Larazotide

Areas of active research — not promised effects

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Larazotide acetate has never received FDA approval as a drug. Clinical investigation was conducted under an IND, but the sponsor (9 Meters Biopharma) discontinued its primary celiac disease program in June 2022 and subsequently filed for bankruptcy, leaving no active NDA or IND sponsor for the original program. It is not on the FDA Category 2 bulk drug substances list (fda19=false) and is not on the FDA 503B bulk drug list, meaning it is not lawfully compoundable by 503A or 503B pharmacies under current FDA policy. Access is limited to any remaining active clinical trials or investigator-sponsored expanded access programs under 21 CFR 312.300.

Transparent blend · bci-1.0 · never paid-placement

Primary name

Larazotide

Origin

Larazotide acetate (AT-1001) is a synthetic 8-amino-acid peptide whose sequence is derived from structural motifs of the Vibrio cholerae-derived zonula occludens toxin (Zot) and its mammalian analogue zonulin, endogenous modulators of intestinal tight junction assembly. It does not occur freely in nature. CAS 258818-34-7; molecular formula C32H55N9O10; MW 725.8 Da. It was developed initially by Alba Therapeutics and later advanced by 9 Meters Biopharma, Inc., which discontinued its celiac disease Phase 3 program in June 2022 and subsequently filed for bankruptcy.

Registry IDs

PubChem CID

9810532

CAS

258818-34-7

InChIKey

ORFLZNAGUTZRLQ-ZMBVWFSWSA-N

DrugBank

DB05645

ChEMBL

CHEMBL2105646

Molecular formula

C32H55N9O10

Molar mass

725.8 g/mol

Monoisotopic

725.40718899 Da

InChIKey

ORFLZNAGUTZRLQ-ZMBVWFSWSA-N

Appearance

White to off-white lyophilized powder

Solubility

Soluble in water; the acetate salt form is freely water-soluble at research conc…

Sequence not available in current seed.

Stability: Peptide is subject to proteolytic degradation in GI fluids; delayed-release enteric formulations have been developed specifically to target mid-duodenal/jejunal

Vial sizes

2 mg · 5 mg

Purity grades

≥98% HPLC

Salt forms

Free base (primary)

• GHS hazard class on file
• PPE & spill response
• Disposal guidance
• Not-for-human-consumption posture

How much research exists, and of what maturity — never a verdict on whether it works.

Mechanism of action

• Larazotide acetate acts as a competitive antagonist at the zonulin receptor on intestinal epithelial cells, blocking the endogenous zonulin signaling cascade that otherwise drives disassembly of occludin- and claudin-based tight junction complexes
• By preventing this opening, the peptide reduces paracellular permeability in the small intestinal epithelium and limits the translocation of dietary antigens — notably gliadin peptides — across the epithelial barrier into the lamina propria
• Secondary mechanistic data suggest inhibition of myosin light chain kinase activity, which reduces actomyosin contraction and thereby facilitates maintenance of tight junction integrity
• The result is a reduction in luminal-antigen-driven immune activation without direct immunosuppression, distinguishing it mechanistically from anti-inflammatory agents

Pharmacokinetics (ADME)

Half-life

Systemic half-life not formally characterized; earlier studies reported inability to detect larazotide in systemic blood samples, consistent with predominantly local (luminal) action

Clearance

Presumed rapid luminal proteolysis and negligible systemic absorption; no formal clearance data published

PK–PD note: A porcine delayed-release formulation study (PMID 33844694) measured peak luminal concentrations of 0.32–1.76 µM in the distal duodenum and proximal jejunum at approximately 1 hour after oral dosing (…

Reading the evidence

• Evidence quality and gaps vary by application — see the cited grades above.
• Indexed-article counts span all evidence tiers, not only completed human trials.
• No first-party human-dosing, efficacy, or benefit claims are made here.

Key reviews & evidence-gap sources

• Hoilat GJ et al. Larazotide acetate for treatment of celiac disease: A systematic review and meta-analysis of randomized controlled trials. Clin Res Hepatol Gastroenterol. 2022;46(1):101782. — Anchoring systematic review/meta-analysis (PubMed pubtype: Meta-Analysis, Systematic Review)
• Slifer ZM et al. Larazotide acetate: a pharmacological peptide approach to tight junction regulation. Am J Physiol Gastrointest Liver Physiol. 2021;320(6):G983-G989. — Mechanism-focused review (tight junction regulator)
• Troisi J et al. The Therapeutic use of the Zonulin Inhibitor AT-1001 (Larazotide) for a Variety of Acute and Chronic Inflammatory Diseases. Curr Med Chem. 2021;28(28):5788-5807. — Review of zonulin-inhibitor therapeutic applications (Fasano senior author)

1 registered trial — 0 currently recruiting.

