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Gastrointestinal

Larazotide

Also called larazotide acetate, AT-1001, INN-202

Larazotide is a small, swallowed peptide designed to tighten the seals between cells lining the gut. It was tested for years as a pill for celiac disease, as an add-on to a gluten-free diet. Its final large trial was stopped in 2022 because it was unlikely to work, and it is not approved anywhere.

Late-stage trialsTested in large human trials (phase 2b/3) but not yet approved in the US.

All printable flashcards

Drawn from its published sequence: 8 residues, one bead each.

Overview

Larazotide is a small, swallowed peptide designed to tighten the seals between cells lining the gut. It was tested for years as a pill for celiac disease, as an add-on to a gluten-free diet. Its final large trial was stopped in 2022 because it was unlikely to work, and it is not approved anywhere.

How it works

Proposed: larazotide is thought to block signaling (linked to the protein zonulin) that loosens tight junctions between intestinal cells, reducing the leak of gluten fragments and other substances through the gut wall. It acts locally in the gut and is poorly absorbed into the blood. Clinical trials did not clearly confirm a meaningful benefit.

What research shows

  • Gluten challenge (Kelly et al. 2013, phase 2b RCT, 184 enrolled and 177 randomized): 1, 4 or 8 mg three times daily for 6 weeks alongside a daily gluten challenge. The primary endpoint, a urinary sugar test of gut permeability, did not differ significantly from placebo at any dose; the 1 mg group showed better symptom scores.
  • Persistent symptoms on a gluten-free diet (Leffler et al. 2015, phase 2b RCT, n=342): 0.5, 1 or 2 mg three times daily for 12 weeks; only the 0.5 mg dose beat placebo on the primary symptom score, and the two higher doses did not differ from placebo on any endpoint.
  • Phase 3 CeDLara trial (NCT03569007, 9 Meters Biopharma): discontinued in 2022. A pre-specified interim analysis indicated that far more patients than planned would be needed to show a significant effect, and the sponsor judged that infeasible.

Doses studied in people

Study or labelDose usedSource
Phase 2b RCT, gluten challenge in celiac disease (Kelly 2013; 184 enrolled, 177 randomized)1, 4 or 8 mg orally three times daily, 15 minutes before meals, for 6 weeks1
Phase 2b RCT, celiac disease with persistent symptoms on a gluten-free diet (Leffler 2015, n=342)0.5, 1 or 2 mg orally three times daily, 15 minutes before meals, for 12 weeks2

Doses are from published phase 2 trials; no dose is approved, and the phase 3 program was discontinued in 2022 after an interim analysis.

Read this first: these are the amounts given to participants in published studies or written on official prescribing labels, reported for reference. They are not recommendations. Trial doses were chosen for specific patients under medical supervision, and a dose that is safe in one person can be harmful in another.

Vial math

Many research vials hold 5 or 10 mg of powder. This table shows how much ends up in each mark on a U-100 insulin syringe for common amounts of added liquid. It is arithmetic only, not a dose.

VialLiquid addedConcentrationPer unit (0.01 mL)
5 mg1 mL5 mg/mL50 mcgOpen in calculator
5 mg2 mL2.5 mg/mL25 mcgOpen in calculator
5 mg3 mL1.67 mg/mL16.7 mcgOpen in calculator
10 mg1 mL10 mg/mL100 mcgOpen in calculator
10 mg2 mL5 mg/mL50 mcgOpen in calculator
10 mg3 mL3.33 mg/mL33.3 mcgOpen in calculator

More sizes: all vial sizes · How this works: Syringes and units · Reconstitution guide.

Safety

  • Generally well tolerated in phase 2 trials; adverse event rates were similar to placebo (Kelly 2013, Leffler 2015).
  • No proven benefit: the phase 3 trial was halted for futility (2022).
  • Unknown long-term safety.

Report side effects of any drug or product to the FDA through MedWatch. For a possible poisoning in the US, call Poison Control at 1-800-222-1222.

History

Developed from research by Alessio Fasano's group on intestinal permeability, first by Alba Therapeutics (as AT-1001), later by Innovate Biopharmaceuticals, which became 9 Meters Biopharma. Phase 2 trials ran from about 2007 to 2015. The phase 3 CeDLara trial (NCT03569007) began in 2019 and was discontinued in 2022 after an interim analysis showed it was unlikely to meet its goal.

Common questions

Is larazotide approved for celiac disease?

No. Its phase 3 celiac trial was stopped in 2022 after an interim analysis showed it was unlikely to succeed 34.

Why was the larazotide phase 3 trial stopped?

An interim check found that far more patients than planned would be needed to show a significant effect, and the sponsor judged that unworkable 4.

What did earlier trials show?

In a gluten-challenge trial, no dose beat placebo on the main gut-permeability test, though the 1 mg group had better symptom scores 1. In a trial of 342 people with ongoing symptoms, only the 0.5 mg dose beat placebo on the main symptom score 2.

What doses were tested?

Phase 2 trials gave 0.5 to 8 mg by mouth three times daily, 15 minutes before meals, for 6 or 12 weeks 12. No dose is approved 4.

Is larazotide safe?

It was generally well tolerated in phase 2 trials, with side effect rates similar to placebo 12.

Is larazotide banned in sport?

It is not named on WADA's 2026 list, but as an unapproved substance it would likely fall under S0, prohibited at all times 6.

Related compounds

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BPC-157

Body Protection Compound-157 · PL 14736

BPC-157 is a lab-made chain of 15 amino acids based on part of a protein found in human stomach juice.

Immune & antimicrobialPreclinical onlyFlashcard

KPV

Lys-Pro-Val · alpha-MSH (11-13)

KPV is a very small peptide made of three amino acids (lysine, proline, valine).

Sources

  1. Larazotide acetate in patients with coeliac disease undergoing a gluten challenge: a randomised placebo-controlled study Journal
  2. Larazotide Acetate for Persistent Symptoms of Celiac Disease Despite a Gluten-Free Diet: A Randomized Controlled Trial Journal
  3. Study to Evaluate the Efficacy and Safety of Larazotide Acetate for the Relief of CeD Symptoms (CeDLara, NCT03569007) ClinicalTrials.gov
  4. 9 Meters Biopharma press release: interim analysis does not support continuation of the phase 3 larazotide trial (June 21, 2022) Regulatory
  5. Bulk Drug Substances Nominated for Use in Compounding Under Section 503A Regulatory
  6. WADA Prohibited List Regulatory
  7. US Patent 9,051,349 B2 — Larazotide acetate compositions (defines the octapeptide sequence) Regulatory

Last reviewed 2026-10-25 · How we research · Found an error? See our corrections policy.