Game-Changing "Leaky Gut" Treatment (Larazotide Acetate) will soon be available

sometexan84

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It's been 5 yrs since @Waverunner posted about this - Mayo Clinic: Is Larazotide Acetate the Answer to Leaky Gut/Celiac Disease?

And it's just now nearing completion, undergoing Phase III trials now.
https://www.beyondceliac.org/research/drugdevelopment/drug-development-pipeline/
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Larazotide Acetate drastically improves intestinal barrier integrity. It's a zonulin antagonist.

Increased serum zonulin levels are accompanied by a leaky intestinal barrier, dysbiosis and inflammation. Zonulin is a fairly new discovery, and it appears can be used as a biomarker for leaky gut & intestinal permeability testing.

Ref 1. Targeting zonulin and intestinal epithelial barrier function to prevent onset of arthritis
Ref 2. All disease begins in the (leaky) gut: role of zonulin-mediated gut permeability in the pathogenesis of some chronic inflammatory diseases

John Temperato (9 Meters Biopharma) says...
He expects to perform an interim analysis by mid-2021 and a final analysis at the end of that year. “We want to petition the FDA for conditional approval.” The waiver helps support that.
 

Waverunner

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@sometexan84 Thanks for posting this. It's been a while. I hope the trial is successful and I hope that they get market access within one or two years following the trial.
 

mitoMAN

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I am about to place an order for custom synthesis of it. Its already available for research purposes.

Anyone already calculated the daily dosages noted down?

@Hip (sorry for abusing you on calculations)

I well let you guys know once I got a price quote and possibly ordered it and had i 3rd party lab checked to confirm identity. Could indeed help out our leaky gut!!
(I have pretty high Zonulin for example)
 
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mitoMAN

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According to this study:
https://pubmed.ncbi.nlm.nih.gov/25683116/

We assessed larazotide acetate 0.5, 1, or 2 mg three times daily to relieve ongoing symptoms in 342 adults with CeD who had been on a GFD for ≥12 months and maintained their current GFD during the study.
Interestingly only 0.5mg 3x daily showed the hoped for benefits (not 1 - 2mg..)

Larazotide acetate is a novel, locally acting non-systemic, synthetic 8-amino acid oral peptide...
Randomization was 1:1:1:1 to larazotide acetate 0·5mg, 1mg, or 2mg capsules, or placebo in identical capsules.

Following the 4-week placebo run-in, study drugs were self-administered three times daily (TID), 15 minutes before meals.

Symptomatic improvement with larazotide acetate 0·5mg was evident by treatment week 2 and was sustained over the 12-week treatment period.
So this one is not for injection but actually oral intake. I need to figure out if it is gastric stable or needs to be taken with gastric juice pH resistant capsules.

Safety Profile seems good as well!
In four prior clinical trials, larazotide acetate demonstrated a safety profile comparable to placebo.14–16 In initial clinical trials utilizing gluten challenge, larazotide acetate prevented gluten-induced symptoms and blunted increases in anti-tTG antibodies, INF-gamma, and intestinal permeability

Their explanation as to why higher dosage is not necessary more successful:
This inversedose effect is not unique to larazotide acetate and has been seen for other minimally or nonabsorbed oral peptides.33 Why higher doses appear to be less effective is unclear, but may involve peptide aggregation at higher doses, reducing activity in vivo.
 
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Frunobulax

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LG comes from shitty diet. We eat tons of stuff that our ancestors never ate, especially grains, with plenty of antinutrients (Lectins especially) that make us sick. And instead of figuring out what in the diet is shitty (fix the root cause), we're hoping for a wonder pill to fix our troubles (control symptoms)? I'm very bearish on this one.

If you have LG, eat paleo and restrict carbs. Your gut will heal, and with any luck you'll see a lot of improvement in other areas. No need at all for more chemistry with god knows which side effects.
 

mitoMAN

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I am on strict diet for years. It's not about Gluten it's about decreasing Zonulin when these symptoms last after patients have been on strict diet for years. And thus high inflammation as cause from Zonulin buildup that is not reduced by a healthy diet.
(I haven't eaten gluten for 7 years and Fodmap for 3 including any other dietary measures)

im happy your approach is working for you tho.
 

