Immune & Inflammation · Dosing reference

Larazotide dosage

Doses given in registered human trials, how long they ran, and the arithmetic for working with vials.

InvestigationalBLimited human dataTrial doses

Full research page Cycle-length evidence Compare Prefer Amiravo on Google

Regulatory status: Investigational
Human amounts: Phase 2b celiac trial (NCT01396213): 0.5, 1 or 2 mg three times daily for 12 weeks; phase 3 (NCT03569007): 0.25 or 0.5 mg three times daily
Route studied: Oral capsule
Frequency: Three times daily (celiac trials)
Half-life: Not established
Evidence grade: Grade B · Limited human data
Vial sizes on the market: Not recorded
Other forms seen: —

What Larazotide is

Larazotide acetate is an investigational oral 8-amino-acid tight-junction regulator peptide that has been tested in randomized trials in celiac disease, where a phase 3 study was terminated by its sponsor.

Larazotide acetate is described as a tight-junction (TJ) regulator that, in vitro, prevents the opening of intestinal epithelial tight junctions ^3,5. Cell and animal findings Tight-junction disassembly: In Caco-2 and IEC6 cells, larazotide inhibited ZO-1 and actin redistribution caused by gliadin fragments and by AT-1002, a peptide derived from the V. cholerae zonula occludens toxin, and inhibited the… How it works →

Key evidence

Paterson et al., Aliment Pharmacol Ther · 2007 · Humans (adults with celiac disease)
No increase in adverse events versus placebo; after gluten exposure, intestinal permeability rose 70% in the placebo group but not in the AT-1001 group, and gastrointestinal symptoms were more frequent with placebo ^4. ⁴
Leffler et al., Am J Gastroenterol · 2012 · Humans (86 adults with diet-controlled celiac disease)
The lactulose/mannitol ratio difference versus placebo was not significant and was highly variable; some lower doses, but not the highest, appeared to limit gluten-induced symptom worsening ^3. ³
Kelly et al., Aliment Pharmacol Ther · 2013 · Humans (184 adults with celiac disease)
No significant difference in lactulose-to-mannitol ratio; the lowest dose limited gluten-induced symptoms and all doses showed lower anti-tTG IgA rise versus placebo; adverse event rates were similar to placebo ^2. ²

All studies on the research page

Doses given in human trials

In the phase 2b trial NCT01396213 (342 adults), participants received larazotide acetate 0.5, 1 or 2 mg capsules three times daily or placebo for 12 weeks, after a 4-week placebo run-in and before a 4-week placebo run-out ^1,11.
In the phase 3 trial NCT03569007 (307 enrolled; terminated by sponsor), arms were larazotide 0.25 mg or 0.50 mg capsules three times daily, or matching placebo ^10.
In the gluten-challenge trial by Kelly et al. (184 patients), arms were 1, 4 or 8 mg three times daily or placebo, with 2.7 g of gluten daily for 6 weeks ^2.
In the long COVID phase 2a trial NCT05747534, participants received 250 or 500 micrograms orally four times daily for 21 days (by body weight below or at least 25.0 kg), or placebo ^12.

How long did human studies run?

No human study durations are recorded for Larazotide.

Cycle-length evidence for Larazotide

Side effects reported in studies

Headache
Among the most common adverse events (rates not given in the abstract) · 86 adults with celiac disease, 14-day trial ³
Urinary tract infection
Among the most common adverse events (rates not given in the abstract) · 86 adults with celiac disease, 14-day trial ³
Overall adverse events
Similar to placebo · 184 adults with celiac disease undergoing 6-week gluten challenge; 342 adults over 12 weeks ²

Full adverse-event data

Supplies and handling

Lyophilized vial
Sealed vial with the freeze-dried cake. Check the label, lot and the certificate of analysis before opening.
Sterile diluent
The diluent named on the product documentation. Bacteriostatic water contains benzyl alcohol; sterile water does not.
Graduated syringes
Sized to the volume being measured. U-100 insulin syringes are graduated in units where 100 units = 1 mL.
Alcohol prep pads
For wiping vial stoppers before each puncture.
Nitrile gloves
Clean gloves for aseptic handling.
Sharps container
Puncture-resistant container for used needles.

Step-by-step reconstitution guide Storage and transport accessories

Storage

Follow the supplier's documentation for the specific lot; peptides of this kind are generally kept dry and protected from heat, light and moisture.

Lyophilized (unmixed) vials: typically stored cold and dry, away from light, as the documentation directs. Many are stable longer frozen.
Reconstituted vials: typically refrigerated (about 2–8 °C), protected from light and not frozen.
Bacteriostatic water contains benzyl alcohol, which inhibits bacterial growth in multi-use vials; sterile water has no preservative.

