AMT-101   Click here for help

GtoPdb Ligand ID: 11645

Immunopharmacology Ligand
Comment: AMT-101 is an orally deliverable IL-10-cholix fusion protein [1]. It combines the anti-inflammatory IL-10 with a nontoxic fragment of the cholix exotoxin from Vibrio cholerae. The exotoxin fragment facilitates delivery of the fusion protein selectively to the intestinal epithelium via transcytosis through intestinal enterocytes into the lamina propria, where it is intended to treat intestinal inflammatory diseases. IL-10 treatment is associated with dose limiting systemic toxicities including anemia and thrombocytopenia. AMT-101 was designed to overcome this limitation by restricting its IL-10 activity to within the GI tract.
Bioactivity Comments
AMT-101 induces dimerisation of the IL-10 receptor subunits in intestinal epithelial cells in vitro (EC50 0.97 nM) which indicates activity of the IL-10 portion of the protein at its intended target [1]. It also mediates anti-inflammatory activity in in vivo models of intestinal inflammation which are indicative of the desired biological activity.