Larazotide Acetate
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Complete Research Guide
Open each section for the available evidence. Gaps are stated rather than inferred.
Overview
Larazotide Acetate is listed as gut / tight-junction regulator.
- •Celiac disease (adjunct)
- •Leaky-gut / barrier dysfunction (research)
Regulatory status: Investigational (9 Meters Biopharma) — Phase 3 CeDLara.
Structure & Properties
Compound: Larazotide Acetate; also known as AT-1001, INN-202.
Pharmacologic class: Gut / Tight-Junction Regulator.
Known delivery routes: Oral.
Sequence, molecular weight, salt form, and excipient details are formulation-specific and are not listed unless verified by a manufacturer or laboratory COA.
How It Works
8-aa peptide that antagonizes zonulin signaling — preserves intestinal tight junctions, reducing paracellular permeability and antigen translocation.
- •Reduced GI symptoms in gluten-exposed celiac patients
- •Decreased intestinal permeability markers
Human Research
Evidence grade: Clinical RCT (Limited)
Clinical RCT (Limited). Phase 2b positive; Phase 3 missed primary endpoint (2022).
Laboratory Research
Phase 2b positive; Phase 3 missed primary endpoint (2022)
Preclinical findings describe biological plausibility, not proven benefit in people. Animal and laboratory doses do not translate directly to human use.
Processing & Interactions
Timing and exposure
Oral, 15 min before each meal (typically 3× daily). Do not take with food — reduces efficacy.
Potential interactions and combinations to avoid
- •Concurrent immunosuppressants without oversight
Absorption, half-life, metabolism, and clearance can vary by formulation and route. Use prescribing information when an approved product exists.
Safety & Precautions
Known or reported risks
- •Headache
- •Mild GI upset
- •Mixed efficacy data
Contraindications
- •Hypersensitivity
- •Pregnancy (insufficient data)
- •Active gastrointestinal malignancy, polyposis, or undiagnosed GI bleeding
- •Colorectal adenoma history without current colonoscopic surveillance
- •Bowel obstruction, stricture, or acute abdominal pain of unknown cause
- •Not FDA-approved for human therapeutic use — no verified purity, sterility, or potency standards
- •Immunocompromised or transplant patients (unverified sterility and immunogenicity risk)
- •Concurrent participation in drug-tested sport (WADA prohibited or non-cleared substance)
- •Known hypersensitivity or prior reaction to this compound or any excipient/diluent
- •Pregnancy, attempting conception, or breastfeeding unless prescribed and monitored by a physician
- •Children and adolescents with open growth plates (unless under specialist endocrine care)
- •Active or recently treated malignancy without oncology clearance
- •Use without a confirmed diagnosis, baseline labs, and licensed clinical supervision
Unknown long-term toxicity should be assumed where controlled human data are limited. Seek urgent care for a severe or unexpected reaction.
Administration & Studied Formulations
Reference range: 0.5 mg TID before meals (trial)
Frequency: 3× daily
Cycling: Continuous with meals.
Oral
15 min before each meal, 3× daily.
Capsule. Empty stomach — do NOT take with food; food destroys efficacy.
Dosing information is educational context, not a personal recommendation. Approved products must follow their label and prescriber instructions.
Applications & Related Therapies
Potentially complementary measures
- •BPC-157, KPV for gut barrier stacks
Clinical use should account for diagnosis, approved alternatives, nutrition, activity, sleep, rehabilitation, current medicines, and appropriate monitoring.
Cases, Considerations & Ethics
Decision framework: establish the clinical goal, confirm evidence quality and legal status, screen contraindications and interactions, compare approved alternatives, define monitoring and stopping criteria, and use shared decision-making with a licensed clinician.
Case evidence: individual reports cannot establish safety or effectiveness and should not outweigh controlled trials.
Ethics: informed consent should distinguish established care from experimental use, disclose uncertainty and cost, avoid overstated claims, and never substitute research products for medically necessary care.
What is Larazotide Acetate?
In plain words
Larazotide acetate is an experimental peptide, a short chain of eight amino acids, designed to act in the gut. It aims to keep the seals between gut-lining cells closed, limiting the passage of substances that may trigger an immune response. Researchers have studied it as an add-on to a gluten-free diet for celiac disease and for problems with the gut barrier. Evidence of benefit is mixed, and reported side effects include headache and mild stomach or bowel upset.
Technical definition
Larazotide acetate (AT-1001, INN-202) is an investigational synthetic octapeptide derived from a sequence of the Vibrio cholerae zonula occludens toxin. It is proposed to antagonize zonulin-mediated signaling, preserving intestinal epithelial tight junctions and limiting paracellular permeability and antigen passage between cells. It is not FDA-approved; randomized trials in celiac disease have produced mixed efficacy findings, and the Phase 3 CeDLara trial was discontinued.
Function
Dosing
Recommended Time of Day
30 minutes before meals.
See “Timing & Interactions” below for full fasted/fed circumstances, what to avoid combining, and what pairs well.
Administration & Technique
Injection & Application Sites
Larazotide Acetate has no injection site — see the routes below.
Diagram is a general illustration, not a medical instruction. Rotate sites every injection, keep 1 in (2.5 cm) between recent sites, and avoid scars, moles, bruises and the navel area.
Cycling
Continuous with meals.
Timing & Interactions
- ·Concurrent immunosuppressants without oversight
- ·BPC-157, KPV for gut barrier stacks
Storage & Reconstitution
Reconstitution Calculator
1 mL = 100 units on a standard U-100 insulin syringe. Draw to the nearest 0.5 unit and confirm dosing with a clinician before injection.
Your Notes
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Benefits
- ·Reduced GI symptoms in gluten-exposed celiac patients
- ·Decreased intestinal permeability markers
Risks
- ·Headache
- ·Mild GI upset
- ·Mixed efficacy data
Contraindications
- ·Hypersensitivity
- ·Pregnancy (insufficient data)
- ·Active gastrointestinal malignancy, polyposis, or undiagnosed GI bleeding
- ·Colorectal adenoma history without current colonoscopic surveillance
- ·Bowel obstruction, stricture, or acute abdominal pain of unknown cause
- ·Not FDA-approved for human therapeutic use — no verified purity, sterility, or potency standards
- ·Immunocompromised or transplant patients (unverified sterility and immunogenicity risk)
- ·Concurrent participation in drug-tested sport (WADA prohibited or non-cleared substance)
- ·Known hypersensitivity or prior reaction to this compound or any excipient/diluent
- ·Pregnancy, attempting conception, or breastfeeding unless prescribed and monitored by a physician
- ·Children and adolescents with open growth plates (unless under specialist endocrine care)
- ·Active or recently treated malignancy without oncology clearance
- ·Use without a confirmed diagnosis, baseline labs, and licensed clinical supervision
Regulatory
Investigational (9 Meters Biopharma) — Phase 3 CeDLara
Veterinary Use (Pets)
No established veterinary protocol for Larazotide Acetate. Consult a licensed veterinarian before considering off-label use in any species.
Full veterinary reference →Functional Groups
Cited Works
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