QAW039, a slowly dissociating CRTh2 antagonist with potential for improved clinical efficacy

David A. Sykes; Michelle E. Bradley; Darren Riddy; Elizabeth Willard; Ellen Powell-Herlaar; Simon J. Watson; Carsten Bauer; David A. Sandham; Gerald Dubois; Steven J Charlton

QAW039, a slowly dissociating CRTh2 antagonist with potential for improved clinical efficacy

David A. Sykes, Michelle E. Bradley, Darren Riddy, Elizabeth Willard, Ellen Powell-Herlaar, Simon J. Watson, Carsten Bauer, David A. Sandham, Gerald Dubois, Steven J Charlton

Research output: Contribution to conference › Poster

Abstract

PGD2 is the major prostanoid released by activated mast cells and is an important proinflammatory mediator in allergic asthma acting through the CRTh2 receptor. QAW039 is an oral, selective, competitive and reversible CRTh2 antagonist currently in clinical development for treatment of asthma. This study describes the detailed investigation of the receptor binding kinetics of QAW039 and compares it to several other known CRTh2 antagonists.

Original language	English
Number of pages	2
Publication status	Published - 2014
Externally published	Yes
Event	Pharmacology 2014 - Queen Elizabeth II Conference Centre, London, United Kingdom Duration: 1 Dec 2014 → …

Conference

Conference	Pharmacology 2014
Country/Territory	United Kingdom
City	London
Period	1/12/14 → …

Access to Document

284505551-oaFinal published version, 273 KB

http://www.pa2online.org/abstract/abstract.jsp?abid=32580&author=riddy&cat=-1&period=-1

Cite this

Sykes, D. A., Bradley, M. E., Riddy, D., Willard, E., Powell-Herlaar, E., Watson, S. J., Bauer, C., Sandham, D. A., Dubois, G., & Charlton, S. J. (2014). QAW039, a slowly dissociating CRTh2 antagonist with potential for improved clinical efficacy. Poster session presented at Pharmacology 2014, London, United Kingdom. http://www.pa2online.org/abstract/abstract.jsp?abid=32580&author=riddy&cat=-1&period=-1

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title = "QAW039, a slowly dissociating CRTh2 antagonist with potential for improved clinical efficacy",

abstract = "PGD2 is the major prostanoid released by activated mast cells and is an important proinflammatory mediator in allergic asthma acting through the CRTh2 receptor. QAW039 is an oral, selective, competitive and reversible CRTh2 antagonist currently in clinical development for treatment of asthma. This study describes the detailed investigation of the receptor binding kinetics of QAW039 and compares it to several other known CRTh2 antagonists.",

author = "Sykes, {David A.} and Bradley, {Michelle E.} and Darren Riddy and Elizabeth Willard and Ellen Powell-Herlaar and Watson, {Simon J.} and Carsten Bauer and Sandham, {David A.} and Gerald Dubois and Charlton, {Steven J}",

year = "2014",

language = "English",

note = "Pharmacology 2014 ; Conference date: 01-12-2014",

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T1 - QAW039, a slowly dissociating CRTh2 antagonist with potential for improved clinical efficacy

AU - Sykes, David A.

AU - Bradley, Michelle E.

AU - Riddy, Darren

AU - Willard, Elizabeth

AU - Powell-Herlaar, Ellen

AU - Watson, Simon J.

AU - Bauer, Carsten

AU - Sandham, David A.

AU - Dubois, Gerald

AU - Charlton, Steven J

PY - 2014

Y1 - 2014

N2 - PGD2 is the major prostanoid released by activated mast cells and is an important proinflammatory mediator in allergic asthma acting through the CRTh2 receptor. QAW039 is an oral, selective, competitive and reversible CRTh2 antagonist currently in clinical development for treatment of asthma. This study describes the detailed investigation of the receptor binding kinetics of QAW039 and compares it to several other known CRTh2 antagonists.

AB - PGD2 is the major prostanoid released by activated mast cells and is an important proinflammatory mediator in allergic asthma acting through the CRTh2 receptor. QAW039 is an oral, selective, competitive and reversible CRTh2 antagonist currently in clinical development for treatment of asthma. This study describes the detailed investigation of the receptor binding kinetics of QAW039 and compares it to several other known CRTh2 antagonists.

M3 - Poster

T2 - Pharmacology 2014

Y2 - 1 December 2014

ER -