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CAS No.: 872365-14-5

Fevipiprant Catalog No. CSN18830

Synonyms: QAW039;NVP-QAW039;NVP-QAW-039 QAW-039

Fevipiprant is a selective, potent, reversible competitive CRTh2 antagonist with an in vitro dissociation constant KD value of 1.1nM at the CRTh2 receptor and an IC50 value of 0.44 nM for inhibition of PGD2-induced eosinophil shape change in human whole blood.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Fevipiprant is a potent and selective CRTh2 (DP2) receptor antagonist with Ki value of 4nM in a human DP₂ receptor scintillation proximity binding assay, and IC50 values of 0.4nM for in both isolated human eosinophil shape change assay and human whole blood eosinophil shape change assay. Fevipiprant dose-dependently antagonize PGD2-stimulated [³⁵S]-GTPγS activation at human CRTh2 receptors expressed in membranes from CHO cells. It inhibited DK-PGD₂ induced cytokine production, including IL-4, IL-5 and IL-13, with IC50 values of 3.1nM, 2.6nM and 1.4nM in human CD₄₊ Th2 cells.
作用机制Fevipiprant could bind to CRTh2 receptor through competition with the native agonist PGD2.^[2]

动物研究

剂量

Rat: 0.03 mg/kg - 0.1 mg/kg^[1] (p.o.)

给药途径

p.o.

动物药代数据

Animal	Rats^[1]
Dose	0.5 mg/kg (i.v.) 3 mg/kg (p.o.)
Administration	i.v. p.o.
F	43% (p.o.)
T_1/2	13.2 h (i.v.)
CL	1.6 ml/min/kg (i.v.)
Vss	1.1 L/kg (i.v.)

临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01804400	Allergic Rhinitis	Phase 2	Completed	-	Germany ... more >> Novartis Investigative Site Hannover, Germany, 30625 Collapse <<
NCT01836471	Asthma	Phase 2	Completed	-	-
NCT01253603	Persistent Asthma	Phase 2	Completed	-	-

更多
参考文献

[1] Sandham DA, Barker L, et al. Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP2 Receptor Antagonist for Treatment of Asthma. ACS Med Chem Lett. 2017 Apr 25;8(5):582-586.
[2] Sykes DA, Bradley ME, et al. Fevipiprant (QAW039), a Slowly Dissociating CRTh2 Antagonist with the Potential for Improved Clinical Efficacy. Mol Pharmacol. 2016 May;89(5):593-605.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3452 mL
- 11.7258 mL
- 23.4516 mL
- 5 mM
- 0.4690 mL
- 2.3452 mL
- 4.6903 mL
- 10 mM
- 0.2345 mL
- 1.1726 mL
- 2.3452 mL

技术信息

CAS号

872365-14-5

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H17F3N2O4S

运输

蓝冰

分子量

426.41

别名

QAW039;NVP-QAW039;NVP-QAW-039 QAW-039

溶解度

DMSO	50.0 mg/mL (117.3 mM)

动物实验配方

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT01804400	Allergic Rhinitis	Phase 2	Completed	-	Germany ... more >> Novartis Investigative Site Hannover, Germany, 30625 Collapse <<
NCT01836471	Asthma	Phase 2	Completed	-	-
NCT01253603	Persistent Asthma	Phase 2	Completed	-	-
NCT01836471	-	-	Completed	-	-
NCT01785602	-	-	Completed	-	-
NCT01437735	Asthma	Phase 2	Completed	-	-
NCT01545726	Asthma	Phase 2	Completed	-	United Kingdom ... more >> Novartis Investigative Site Leicester, United Kingdom, LE3 9QP Collapse <<
NCT02555683	Asthma	Phase 3	Recruiting	December 20, 2019	-
NCT02563067	Asthma	Phase 3	Active, not recruiting	September 19, 2019	-
NCT03665701	Atopic Asthma	Not Applicable	Enrolling by invitation	December 31, 2018	Germany ... more >> Fraunhofer ITEM im CRC Hannover, Niedersachsen, Germany, 30625 Collapse <<
NCT03215758	Asthma	Phase 3	Recruiting	November 20, 2019	-
NCT03087942	Renal Insufficiency	Phase 1	Completed	-	United States, Florida ... more >> Novartis Investigative Site Orlando, Florida, United States, 32809 Germany Novartis Investigative Site Grunstadt, Germany, 67269 Collapse <<
NCT03629249	Asthma Bronch... more >>ial Diseases Respiratory Tract Diseases Lung Diseases, Obstructive Lung Diseases Respiratory Hypersensitivity Hypersensitivity, Immediate Hypersensitivity Immune System Diseases Physiological Effects of Drugs Collapse <<	Phase 4	Not yet recruiting	May 27, 2021	-
NCT01785602	Atopic Dermatitis	Phase 2	Completed	-	Australia, Australian Capital ... more >>Territory Novartis Investigative Site Phillip, Australian Capital Territory, Australia, 2606 Australia, Queensland Novartis Investigative Site Benowa, Queensland, Australia, 4217 Novartis Investigative Site Woolloongabba, Queensland, Australia, 4102 Austria Novartis Investigative Site Vienna, Austria Belgium Novartis Investigative Site Bruxelles, Belgium, 1200 Novartis Investigative Site Leuven, Belgium, 3000 Novartis Investigative Site Liège, Belgium, 4000 Bulgaria Novartis Investigative Site Sofia, Bulgaria, 1612 Germany Novartis Investigative Site Berlin, Germany, 10098 Novartis Investigative Site Berlin, Germany, 10117 Novartis Investigative Site Bonn, Germany, 53105 Novartis Investigative Site Dresden, Germany, 01307 Novartis Investigative Site Muenster, Germany, 48149 Netherlands Novartis Investigative Site Amsterdam, Netherlands, 1105 AZ Novartis Investigative Site Groningen, Netherlands Novartis Investigative Site Utrecht, Netherlands, 3508 GA Romania Novartis Investigative Site Bucharest, Romania, 011461 South Africa Novartis Investigative Site Durban, South Africa, 4001 Collapse <<
NCT03681093	Asthma Nasal ... more >>Polyps Bronchial Diseases Lung Diseases Nose Diseases Respiratory Hypersensitivity Hypersensitivity Collapse <<	Phase 3	Not yet recruiting	July 6, 2020	-
NCT03226392	Asthma	Phase 3	Recruiting	November 20, 2019	-
NCT03650400	Asthma	Phase 2	Not yet recruiting	January 28, 2020	-
NCT03048448	Hepatic Impairment	Phase 1	Recruiting	August 30, 2018	United States, California ... more >> Novartis Investigative Site Recruiting Anaheim, California, United States, 92801 United States, Florida Novartis Investigative Site Recruiting Orlando, Florida, United States, 32809 Collapse <<
NCT03052517	Asthma	Phase 3	Recruiting	November 18, 2022	-

Fevipiprant Catalog No. CSN18830

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