托芬那酸(Tolfenamic Acid) - 药物靶点：COX_在研适应症：关节炎，痛经，偏头痛_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Tolfenamic acid (JAN/INN)、NTX 010、NTX-010

+ [3]

靶点

COX

作用机制

COX抑制剂(环氧化酶抑制剂)

治疗领域

神经系统疾病皮肤和肌肉骨骼疾病内分泌与代谢疾病+ [1]

在研适应症

非在研适应症

原研机构

在研机构

NeuroTau, Inc.初创企业

非在研机构-

最高研发阶段批准上市

首次获批日期

中国 (2005-07-13),

关节炎痛经偏头痛

最高研发阶段(中国)批准上市

特殊审评-

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结构

分子式C14H12ClNO2

InChIKeyYEZNLOUZAIOMLT-UHFFFAOYSA-N

CAS号13710-19-5

关联

2

项与托芬那酸相关的临床试验

NCT04253132 / Unknown status临床1/2期

A Phase 2a Randomized, Double-blind, Placebo-controlled Study to Evaluate the Safety and Efficacy of Tolfenamic Acid for the Treatment of Progressive Supranuclear Palsy

This is a 12-week study of oral tolfenamic acid vs. placebo in Progressive Supranuclear Palsy (PSP)

开始日期2021-01-01

申办/合作机构

NeuroTau, Inc.初创企业

[+1]

NCT02159248 / Withdrawn临床1期IIT

09.017 - A Phase I Study of Tolfenamic Acid With Gemcitabine and Radiation in Patients With Locally Advanced or Metastatic Pancreatic Cancer Requiring Definitive or Palliative Radiation Therapy

The purposes of this study are to:
Evaluate the safety and toxicity of tolfenamic acid when used with gemcitabine and radiation therapy in patients with locally advanced or metastatic pancreatic cancer.
Determine the maximum-tolerated dose (MTD) of tolfenamic acid when used with gemcitabine and radiation in pancreatic cancer.
Characterize the pharmacokinetic profile of tolfenamic acid when used with gemcitabine and radiation.
Assess the anti-tumor response to tolfenamic acid when used with gemcitabine and radiation in patients with advanced pancreatic malignancies.

开始日期2014-03-01

申办/合作机构

Orlando Health, Inc.

100 项与托芬那酸相关的临床结果

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100 项与托芬那酸相关的转化医学

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100 项与托芬那酸相关的专利（医药）

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410

项与托芬那酸相关的文献（医药）

2023-12-01·Biochimica et biophysica acta. Molecular cell research

Tolfenamic acid negatively regulates YAP and TAZ expression in human cancer cells

Article

作者: Lertpatipanpong, Pattawika ; Hong, Yukyung ; Kim, Ilju ; Yoon, Yongdae ; Lee, Jaehak ; Ryu, Junsun ; Baek, Seung Joon ; Boonruang, Kanokkan

Several diseases are associated with improper regulation of the Hippo pathway, which plays an important role in cell proliferation and cancer metastasis. Overactivation of the YAP and TAZ proteins accelerates cell proliferation, invasion, and migration during tumorigenesis. Tolfenamic acid (TA) is a non-steroidal anti-inflammatory drug (NSAID) that exhibits activity against various types of cancer. In this study, we observed that TA decreased YAP and TAZ protein levels in cancer cells. TA increased the phosphorylation of YAP and TAZ, leading to the degradation of YAP and TAZ in the cytoplasm and nucleus. TA predominantly affected multiple phosphodegron sites in the YAP and TAZ and lowered 14-3-3β protein expression, causing YAP and TAZ to enter the ubiquitination pathway. Proteins that affect YAP and TAZ regulation, such as NAG-1 and several YAP/TAZ E3 ligases, were not involved in TA-mediated YAP/TAZ degradation. In summary, our results indicate that TA affects phosphodegron sites on YAP/TAZ, demonstrating a novel effect of TA in tumorigenesis.

2023-08-01·Animal bioscience

Administration of ketoprofen in postpartum sows to control the incidence of post-parturient disorders and improve piglet survival rate.

