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Description

Teduglutide is a glucagon-like peptide-2 (GLP-2) analogue. It is made up of 33 amino acids and is manufactured using a strain of Escherichia coli modified by recombinant DNA technology. Teduglutide differs from GLP-2 by one amino acid (alanine is substituted by glycine). The significance of this substitution is that teduglutide is longer acting than endogenous GLP-2 as it is more resistant to proteolysis from dipeptidyl peptidase-4. GLP-2 is known to increase intestinal and portal blood flow, and inhibit gastric acid secretion. Teduglutide binds to the glucagon-like peptide-2 receptors located in intestinal subpopulations of enteroendocrine cells, subepithelial myofibroblasts and enteric neurons of the submucosal and myenteric plexus. Activation of these receptors results in the local release of multiple mediators including insulin-like growth factor (IGF)-1, nitric oxide and keratinocyte growth factor (KGF). FDA approved on December 21, 2012. In Europe it has been granted orphan drug status and is marketed under the brand Revestive by Nycomed. It works by promoting mucosal growth and possibly restoring gastric emptying and secretion.

CNS Activity

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
GATTEX KIT

PubMed

Sample Use Guides

In Vivo Use Guide
The recommended once daily dose of GATTEX (teduglutide [rDNA origin]) is 0.05 mg/kg. Administer by subcutaneous injection; alternate sites between 1 of the 4 adjusted, and GATTEX treatment reassessed quadrants of the abdomen, or into alternating thighs or alternating arms.
Route of Administration: Other
In Vitro Use Guide
Proliferation was assessed using a colorimetric MTS assay after Caco-2 cells were incubated with 0 to 1000 nM teduglutide.
Substance Class Protein
Protein Sub Type
Sequence Type COMPLETE
Record UNII
7M19191IKG
Record Status Validated (UNII)
Record Version
Subunit 0