JES

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LG comes from shitty diet. We eat tons of stuff that our ancestors never ate, especially grains, with plenty of antinutrients (Lectins especially) that make us sick. And instead of figuring out what in the diet is shitty (fix the root cause), we're hoping for a wonder pill to fix our troubles (control symptoms)? I'm very bearish on this one.

If you have LG, eat paleo and restrict carbs. Your gut will heal, and with any luck you'll see a lot of improvement in other areas. No need at all for more chemistry with god knows which side effects.
Not good enough. Most of us have tried all kinds of things with diets without any huge jump in health. What we need is better and more research and the involves chemistry, just as our bodies are one big chemical factory.
 

Frunobulax

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Not good enough. Most of us have tried all kinds of things with diets without any huge jump in health. What we need is better and more research and the involves chemistry, just as our bodies are one big chemical factory.
I agree, partially. The key is to research the root causes: Why do we get LG in the first place, and will eliminating the root causes fix the disease? Looking for new drugs is only a small part of that, unfortunately in our pharma-driven society we spend 95% of research on drugs and 5% on etiology, root causes and prevention.

As for treatment, a lot of people I know personally were able to fix LG with a paleo/low carb diet. But this doesn't mean that their health issues will magically go away, as LG is only one of many issues leading to our maladities. And yes, we do need more research here.

The problem of course is that with various other issues (histamine intolerance/MCAS, allergies, oxalates, fodmaps, salicylates and whatnot) it can become very challenging to find something that we can eat at all. In these cases, a drug may be useful. But that's a small minority of all LG patients (though a lot of us ME sufferers might fall into this category).
 

Frunobulax

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I am on strict diet for years. It's not about Gluten it's about decreasing Zonulin when these symptoms last after patients have been on strict diet for years.
LG has almost nothing to do with Gluten, which is is only one of a gazillion of antinutrients. With LG you'll have to avoid all lectins, and strictly reduce omega-6 fats, sugar and carbs. But this is only a part of the solution. Unfortunately there is no twitter-compatible method to fix your gut microbiome. Heavy books have been written on that, with good reason.

Just as gardening is a bit more complicated than "put seeds in ground, water occasionally" -- it's a good start, no more and no less. The gut microbiome is like a garden that needs seeds, water, fertilizer, occasional weeding, good soil and the right amount of sun. A functional garden won't detoriate in a short time, but it's another story if you've got a wasteland. If all you've got left is weeds, you'll need a lot of effort to make this into a garden. Fixing the gut microbiome needs a LOT more than a gluten free diet.
 

junkcrap50

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If you want to join me on the order and 3rd Party lab testing the source. Feel Free to PM me
I will consider this and check my finances.

Would you divide up one order of 1gram of larazotide acetate, since the dose is so small? How would you divide it? (I guess it's easier since it's taken orally, right? And doesn't need to be sterile for injection.) Or would each person need to order $450 worth at a time?

But I've had good success with gluten free and dairy free diet. But studies of this treatment showed it was better than gluten free diet alone. So it's intriguing.
 

mitoMAN

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Its worth to consider if your ZONULIN is stll high.

We would share 1 gram with maybe 5 Persons I think! Everyone only needs 45mg per Month.
The lab test would cost 300€ tho. Again shared by everyone involvd of course.

I would suggest buying a fine miligram scale and then buying a very tiny spoon that holds about 0.5mg.
Amazon is your friend for that : )
 
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I PM'd Mito and I'm interesting in splitting it. However, I'm curious how hard it would be to get the dosing right. I've done other peptides like BPC-157 before, but I feel those are easier to dose. I haven't done any chemistry in the last 15 years. Can someone more knowledgeable please tell me how hard it would be for a rank amateur to split something like Larazotide Acetate and get the dosing correct considering it's such a minute amount? :)
 

mitoMAN

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its pretty easy. Especiall if you constitute it with BAC. We just have to do another stability testing then to see how stable it is in water without degradation.
Which can be done at my 3rd Party lab via HPLC.