Article

作者: Suwimonteerabutr, Junpen ; Theerakulpisut, Thanabat ; Taechamaeteekul, Preechaphon ; Tummaruk, Padet ; Jeeraphokhakul, Suwicha ; Khampoomee, Pitchapa ; Chaiwangna, Jakkrit ; Dumniem, Natchanon

OBJECTIVE:

Inflammation and pain management in postpartum hyperprolific sows is currently an important animal welfare issue in the swine industry. The present study investigates effects of ketoprofen treatment on the incidence of post-parturient disorders, feed intake, colostrum yield, piglet colostrum intake, colostrum immunoglobulin G (IgG) and piglet mortality rate during the first 3 days of postnatal life.

METHODS:

In total, 61 Danish Landrace×Yorkshire crossbred sows and their offspring (n = 833) were included in the experiment. The sows were randomly distributed into two groups: i) control (n = 31), sows were treated with tolfenamic acid 2 mg per kg for 2 days postpartum; ii) ketoprofen (n = 30), sows were treated with ketoprofen 3 mg per kg for 2 days postpartum. The farrowing process of the sows was monitored for 24 h daily, and data associated with farrowing were collected. Piglet colostrum intake, sow colostrum yield and colostrum IgG were determined.

RESULTS:

During the first 3 days postpartum, the incidence of sows that had fever did not differ between control and ketoprofen groups (51.6% and 56.7%, respectively, p = 0.692). Piglet colostrum intake did not differ between control and ketoprofen groups (p = 0.736). However, the proportions of piglets that had inadequate colostrum intake were 71.3%, 22.6%, and 5.4% in those with birth weights of <1.0 kg, 1.0 to 1.29 kg, and ≥1.30 kg, respectively (p<0.001). The piglet mortality rate did not differ between control and ketoprofen groups (p = 0.808).

CONCLUSION:

Administration of ketoprofen in postpartum sows for 2 days can control the evidence of post-parturient disorders in sows as effectively as the use of tolfenamic acid. No deleterious effect of ketoprofen was detected on sow colostrum yield, piglet colostrum intake and piglet mortality. Therefore, ketoprofen can be recommended as an alternative anti-inflammatory drug used in postpartum sows.

2023-08-01·Materials today. Bio

Self-assembly nanoplatform of platinum (Ⅳ) prodrug for enhanced ovarian cancer therapy

Article

作者: Liu, Yangjia ; Tan, Jinxiu ; Ma, Xiao ; Wang, Zhenjie ; Yi, Wenying ; Yu, Zhiqiang ; Wang, Xuefeng ; Wu, Hanmei

Cisplatin is a metal platinum complex commonly used in the field of anti-tumor and one of the most commonly used drugs in combination chemotherapy. However, chemotherapy with Cisplatin induced overexpression of cyclooxygenase-2 (COX-2) protein in tumor cells, which could impair the therapeutic effect of chemotherapy on tumor progression. Here, we presented a novel method for the treatment of ovarian cancer with a self-assembly based nano-system. Cisplatin and tolfenamic acid were each linked to linoleic acid to give them the ability to self-assemble into nanoparticles in water. TPNPs had flexible drug ratio adjustability, homogeneous stability, and high drug loading capacity. Compared with Cisplatin, TPNPs could promote cellular uptake and tumor aggregation, co-induce enhanced apoptosis and tumor growth inhibition by inhibiting COX-2 in the mice xenograft model of human ovarian cancer, and reduce systemic toxicity. Therefore, TPNPs is a promising antitumor drug as a kind of self-assembly nano-prodrug with high drug load.

100 项与托芬那酸相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D01183	托芬那酸	M01AG02	DB09216

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
关节炎	中国	杭州民生药业股份有限公司	2005-07-13
痛经	中国	杭州民生药业股份有限公司	2005-07-13
偏头痛	中国	杭州民生药业股份有限公司	2005-07-13

未上市

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适应症	最高研发状态	国家/地区	公司	日期
进行性核上性麻痹	临床2期	美国	NeuroTau, Inc.初创企业	2021-01-01
额颞痴呆	临床2期	-	NeuroTau, Inc.初创企业	-

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临床结果

适应症

分期

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


AACR2010	临床1期	卵巢癌	-	Tolfenamic Acid	醖艱蓋蓋鬱觸積糧衊齋(鬱鹹構壓顧築鹽艱齋鑰) = 壓鑰選鹽製網膚網願夢鹹選醖願鹽繭構獵鹽製 (選積觸鬱簾獵醖膚選蓋 )	-	2010-04-15