Phase 2
NCT00362856
Safety and Tolerability Study of Larazotide Acetate in Celiac Disease Subjects

COMPLETED

Summary (literature)

Across multiple Phase 1 and Phase 2 trials, larazotide acetate demonstrated a safety profile comparable to placebo. In Phase 1 studies of healthy volunteers, single and repeat doses ranging from 0.25 mg to 36 mg (oral) produced no severe drug-related adverse events; mild headache…

WADA status

Not specifically listed on the WADA 2026 Prohibited List. Larazotide acts locally in the gastrointestinal tract with negligible systemic absorption and has no k…

Dominant research route: Oral (PO)

Phase I, Phase II (RCT, 342 adults with celiac disease, NCT00620451), Phase III (NCT03569007, discontinued), and porcine in vivo PK with delayed-release formulation

Bioavailability: Designed as a non-systemic, intestine-targeted (NSIT) drug; earlier studies attempted unsuccessfully to determine LA pharmacokinetics from plasma because the peptide is broken down in the small intestine with no systemic absorption of LA or fragments. Intestinal fluid sampling in pigs was required to quantify concentrations at the site of action.

Larazotide acetate is an orally administered, locally acting synthetic 8-amino-acid peptide that acts as a tight junction regulator / zonulin antagonist in the intestinal lumen. All clinical trials (Phase I through III) and animal PK studies used the oral route. A delayed-release formulation was developed to target release in the mid-duodenum and jejunum, the site of celiac disease pathology.

Animal & human figures are kept visibly separate so studied animal doses are never misread as human guidance.

Sorted A–Z by vendor — never by price

Researched storefront prices, bucketed

p25 $9.00 · median $9.60 · p75 $12.75 · 5 researched vendors

Legit, COA-backed band: $6.75–$12.80/mg.

Value rule: don't just buy the cheapest — a price under $3/mg is a red flag. Pair price with COA and independent-test grade.

Estimated cost of research (10 mg)

Vial (best researched price)

$68

Bacteriostatic water (generic estimate)

$6

Syringes / supplies (generic estimate)

$12

What each test proves — general guidance, plus this compound's researched purity data

Purity on the current market (researched)

Research-chemical vendors self-report purity of ≥98% by HPLC (e.g., AOBIOUS, Cayman Chemical) to ≥99% by HPLC (e.g., Research Scientific Ltd). These are vendor-supplied CoA claims, not independently verified by a third-party laboratory.

Independent labs cited for this compound

No FDA recalls or market withdrawals specific to larazotide acetate were found in FDA Enforcement Reports or recall databases as of the date of this review.

Buyer red-flag checklist

• Larazotide acetate explicitly named in FDA Warning Letter to Darmerica, LLC (Dec 2025) as ineligible for human drug compounding under section 503A of the FD&C Act
• Phase 3 CeDLara trial discontinued in 2022 after failing to meet primary endpoint; no FDA-approved indication exists
• No independent third-party lab test results (Janoshik or equivalent) publicly available for larazotide sold as a research chemical
• Research-chemical vendor purity claims (≥98–99% HPLC) are self-reported and unverified by independent analysis
• Larazotide sold by online research-chemical vendors is not the same material used in clinical trials (which was manufactured under GMP for investigational use)

GMP vs research-grade: the chemistry (SPPS + HPLC + MS) is identical — the difference is the quality system.

Underdosing / mislabeling: No independent lab testing data (Janoshik, MZ Biolabs, Finnrick, or similar) was found for larazotide acetate. The Janoshik public results portal was not accessible (HTTP 403). No underdosing prevalence data is available for this compound.

• An RUO label is not an import exemption — CBP judges actual intended use.
• Lyophilized powder is ambient-stable in transit; temperature control needed for > 7-day transit.
• US-warehouse vendors dodge import scrutiny — they cost more but ship more reliably.

Every item dated & sourced

Not listed on the WADA Prohibited List. Larazotide is not identified as a prohibited substance in any WADA prohibited list edition. It is an investigational tight-junction regulator peptide with no known performance-enhancing properties.

No granted patents identified in current seed. Composition-of-matter coverage is limited given the peptide's synthetic origin.

• IACUC / IRB research context
• RUO buyer responsibilities & documentation
• Veterinary / alternative-use where lawful
• Jurisdiction-aware "who may lawfully obtain"

What people discuss

Reported concerns — discussion, not established effects

Reading caveats

• Self-experimentation outside clinical trials discussed
• Research-chemical sourcing without independent verification
• Small-sample anecdotal reports dominate personal-experience threads
• Phase 3 failure context often omitted in positive anecdotes
• Pediatric off-label use discussed without clinical oversight

Manually researched from reddit, youtube— theme weights are research estimates, not live counts; aggregated & de-identified. No individual posts, quotes, or usernames are ever shown.

Relative research / market volume — populated once the activity stream is wired

Inline tooltips for lyophilized, RUO, EU/mg, SPPS, 503A and more.

Toggle plain-language ↔ scientific in the header.

• How to read a COA
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• Understanding evidence grades

Synthetic 8-amino-acid tight junction regulator studied in celiac disease and MIS-C for its intestinal permeability-reducing effects. Approximately 81 articles are indexed (literature last scanned 2026-05-29). US regulatory status: Investigational; no FDA approval; IND program effectively inactive following 9 Meters Biopharma bankruptcy. Research use only.

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