Galectin-1 is a member of a family of evolutionarily conserved glycan-binding proteins, displays broad anti-inflammatory and pro-resolving activities by targeting multiple immune cell types[1]. Galectin-1 is also a carbohydrate-binding protein is implicated in cancer cell proliferation, invasion and tumor angiogenesis. OTX008 is a calixarene-based compound and selective galectin-1 (Gal-1) inhibitor with potential anti-angiogenic and antineoplastic activities. OTX008 inhibited tumor cell proliferation, though inhibition was very variable, with IC50 ranging from 1.7 to 192.3 μM. In vivo, the human ovarian carcinoma A2780-1A9 and human glioblastoma U87MG showed a different degree of sensitivity to OTX008 (IC50 of 2.1 and 35.8 μM, respectively). OTX008 achieved a Cmax of 14.39 μg/mL (15.35 μM) and then the drug was rapidly distributed through the body with half-life (HL) of 20 min and cleared from plasma with a long elimination HL of 31.4 h. In vitro, OTX008 inhibited endothelial cell proliferation in a concentration-dependent manner with a mean IC50 values of 9.9 ± 4.2, 8.7 ± 1.7, and 12.9 ± 3.3 μM respectively[2].
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