Larazotide (AT-1001)

Larazotide is an eight amino acid peptide with the sequence glycine-glycine-valine-leucine-valine-glutamine-proline-glycine, usually supplied as the acetate salt. Its structure derives from a protein secreted by Vibrio cholerae, the zonula occludens toxin, and it was developed as an antagonist at that pathway rather than as an agonist. Alba Therapeutics took it into celiac disease (PMID: 17697209), and it was later developed by 9 Meters Biopharma under the code INN-202 (NCT03569007). It is not approved anywhere.

The target is the intestinal tight junction. In celiac disease, gluten peptides reach the lamina propria and trigger an immune response, and increased paracellular permeability is one route by which they get there. Larazotide acts locally in the gut lumen to keep tight junctions closed. Mechanistic work links it to redistribution and rearrangement of tight junction proteins and actin filaments, and more recently to inhibition of myosin light chain kinase, which reduces tension on actin filaments and lets the junction close (PMID: 33881350). Because it works in the lumen and is taken orally, it is not designed to reach the systemic circulation.

Animal work supports the barrier mechanism outside celiac disease. In interleukin 10 gene-deficient mice, treatment reduced small intestinal permeability and attenuated colitis, with lower colonic tumor necrosis factor alpha secretion at 17 weeks (PMID: 18829978). In pigs, it induced recovery of ischemia-injured jejunum through repair of tight junctions (PMID: 33886649). Rat studies report reduced intestinal permeability and bacterial translocation in acute pancreatitis (PMID: 38441784) and reduced liver and intestinal damage in acute liver failure (PMID: 34791921).

The human record is unusually complete for a compound sold as a research chemical, and it is mixed. A proof of concept study in celiac disease subjects challenged with gluten found no increase in adverse events, no rise in intestinal permeability in the treated group against a 70 percent rise on placebo, and fewer gastrointestinal symptoms (PMID: 17697209). Two gluten-challenge trials in 86 and 184 patients failed to separate from placebo on the lactulose to mannitol permeability ratio, but reported reductions in symptoms and, in the larger trial, lower anti-transglutaminase antibody rises (PMID: 22825365, PMID: 23163616). A 342-patient phase 2b trial in patients who still had symptoms on a gluten-free diet met its primary symptom endpoint at the lowest dose tested and not at higher doses (PMID: 25683116). The phase 3 trial then stopped: NCT03569007 enrolled 307 patients and was terminated in 2022 after a pre-specified interim analysis indicated that the number of additional patients needed to show a significant clinical effect was too large to continue (NCT03569007; sponsor announcement, June 2022).

Interest has since moved to other barrier-driven conditions. A phase 2a randomized trial in 12 children with multisystem inflammatory syndrome after COVID-19 reported no larazotide-related adverse events, faster clearance of circulating SARS-CoV-2 spike antigen and faster resolution of gastrointestinal symptoms (PMID: 40737433). A long COVID phase 2a trial has completed (NCT05747534). What is sold as a research chemical capsule is an investigational drug, not an approved medicine.

Larazotide (AT-1001) is available in capsule form.

Compare prices, payment methods, shipping, and COA scores across 1 vendor.

1 of the vendors BodyHackGuide tracks list Larazotide (AT-1001) (1 listing). The lowest listed price BodyHackGuide has recorded for Larazotide (AT-1001) is $99.99. No Larazotide (AT-1001) listing recorded as in stock carries a milligram count, so BodyHackGuide states no price per milligram for Larazotide (AT-1001).

BodyHackGuide holds 1 third-party certificate record for Larazotide (AT-1001), from Disguised Alpha. No editor has read any of BodyHackGuide's 1 certificate record for Larazotide (AT-1001). The laboratory named on BodyHackGuide's Larazotide (AT-1001) certificate record is Freedom Diagnostics Testing, and the test date on it is 30 July 2026. Each vendor page on BodyHackGuide shows how many certificate records BodyHackGuide holds for that vendor and links to each record that has its own page.