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Milategrast (E6007) is an orally administered small molecule integrin activation inhibitor developed primarily for the treatment of inflammatory bowel diseases such as ulcerative colitis. Its mechanism of action involves inhibiting the interaction between calreticulin and integrin α4, thereby blocking leukocyte adhesion and infiltration into inflamed tissues. This anti-inflammatory effect is achieved by suppressing the activity of integrins on leukocytes, which are key mediators in the pathogenesis of inflammatory bowel disease. Milategrast was developed by Eisai and EA Pharma but its clinical development for ulcerative colitis and other inflammatory bowel diseases has been discontinued due to business priorities[2][3][5].
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