Introduction
inflammation, fibrotic illness, fibrosis
PROLIFERATION, INFLAMMATION, DISEASE, FIBROSIS
Galectin-3 is a β-galactoside-binding lectin, which plays an important role in cell proliferation, differentiation, angiogenesis and apoptosis, and is a key regulator of fibrosis and inflammation in the lungs, liver and kidneys [There is interest surrounding the therapeutic potential for galectin-3 inhibition in fibrotic disease [Galectin-3 inhibition as treatment for fibrotic illness has recently been observed in human studies. GB0139 (also known as TD139), is a potent thiodigalactoside inhibitor of galectin-3 [The small molecule galectin-3 inhibitor, GB1211, has been developed amongst a new class of galactopyranosides, whereby non-natural aromatic substituents are introduced to the 1- and 3-position of α-D-galactopyranosides, and affinity subsequently optimized by specific interactions, such as fluorine-amide, phenyl-arginine, sulphur-π, and halogen bonds [We report the results of a phase 1 trial of GB1211; the first clinical study of GB1211. The aim of this study was to evaluate the safety, tolerability and PK of oral GB1211 in healthy participants.