Larazotide Acetate at a glance
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Larazotide acetate (AT-1001) is a synthetic 8-amino acid peptide that acts as a tight junction regulator in the intestinal epithelium. It was developed as a targeted therapy for conditions involving dysregulated intestinal permeability - most notably celiac disease, but also Crohn's disease, type 1 diabetes, and irritable bowel syndrome with diarrhea.
The mechanism centers on zonulin, an endogenous protein released by intestinal epithelial cells in response to gluten and other triggers that opens tight junctions paracellularly, increasing intestinal permeability. Larazotide competitively inhibits zonulin receptor activation, maintaining tight junction integrity and reducing the transepithelial passage of antigens, pathogens, and pro-inflammatory molecules.
In celiac disease, this mechanism is particularly relevant: gliadin fragments from wheat gluten trigger zonulin release, which opens tight junctions and allows gluten peptides to cross the epithelium and trigger the adaptive immune response. By reducing this permeability, larazotide does not treat celiac disease's underlying autoimmunity but acts as a complementary barrier-protective therapy on top of a gluten-free diet.
Phase 2b clinical trials in celiac disease patients demonstrated that larazotide 0.5 mg three times daily significantly reduced GI symptom scores, decreased intestinal permeability markers, and lowered IL-10 and IFN-γ levels compared to placebo - even in patients on a gluten-free diet who still experience symptoms. A subsequent Phase 3 trial (INN-202) in non-responsive celiac disease is ongoing, representing the most advanced clinical development of a tight junction regulator peptide.
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