Discovery of fevipiprant (NVP-QAW039), a potent and selective DP2 receptor antagonist for treatment of asthma

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

doi:10.1021/acsmedchemlett.7b00157

All Outputs (2)

Extrapyramidal side effects of antipsychotics are linked to their association kinetics at dopamine D2 receptors (2017)
Journal Article
Sykes, D. A., Moore, H., Stott, L., Holliday, N., Javitch, J. A., Lane, J. R., & Charlton, S. J. (2017). Extrapyramidal side effects of antipsychotics are linked to their association kinetics at dopamine D2 receptors. Nature Communications, 8(1), Article 763. https://doi.org/10.1038/s41467-017-00716-z

Atypical antipsychotic drugs (APDs) have been hypothesized to show reduced extrapyramidal side effects (EPS) due to their rapid dissociation from the dopamine D2 receptor. However, support for this hypothesis is limited to a relatively small number o... Read More about Extrapyramidal side effects of antipsychotics are linked to their association kinetics at dopamine D2 receptors.

Discovery of fevipiprant (NVP-QAW039), a potent and selective DP2 receptor antagonist for treatment of asthma (2017)
Journal Article
Sandham, D. A., Barker, L., Brown, L., Brown, Z., Budd, D., Charlton, S. J., …Willis, J. (2017). Discovery of fevipiprant (NVP-QAW039), a potent and selective DP2 receptor antagonist for treatment of asthma. ACS Medicinal Chemistry Letters, 8(5), 582-586. https://doi.org/10.1021/acsmedchemlett.7b00157

Further optimization of an initial DP2 receptor antagonist clinical candidate NVPQAV680 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,... Read More about Discovery of fevipiprant (NVP-QAW039), a potent and selective DP2 receptor antagonist for treatment of asthma.