Selvigaltin (GB1211) is a highly potent, selective and orally active Galectin-3 inhibitor with binding Kd of 25 nM in FP assays.
GB1211 displays >100-fold selectivity over Galectin-1 as well as low CYP P450 inhibition, also shows no affinity against a panel of 87 different targets (enzymes, receptors, and ion channels).
GB1211 inhibits galectin-3 expression in human monocyte THP1 cells with IC50 of 220.3 nM, inhibits TGFβ stimulated pro-fibrotic gene expression in human liver stellate cell line (LX2) in vitro.
GB1211 (2 mg/kg or 10 mg/kg bid, oral) reduces fibrosis in mouse CCl4-induced liver fibrosis model.
GB1211 is currently in clinical development as a novel, orally active therapy for liver fibrosis.
