- Guide to PHARMACOLOGY
Synonyms: galectin 3 | GALIG | LGALS2 | MAC-2
Compound class: Endogenous peptide in human, mouse or rat
Comment: Galectin 3 (Gal-3) is one of a group of 14 lectins that bind β-galactoside-containing carbohydrates, via a carbohydrate recognition domain (CRD), and it binds to galectin-3 binding protein. It plays regulatory functions in multiple biological processes, including cell-cell adhesion, cell-matrix interactions, macrophage activation, leukocyte migration, inflammation, angiogenesis, metastasis, apoptosis  and fibrosis. Galectin 3 is being investigated as a molecular target for the development of novel therapeutics for cancer [9,11], cardiovascular disease [3,5] and fibrosis (e.g. liver fibrosis in nonalcoholic fatty liver disease (NAFLD) and nonalcoholic steatohepatitis (NASH) ) . GM-MD-02 (Galectin Therapeutics) is a galactoarabino-rhamnogalacturonan polysaccharide polymer (pectin) that binds to Gal-3 (Kd 8 μM: Gal-1 Kd 10 μM)) and reduces inflammation and fibrosis-associated effects in experimental models , but no clinical efficacy was observed in Phase 2 evaluation in patients with NASH cirrhosis (NCT02462967), although in the subset of patients with cirrhosis who had no esophageal varices some clinical benefit has been indicated, and Phase 3 testing in this subset of cirrhosis patients is planned.
In relation to cardiovascular disease, galectin 3/galectin 3 binding protein complexes co-localize to the leukocyte/endothelial cell interface of vein walls in mice and galectin 3 increases vein wall IL-6 levels and promotes venous thrombosis . In human patients, elevated circulating galectin-3 binding protein correlates with acute venous thrombosis.
|No information available.|
|Summary of Clinical Use|
|GB1211 has entered phase 1 safety and tolerability evaluation.|
|Clinical Trial ID||Title||Type||Source||Comment||References|
|NCT03809052||A First in Human Study to Evaluate the Safety, Tolerability and Pharmacokinetics of GB1211 in Healthy Subjects and in Subjects With Suspected Non-Alcoholic Steato-Hepatitis (NASH) and Liver Fibrosis||Phase 1 Interventional||Galecto Biotech AB|