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)

+ [4]

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

特殊审评孤儿药 (欧盟)

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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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421

项与托芬那酸相关的文献（医药）

2024-11-01·Veterinary Medicine and Science

Plasma and Milk Pharmacokinetics and Estimated Milk Withdrawal Time of Tolfenamic Acid in Lactating Sheep

Article

作者: Elmas, Muammer ; Cetin, Gul ; Uney, Kamil ; Coskun, Devran ; Corum, Orhan ; Durna Corum, Duygu

ABSTRACTObjectiveThis study aimed to investigate the plasma and milk pharmacokinetics, as well as the withdrawal time (WT) from milk of tolfenamic acid (2 and 4 mg/kg) following intravenous (IV) administration to eight healthy lactating Akkaraman sheep.MethodsThe trial was conducted in two periods in accordance with a crossover pharmacokinetic design. The concentrations of tolfenamic acid in the plasma and milk were determined using high‐pressure liquid chromatography and evaluated using non‐compartmental analysis. The WT of tolfenamic acid in milk was calculated using the WT 1.4 software.ResultsCompared to the 2 mg/kg dose, plasma volume of distribution at steady state (from 0.43 to 0.50 L/kg), terminal elimination half‐life (from 2.41 to 4.14 h) and dose‐normalized area under the plasma concentration–time curve (AUC0−∞, from 9.46 to 30.11 h µg/mL) increased, whereas total body clearance (from 0.21 to 0.13 L/h/kg) decreased at the 4 mg/kg dose. The peak milk concentration (Cmax) and AUC0−∞ values in milk were 0.26 µg/mL and 0.28 h µg/mL, respectively, for 2 mg/kg, and 0.43 µg/mL and 0.55 h µg/mL, respectively, for 4 mg/kg. Although the dose‐normalized Cmax of milk decreased depending on the dose, no difference was observed in dose‐normalized AUC0−∞. The AUC0−∞ milk/AUC0−∞ plasma ratio was 0.03 for 2 mg/kg and 0.02 for 4 mg/kg. The WT values calculated for milk at dosages of 2 and 4 mg/kg were 3 and 4 h, respectively.ConclusionsA decrease in plasma elimination and an increase in plasma concentration of tolfenamic acid were observed depending on the dose. Tolfenamic acid lowly passed into sheep's milk at 2 and 4 mg/kg doses. This study may provide valuable information for clinicians’ decision‐making processes.

2024-07-01·Veterinary Medicine and Science

Pharmacokinetics, bioavailability and plasma protein binding of tolfenamic acid in rainbow trout (Oncorhynchus mykiss)

Article

作者: Uney, Kamil ; Acar, Omer Faruk ; Marin, Pedro ; Corum, Orhan ; Durna Corum, Duygu ; Aksoy, Mert

AbstractBackgroundAlthough research on the mechanism and control of pain and inflammation in fish has increased in recent years, the use of analgesic drugs is limited due to the lack of pharmacological information about analgesic drugs. Tolfenamic acid is a non‐steroidal anti‐inflammatory drug and can be used in fish due to its low side effect profile and superior pharmacokinetic properties.ObjectivesThe pharmacokinetics, bioavailability and plasma protein binding of tolfenamic acid were investigated following single intravascular (IV), intramuscular (IM) and oral administration of 2 mg/kg in rainbow trout at 13 ± 0.5°C.MethodsThe experiment was carried out on a total of 234 rainbow trout (Oncorhynchus mykiss). Tolfenamic acid was administered to fish via IV, IM and oral route at a dose of 2 mg/kg. Blood samples were taken at 13 different sampling times until the 72 h after drug administration. The plasma concentrations of tolfenamic acid were quantified using high pressure liquid chromatography–ultraviolet (UV) and pharmacokinetic parameters were assessed using non‐compartmental analysis.ResultsThe elimination half‐life (t1/2ʎz) of tolfenamic acid for IV, IM and oral routes was 3.47, 6.75 and 9.19 h, respectively. For the IV route, the volume of distribution at a steady state and total body clearance of tolfenamic acid were 0.09 L/kg and 0.03 L/h/kg, respectively. The peak plasma concentration and bioavailability for IM and oral administration were 8.82 and 1.24 µg/mL, and 78.45% and 21.48%, respectively. The mean plasma protein binding ratio of tolfenamic acid in rainbow trout was 99.48% and was not concentration dependent.ConclusionsWhile IM route, which exhibits both the high plasma concentration and bioavailability, can be used in rainbow trout, oral route is not recommended due to low plasma concentration and bioavailability. However, there is a need to demonstrate the pharmacodynamic activity of tolfenamic acid in rainbow trout.

2024-04-08·Biomacromolecules

Irradiation Behavior of Analgesic and Nonsteroidal Anti-Inflammatory Drug-Loaded UHMWPE for Joint Replacement

Article

作者: Inverardi, Nicoletta ; Hugard, Shannon ; Muratoglu, Orhun K. ; Lekkala, Sashank ; Oral, Ebru ; Grindy, Scott C.

Local delivery of pain medication can be a beneficial strategy to address pain management after joint replacement, as it can decrease systemic opioid usage, leading to less side and long-term effects. In this study, we used ultrahigh molecular weight polyethylene (UHMWPE), commonly employed as a bearing material for joint implants, to deliver a wide set of analgesics and the nonsteroidal anti-inflammatory drug tolfenamic acid. We blended the drugs with UHMWPE and processed the blend by compression molding and sterilization by low-dose gamma irradiation. We studied the chemical stability of the eluted drugs, drug elution, tensile properties, and wear resistance of the polymer blends before and after sterilization. The incorporation of bupivacaine hydrochloride and tolfenamic acid in UHMWPE resulted in either single- or dual-drug loaded materials that can be sterilized by gamma irradiation. These compositions were found to be promising for the development of clinically relevant drug-eluting implants for joint replacement.

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

10 条进展最快的记录,

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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	襯窪鹹艱觸壓選鑰鬱廠(醖構願鑰鹹獵繭鑰鬱範) = 積壓襯壓積觸鹽廠選繭繭簾膚蓋選鬱淵醖壓鏇 (醖繭襯築蓋糧齋膚艱製 )	-	2010-04-15