltd. The blood drug concentrations of the two preparations after oral administration were measured, the pharmacokinetic parameters were calculated, and the absorption rate and absorption extent were compared to evaluate the bioequivalence of the two preparations, so as to provide a reference for the production and rational clinical use of this product.

Start Date05 Jun 2014

Sponsor / Collaborator

Xi'an Datang Pharmaceutical Group Co., Ltd.

100 Clinical Results associated with Oxaprozin

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100 Translational Medicine associated with Oxaprozin

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100 Patents (Medical) associated with Oxaprozin

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175

Literatures (Medical) associated with Oxaprozin

08 Aug 2024·Journal of Medicinal Chemistry

Structural Optimization of Oxaprozin for Selective Inverse Nurr1 Agonism

Article

Author: Ballarotto, Marco ; Arifi, Silvia ; Zaienne, Daniel ; Ohrndorf, Julia ; Rüger, Lorena A ; Pabel, Jörg ; Proschak, Ewgenij ; Kasch, Till ; López-García, Úrsula ; Willems, Sabine ; Lillich, Felix F ; Renelt, Beatrice ; Busch, Romy ; Marschner, Julian A ; Nawa, Felix ; Merk, Daniel

Nuclear receptor related 1 (Nurr1, NR4A2) is a ligand-sensing transcription factor with neuroprotective and anti-inflammatory roles widely distributed in the CNS. Pharmacological Nurr1 modulation is considered a promising experimental strategy in Parkinson's and Alzheimer's disease but target validation is incomplete. While significant progress has been made in Nurr1 agonist development, inverse agonists blocking the receptor's constitutive activity are lacking. Here we report comprehensive structure-activity relationship elucidation of oxaprozin which acts as moderately potent and nonselective inverse Nurr1 agonist and RXR agonist. We identified structural determinants selectively driving RXR agonism or inverse Nurr1 agonism of the scaffold enabling the development of selective inverse Nurr1 agonists with enhanced potency and strong efficacy.

14 Jun 2024·Organic Letters

Construction of 5-Amino-1,2-Selenazole Scaffolds through N-Selenocyanation/Cyclization of Enaminones Using KSeCN

Article

Author: Huang, Yi ; Tang, Qilin ; Zhang, Hongbin ; Huang, Xuankun ; Yang, Jing ; Guo, Jianhua ; Shen, Yiwen ; Shang, Na ; Yuan, Caifeng ; Tang, E

A metal-free and mild approach for constructing 5-amino-1,2-selenazole skeletons by NBS/KSeCN-mediated N-selenocyanation and nucleophilic cyclization of β-enaminones has been developed. Various isoselenazole compounds and the isoselenazolyl derivatives of anti-inflammatory medicines, including isosepac, oxaprozin, and ibuprofen, have been obtained with good yields. This efficient, "one-pot", and atomic economy strategy may represent an alternative route for the construction of a 1,2-selenazole framework via the "⁺SeCN" pathway and provide new access to heterocycles containing a Se-N bond.

01 Jun 2024·Liver International

Drug‐induced liver injury (DILI) ascribed to non‐steroidal anti‐inflammatory drugs (NSAIDs) in the USA—Update with genetic correlations

Article

Author: Nicoletti, Paola ; Bonkovsky, Herbert L ; Phillips, Elizabeth J ; Gu, Jiezhun ; Kleiner, David E ; Aithal, Guruprasad P ; Fontana, Robert J ; Barnhart, Huiman ; Ghabril, Marwan ; Dellinger, Andrew ; Daly, Ann K

AbstractObjectiveTo describe patients with NSAID‐DILI, including genetic factors associated with idiosyncratic DILI.MethodsIn DILIN, subjects with presumed DILI are enrolled and followed for at least 6 months. Causality is adjudicated by a Delphic approach. HLA sequencing of multiethnic NSAID‐DILI patients and HLA allele imputation of matching population controls were performed following overall, class and drug‐based association analysis. Significant results were tested in a non‐Hispanic White (NHW) case–control replication cohort.ResultsBetween September 2004 and March 2022, causality was adjudicated in 2498, and 55 (41 [75%] women) were assessed as likely due to NSAIDs. Median age at onset was 55 y (range 22–83 y). Diclofenac was the causative drug in 29, celecoxib in 7, ibuprofen in 5, etodolac and meloxicam each in 4. Except for meloxicam and oxaprozin (n = 2), the liver injury was hepatocellular with median R 15–25. HLA‐DRB1*04:03 and HLA‐B*35:03 were significantly more frequent in NSAID‐DILI patients than in non‐NSAID DILI controls. Interestingly, 85% of the HLA‐DRB1*04:03 carriers developed DILI due to the use of acetic acid derivative NSAIDs, supporting the hypothesis that HLA‐DRB1*04:03 could be a drug and/or class risk factor. HLA‐B*35:03 but not HLA‐DRB1*04:03 association was confirmed in the independent NHW replication cohort, which was largely driven by diclofenac.ConclusionsDespite prevalent use, NSAID‐DILI is infrequent in the United States. Diclofenac is the most commonly implicated, and adherence to warnings of risk and close observation are recommended. The increased frequency of HLA‐B*35:03 and DRB1*04:03, driven by diclofenac, suggests the importance of immune‐mediated responses.

100 Deals associated with Oxaprozin

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External Link

KEGG	Wiki	ATC	Drug Bank
D00463	Oxaprozin	M01AE12	DB00991

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Ankylosing Spondylitis	CN	Sunflower Pharmaceutical Group Co., Ltd.	01 Jan 1995
Cervicobrachial syndrome	CN	Sunflower Pharmaceutical Group Co., Ltd.	01 Jan 1995
Pain	CN	Sunflower Pharmaceutical Group Co., Ltd.	01 Jan 1995
Periarthritis	CN	Sunflower Pharmaceutical Group Co., Ltd.	01 Jan 1995
Post procedural inflammation	CN	Sunflower Pharmaceutical Group Co., Ltd.	01 Jan 1995
Juvenile Idiopathic Arthritis	US	Pfizer Inc.	29 Oct 1992
Bursitis	JP	Taisho Pharmaceutical Co., Ltd.	22 Aug 1985
Gout	JP	Taisho Pharmaceutical Co., Ltd.	22 Aug 1985
Low Back Pain	JP	Taisho Pharmaceutical Co., Ltd.	22 Aug 1985
Osteoarthritis	JP	Taisho Pharmaceutical Co., Ltd.	22 Aug 1985
Pain, Postoperative	JP	Taisho Pharmaceutical Co., Ltd.	22 Aug 1985
Rheumatoid Arthritis	JP	Taisho Pharmaceutical Co., Ltd.	22 Aug 1985