Larazotide
aka Larazotide acetate · AT-1001 · INN-202 · GGVLVQPG
Mechanism
Synthetic eight-amino-acid peptide that acts as a zonulin antagonist and tight-junction regulator, helping restore and maintain intestinal epithelial barrier function (reducing paracellular 'leaky gut' permeability). It was developed (as larazotide acetate, AT-1001 / INN-202) primarily for celiac disease as an adjunct to a gluten-free diet. It is not FDA-approved: a Phase 3 trial (CeDLara) in celiac disease was discontinued for futility, and the compound remains investigational with no approved human indication. The acetate salt form carries CAS 881851-50-9.
Studied uses
- investigational adjunct therapy for celiac disease (unapproved)
- intestinal barrier / tight-junction permeability research
- experimental study of 'leaky gut'-associated conditions (research only)
Identification
| CAS number | 258818-34-7 |
|---|---|
| Molecular formula | C32H55N9O10 |
| Sequence | GGVLVQPG |
| Typical dose | 0.25-0.5 mg taken orally three times daily before meals (clinical-trial dosing); acts locally in the gut lumen with minimal systemic absorption |
| Half-life | Minimal systemic exposure; acts locally in the gastrointestinal tract rather than via sustained plasma levels |
Safety
Not FDA-approved for any indication; clinical development for celiac disease did not demonstrate efficacy in Phase 3. Reported trial adverse effects were generally mild and gastrointestinal. Not a WADA-prohibited substance.
Vendors selling Larazotide
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Research
Coeliac disease is characterised by immune-mediated damage to the small intestine in response to dietary gluten in genetically predisposed individuals. Increased intestinal permeability is a central component to its pathophysiology.
source →Introduction Potassium-competitive acid blockers (P-CABs) have been empirically administered to treat non-esophageal eosinophilic gastrointestinal diseases, although their efficacy remains unproven.
source →Celiac disease is a chronic, immune-mediated enteropathy triggered by dietary gluten ingestion in a genetically susceptible individual.
source →Celiac disease (CeD) is a chronic autoimmune enteropathy triggered by gluten ingestion in genetically susceptible individuals carrying human leukocyte antigen (HLA)-DQ2 or HLA-DQ8 haplotypes.
source →Celiac disease (CeD) is a chronic autoimmune enteropathy triggered by dietary gluten in genetically predisposed individuals. Currently, a gluten-free diet (GFD) is the only available treatment, being effective in improving mucosal health and symptoms.
source →An open-label study to evaluate the safety, pharmacokinetics (PK), pharmacodynamics (PD), and efficacy of migalastat treatment in pediatric subjects 2 to \< 12 years of age with Fabry disease and with amenable GLA variants.
source →Multisystem inflammatory syndrome (MIS) is a severe disease that occurs weeks to months after acute infection with SARS-CoV-2, often occurring in children (MISC). Symptoms include high fever, rash, nausea, diarrhea, and abdominal pain.
source →Background/Objective : Larazotide acetate (LA) is a synthetic octapeptide under development as a therapeutic candidate for celiac disease, acting to reduce intestinal permeability and regulate tight junctions (TJs).
source →Gut barrier loss exacerbated gut microbiota dysbiosis by permitting pathogenic blooms, while gut microbiota dysbiosis caused the development of gut mucosal wounds by reducing mucus and breaking down epithelial tight junction.
source →Atopic dermatitis (AD) is a chronic inflammatory skin condition with evidence of defects in the barrier properties of the epidermis. Changes in the permeability properties of the tight junction have been reported in AD, and reversing this leaky tight junction may be a potential treatment for AD.
source →Celiac disease (CeD) is a chronic, immune-mediated enteropathy triggered by dietary gluten in genetically susceptible individuals, with environmental and epigenetic factors also contributing to its pathogenesis.
source →Pediatric gastroenterology is entering a pivotal phase marked by significant challenges and emerging opportunities in treating conditions like celiac disease (CeD), eosinophilic esophagitis (EoE), inflammatory bowel disease (IBD), and autoimmune hepatitis (AIH) pose significant clinical hurdles, but new therapeutic ave…
source →An Open-label Study to Evaluate the Safety and Pharmacokinetics of Migalastat HCl in Subjects with Fabry Disease and Amenable GLA Variants and Severe Renal Impairment (SRI) or End Stage Renal Disease (ESRD)
source →Study to compare the efficacy and safety of migalastat and enzyme replacement therapy (ERT) in male and female participants with Fabry disease who are currently receiving ERT and who have an alpha galactosidase-A (α Gal-A) mutation that is amenable to migalastat, based on the clinical trial human embryonic kidney cell…
source →This was a long-term, open-label study of migalastat (123 milligrams \[mg\] of migalastat \[equivalent to 150 mg of migalastat hydrochloride\]) (migalastat) in participants with Fabry disease who completed treatment in a previous monotherapy trial with migalastat.
source →The primary objective of this study was to compare the effect of migalastat (123 milligrams \[mg\] of migalastat \[equivalent to 150 mg of migalastat hydrochloride\]) (migalastat) versus placebo on kidney globotriaosylceramide (GL-3).
source →This study was conducted to evaluate the efficacy of multiple doses of larazotide acetate in preventing intestinal permeability changes induced by a 6- week gluten challenge in subjects with celiac disease.
source →Study to evaluate the safety, tolerability, pharmacokinetics, and pharmacodynamics of migalastat hydrochloride (HCl) (migalastat) in participants with Fabry disease.
source →To demonstrate the safety, tolerance and pharmacokinetics of multiple, oral doses of larazotide acetate.
source →