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BL1106 is an orally available small molecule inhibitor of tissue transglutaminase 2 (tTG2), originally developed by BioLineRx for the treatment of Celiac disease. The drug targets the enzymatic activity of tTG2 in the small intestine, which is responsible for the deamidation of gluten-derived gliadin peptides. This deamidation increases the binding affinity of these peptides to HLA-DQ2 and HLA-DQ8, leading to the activation of gluten-specific T-cells and the characteristic inflammatory response seen in Celiac patients. By inhibiting tTG2, BL1106 was intended to prevent the initiation of this autoimmune cascade. Development was discontinued in the early stages of clinical planning.
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