BBT-209

**BBT-209** is a first-in-class small molecule agonist of G protein-coupled receptor 19 (GPCR19, also known as TGR5), originally developed by Shaperon and exclusively licensed by Bridge Biotherapeutics in 2022 for idiopathic pulmonary fibrosis (IPF). It controls GPCR19-P2X7 signaling to downregulate NLRP3 inflammasome component proteins, suppressing inflammatory cytokine networks including IL-1β (EC50 0.031 μM) and TNF-α (EC50 0.36 μM), while inhibiting α-smooth muscle actin (α-SMA) expression and fibrosis in bleomycin-induced mouse models. Nonclinical data demonstrate potent anti-inflammatory (>80%) and antifibrotic effects, positioning it as a novel IPF candidate alongside Bridge's other assets like BBT-301 and BBT-877.[1][2][3][5][7]

Other names

GPCR19 agonistGPCR-19 agonistGPCR 19 agonist