molecules of the month

Context. GB1211 (Galecto Biotech) is an oral galectin-3 inhibitor under development for fibrotic disease. First described in 1971, galectin-3, a unique subtype of a 15-member family of carbohydrate-binding proteins, has been implicated in a host of different diseases, such as cancer, liver cirrhosis, and atherosclerosis. Incredibly, over 8000 papers featuring the protein have since been published. Despite the promise for drug discovery, key liabilities such as low affinity and/or limited bioavailability have precluded the clinical success of previously described galectin-3 inhibitors, challenges Galecto Biotech are hoping to overcome. GB1211, the flagship compound of a new class of α-d-monogalactopyranoside with nanomolar affinity and improved oral bioavailability, demonstrated promising preclinical efficacy and is currently in early clinical development for liver fibrosis and…