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Intrinsic Factor has the potential to revolutionize drug delivery. May improve protein stability, facilitate oral absorption and 'Precision Liver Targeting'. *

IF's Unique Properties

Protect B12 from intestinal degradation.

Present B12 to  absorption receptors.

IF's unique role can be harnessed to protect protein therapeutics.

Gastrointestinal Gauntlet

Protein drugs like insulin are damaged in the gastrointestinal tract and cannot be given orally and retain efficacy. Protease enzymes like trypsin and chymotrypsin are designed to break down proteins and prepare them for absorption.

Intestinal Enzymes & IF

IF binds to B12 and protects it from being destroyed by trypsin and chymotrypsin in the intestine. That is the reason IF is designed to be resistant to these enzymes. [1]

IF Protects Proteins in GI tract

IF protects B12 and a published in-vitro study has shown that IF may protect protein drugs that are attached to B12 as well. This could be a 'game-changer' for certain drugs.[1]

IF Protects Proteins in Bloodstream

An in-vitro study also showed that IF has the potential to protect protein drugs in the circulation against a powerful protein degrading enzyme called meprin, which could extend the activity of injected protein drugs. [1]

stabilizes & transports

IF, which is shaped like a donut, pulls most of the B12 molecule into the 'donut hole' and this protects the more vulnerable parts of the B12 molecule from destruction on its long journey (20 feet) to the receptors. [2]

EXEN 4 - B12 Complex

EXEN 4-B12 image courtesy Prof. Robert Doyle, Syracuse University
Key to the Receptor 'Lock'

Vitamin B12 is the only nutrient absorbed into the body via a specific receptor.

membrane receptor

A receptor is a protein that straddles a cell membrane and is designed to recognize and transport specific molecules across the membrane into the cell. [3]

key to b12 receptors

Vitamin B12 by itself is not recognized by the B12 receptor. It needs to be attached to IF. The IF-B12 complex is the 'key' to the lock that absorbs B12. [3]

conjugating b12

Conjugating (joining) B12 to a protein drug allows the IF to become associated with the drug and creating a 3-member complex that could be recognized by B12-IF receptors and potentially gain access to the body via the oral route. [4-8]

precision Pharmaceutical targeting

Xeragenx's IF (rh-IF) has also been shown in a pre-clinical study to be recognized by specific multi-ligand endocytic mannose receptors (CD206) of activated macrophages and can be used to target specific organs like liver and lung.[9,10]

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