Handling mistakes and troubleshooting

Added the wrong volume of diluent: The concentration changes, not the amount of compound in the vial. Recalculate with the volume actually added and relabel the vial.
Shook the vial and it foamed: Let it settle in the refrigerator. Foam is a sign of agitation; some peptides aggregate when shaken. Note it on the label.
The solution is cloudy or has particles: Do not use it. Cloudiness can indicate incomplete dissolution, contamination or degradation. Record the lot and contact the supplier with the certificate of analysis.
The powder cake looks melted or shrunken before reconstitution: This can indicate the vial was exposed to heat or moisture. Record the lot and condition on arrival.
Liquid sprayed back when the needle was removed: Pressure built up in the vial. Withdraw a small volume of air while adding diluent to keep pressure neutral.

Regulatory status

Status: Investigational; not FDA-approved for any use as of 2026-10-24. The phase 3 celiac disease trial (NCT03569007) is recorded as terminated by the sponsor, and phase 2a trials in long COVID and MIS-C have been run by Massachusetts General Hospital ^10,12,13.
United States (FDA): No FDA approval was identified as of 2026-10-24; the phase 3 trial NCT03569007 is recorded as terminated by the sponsor (last update July 2022) ^10.
Sport (WADA): Larazotide is not named on the WADA 2026 Prohibited List; S0 prohibits at all times any pharmacological substance not addressed elsewhere on the List with no current governmental approval for human therapeutic use, such as drugs under clinical development ^14.

Status varies by country and changes over time. How we describe regulatory status.

Larazotide compared with related compounds

Compound	Status	Evidence	Human amounts	Half-life
Larazotide	Investigational	B	Trial doses	—
Thymulin	Not approved — research use only	C	None established	Not located in the sources reviewed for
LL-37	Not approved — research use only	B	None established	—
KPV	Not approved — research use only	C	None established	—
Thymosin Alpha-1	Approved outside the US	B	None established	—
VIP	Investigational	A	Trial doses	A review of VIP in cardiopulmonary disea

Frequently asked questions

What doses of Larazotide have been studied in humans?

Larazotide is investigational. This page lists the amounts given in each cited trial as facts about those studies.

Is there an established Larazotide cycle length?

No. We found no human studies that report treatment duration for Larazotide.

How much bacteriostatic water should be added to a Larazotide vial?

There is no compound-specific volume. The diluent volume only sets the concentration: concentration = mass in the vial ÷ volume added (for example, 10 mg in 2 mL gives 5 mg/mL). The calculator on this page shows the arithmetic for any combination.

How many units is a given amount on an insulin syringe?

On a U-100 syringe, 100 units = 1 mL. Units for an amount = amount ÷ (concentration per unit). The calculator converts any amount you enter at the concentration you choose; a unit is a volume mark, not an amount of compound.

Is Larazotide FDA-approved?

Investigational. Investigational; not FDA-approved for any use as of 2026-10-24. The phase 3 celiac disease trial (NCT03569007) is recorded as terminated by the sponsor, and phase 2a trials in long COVID and MIS-C have been run by Massachusetts General Hospital ^10,12,13.

References

Larazotide acetate for persistent symptoms of celiac disease despite a gluten-free diet: a randomized controlled trial Gastroenterology. 2015
Larazotide acetate in patients with coeliac disease undergoing a gluten challenge: a randomised placebo-controlled study Aliment Pharmacol Ther. 2013
A randomized, double-blind study of larazotide acetate to prevent the activation of celiac disease during gluten challenge Am J Gastroenterol. 2012
The safety, tolerance, pharmacokinetic and pharmacodynamic effects of single doses of AT-1001 in coeliac disease subjects: a proof of concept study Aliment Pharmacol Ther. 2007
Larazotide acetate regulates epithelial tight junctions in vitro and in vivo Peptides. 2012
Larazotide acetate promotes tight junction assembly in epithelial cells Peptides. 2012
Larazotide acetate for treatment of celiac disease: A systematic review and meta-analysis of randomized controlled trials Clin Res Hepatol Gastroenterol. 2022
Viral spike antigen clearance and augmented recovery in children with post-COVID multisystem inflammatory syndrome treated with larazotide Sci Transl Med. 2025
Lack of relationship of AT1001 to zonulin and prehaptoglobin-2: clinical implications Gut. 2021
ClinicalTrials.gov record NCT03569007: Phase 3 study of larazotide acetate for persistent symptoms in celiac disease on a gluten-free diet (terminated) ClinicalTrials.gov. 2026
ClinicalTrials.gov record NCT01396213: Phase 2 dose-ranging study of larazotide acetate in celiac disease ClinicalTrials.gov. 2026
ClinicalTrials.gov record NCT05747534: Phase 2a study of larazotide (AT1001) for long COVID in children and adults ClinicalTrials.gov. 2026
ClinicalTrials.gov record NCT05022303: Phase 2a study of AT1001 for COVID-19 related MIS-C (terminated) ClinicalTrials.gov. 2026
World Anti-Doping Agency Prohibited List 2026 (online version) WADA. 2026
PubChem compound record for larazotide PubChem. 2026

Last reviewed October 24, 2026 by the Amiravo editorial team. Editorial policy · Report an error