Delving into the Latest Updates on QAV-680 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

NVPQAV-680, QAV 680, QAV680

Target

CRTH2

Action

antagonists

Mechanism

CRTH2 antagonists(Prostaglandin D2 receptor 2 antagonists)

Therapeutic Areas

Immune System DiseasesInfectious DiseasesOtorhinolaryngologic Diseases+ [1]

Active Indication-

Inactive Indication

Persistent asthmaRhinitis, Allergic, Seasonal

Originator Organization

Novartis Pharma AG

Active Organization-

Inactive Organization

Novartis Pharmaceuticals Canada, Inc.

Novartis AG

License Organization-

Drug Highest PhaseDiscontinuedPhase 2

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC18H18N2O4S

InChIKeyYOPFAMROKXHVCQ-UHFFFAOYSA-N

CAS Registry872365-16-7

This study will determine the capacity of more frequent dosing of QAV680 to suppress allergic inflammation. The study will investigate the paradigm of multiple receptor antagonism in allergic disease by combining QAV680 with a second generation H1 histamine receptor antagonist to assess possible additive or synergistic anti-allergic effects of the two compound classes.

Start Date22 Mar 2010

Sponsor / Collaborator

Novartis Pharmaceuticals Corp.

NCT01103037

/ TerminatedPhase 2

A Randomized, Double-blind, Parallel Group Study to Compare the Pharmacodynamics/Efficacy, Safety and Pharmacokinetics of QAV680 Versus Placebo in Patients With Moderate Persistent Asthma

This study will assess the safety and efficacy of QAV680 in patients with mild to moderate asthma

Start Date01 Mar 2010

Sponsor / Collaborator

Novartis Pharmaceuticals Canada, Inc.

NCT00814216

/ CompletedPhase 2

Randomized, Double-blind, Two Way Cross-over, Proof of Concept Study to Compare Efficacy, Safety, Pharmacokinetics & Pharmacodynamics of QAV680 Versus Placebo, With an Extended Open-label Corticosteroid Period, in Steroid-free, Mild to Moderate Persistent Asthma Patients.

This study aims to study the efficacy (as measured by change in FEV1) and safety of two-week administration of oral QAV680 in the treatment of patients with asthma.'

Start Date01 Dec 2008

Sponsor / Collaborator

Novartis AG

100 Clinical Results associated with QAV-680

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100 Translational Medicine associated with QAV-680

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100 Patents (Medical) associated with QAV-680

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3

Literatures (Medical) associated with QAV-680

11 May 2017·ACS medicinal chemistry lettersQ3 · MEDICINE

Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP₂ Receptor Antagonist for Treatment of Asthma

Q3 · MEDICINE

Article

Author: Brown, Lyndon ; Riddy, Darren ; West, Ryan ; Duggan, Nicholas ; Williams, Gareth ; Stringer, Rowan ; Hatto, Julia ; Willis, Jennifer ; Willard, Elisabeth ; Ritchie, Catherine ; Charlton, Steven J. ; Shaw, Duncan ; Thomas, Matthew ; Budd, David ; Turner, Katharine L. ; Sohal, Bindi ; Sandham, David A. ; Barker, Lucy ; Chatterjee, Devnandan ; Dubois, Gerald ; Manini, Jodie ; Profit, Rachael ; Cox, Brian ; Watson, Simon J. ; Hall, Edward ; Maas, Janet ; Sykes, David A. ; Brown, Zarin

Further optimization of an initial DP₂ receptor antagonist clinical candidate NVP-QAV680 led to the discovery of a follow-up molecule 2-(2-methyl-1-(4-(methylsulfonyl)-2-(trifluoromethyl)benzyl)-1H-pyrrolo[2,3-b]pyridin-3-yl)acetic acid (compound 11, NVP-QAW039, fevipiprant), which exhibits improved potency on human eosinophils and Th2 cells, together with a longer receptor residence time, and is currently in clinical trials for severe asthma.

01 Mar 2014·JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS

Synthetic approaches to site selective deuterium incorporation in a novel CRTh2 receptor antagonist clinical candidate

Article

Author: Sandham, David A. ; Page, Christopher J.

Selection of acidic or basic reaction conditions, combined with appropriate temperatures, allowed for site selective direct incorporation of deuterium at multiple positions in the 7-azaindole-3-acetic acid CRTh2 receptor antagonist clinical candidate NVP-QAV680.

01 Nov 2013·Bioorganic & medicinal chemistryQ3 · MEDICINE

Discovery and characterization of NVP-QAV680, a potent and selective CRTh2 receptor antagonist suitable for clinical testing in allergic diseases

Q3 · MEDICINE

Article

Author: David Budd ; Josef Meingassner ; Lucy Barker ; Karen England ; John Westwick ; Simon J. Watson ; Heinrich Aschauer ; Zarin Brown ; Alfred Schmidt ; Frank Kalthoff ; Caroline Wilson ; Matthew Thomas ; Cerys Docx ; Lyndon Brown ; Brian Cox ; Bindi Sohal ; Jodie Manini ; Rowan Stringer ; Anna King ; Jennifer Simmons ; Christoph Walker ; Gerald Dubois ; Kamlesh Bala ; Catherine J. Leblanc ; David A. Sandham ; Brian Everatt ; Nicholas Duggan ; Edward Hall ; Marcus Furegati ; Jennifer Willis ; Katharine L. Turner ; Nicola Arnold ; Gareth Williams ; Rachael Profit

Optimization of a 7-azaindole-3-acetic acid CRTh2 receptor antagonist chemotype derived from high throughput screening furnished a highly selective compound NVP-QAV680 with low nM functional potency for inhibition of CRTh2 driven human eosinophil and Th2 lymphocyte activation in vitro. The molecule exhibited good oral bioavailability in the rat, combined with efficacy in rodent CRTh2-dependent mechanistic and allergic disease models and was suitable for clinical development.

100 Deals associated with QAV-680

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