BMS-986020

BMS-986020 (BMS986020, AM-152) is a potent, selective, orally available LPA1 receptor antagonist for treating idiopathic pulmonary fibrosis.Cystic Fibrosis, Phase 2 Clinical (In Vitro) :BMS-986020 (0.1-10 nM; pre-incubated) concentration-dependent displacement of [18F]BMT-083133 binding is observed in LPA1+ cells and lung sections. At 0.1 nM, the percent displacement in healthy mice, bleomycin mice, and IPF lungs is 18%, 24%, and 31%, respectively. At 10 nM, the percent displacement is 73%, 76%, and 64%, respectively.BMT-083133, a radioligand targeting LPA1 is developed as a translational research tool for assessment of lung LPA1 engagement of BMS-986020 using in vitro autoradiography (ARG) .