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In a phase 2 proof-of-concept trial, patients with celiac disease controlled on a gluten-free diet were assigned to one of three dose levels of ZED1227 (a selective transglutaminase 2 inhibitor) or placebo. Patients were challenged with 3 g of gluten daily for 6 weeks. Comparison of duodenal-biopsy samples between baseline and 6 weeks showed that ZED1227 attenuated gluten-induced mucosal damage.