Pharmacological characterisation of CR6086, a potent prostaglandin E2 receptor 4 antagonist, as a new potential disease-modifying anti-rheumatic drug.
Gianfranco CaselliAlbino BonazziMarco LanzaFlora FerrariDaniele MaggioniCristian FerioliRoberto GiambelliEleonora ComiSilvia ZerbiMarco PerrellaOrnella LetariElena Di LuccioMilena ColovicStefano PersianiTiziano ZanelliLaura MennuniTiziana PiepoliLucio Claudio RovatiPublished in: Arthritis research & therapy (2018)
CR6086 is a novel, potent EP4 antagonist showing favourable immunomodulatory properties, striking DMARD effects in rodents, and anti-inflammatory activity targeted to immune-mediated inflammatory diseases and distinct from the general effects of cyclooxygenase inhibitors. These results support the clinical development of CR6086, both as a stand-alone DMARD and as a combination therapy with methotrexate. The proof-of-concept trial in patients with RA is ongoing.