DescriptionCurator's Comment: description was created based on several sources, including
http://www.ncbi.nlm.nih.gov/pubmed/?term=24068167;
http://www.ncbi.nlm.nih.gov/pubmed/23729002
Curator's Comment: description was created based on several sources, including
http://www.ncbi.nlm.nih.gov/pubmed/?term=24068167;
http://www.ncbi.nlm.nih.gov/pubmed/23729002
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
Sources: http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Public_assessment_report/human/002345/WC500132928.pdf
Curator's Comment: Samples of cerebrospinal fluid (CSF) and plasma were collected from rats administered teduglutide s.c. at a single dose of 3 or 10 mg/kg. The CSF teduglutide concentration did not exceed 5% of the peak concentrations in plasma. The results indicated that teduglutide did not readily penetrate the blood-brain barrier.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: O95838 Gene ID: 9340.0 Gene Symbol: GLP2R Target Organism: Homo sapiens (Human) |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | GATTEX KIT Approved UseGATTEX® (teduglutide [rDNA origin]) for injection is a glucagon-like peptide-2 (GLP-2) analog indicated for the treatment of adult patients with Short Bowel Syndrome (SBS) who are dependent on parenteral support Launch Date2012 |
PubMed
Title | Date | PubMed |
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The long road to a new short-bowel therapy: teduglutide for clinical use. | 2013 Jul |
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Teduglutide: a review of its use in the treatment of patients with short bowel syndrome. | 2013 Jun |
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Efficacy and safety of crofelemer for noninfectious diarrhea in HIV-seropositive individuals (ADVENT trial): a randomized, double-blind, placebo-controlled, two-stage study. | 2013 Nov-Dec |
Sample Use Guides
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
Sources: http://www.ncbi.nlm.nih.gov/pubmed/?term=24068167
Proliferation was assessed using a colorimetric MTS assay after Caco-2 cells were incubated with 0 to 1000 nM teduglutide.
Substance Class |
Protein
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Sequence Type | COMPLETE |
Record UNII |
7M19191IKG
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Validated (UNII)
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EU-Orphan Drug |
EU/3/01/077
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WHO-ATC |
A16AX08
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FDA ORPHAN DRUG |
784820
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NDF-RT |
N0000190992
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EMA ASSESSMENT REPORTS |
REVESTIVE (AUTHORIZED: MALABSORPTION DISEASES)
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FDA ORPHAN DRUG |
126999
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NCI_THESAURUS |
C548
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WHO-VATC |
QA16AX08
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4718
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m10518
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CHEMBL2104987
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DB08900
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C66582
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N0000175140
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PRIMARY | Glucagon-Like Peptide 2 [Chemical/Ingredient] | ||
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100000124173
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1364468
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7M19191IKG
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TEDUGLUTIDE
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N0000190990
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8337
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197922-42-2
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N0000175452
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7M19191IKG
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PP-09
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SUB31909
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DTXSID501027767
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ACTIVE MOIETY |
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Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Molecular Formula | CHEMICAL |
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Biological Half-life | PHARMACOKINETIC |
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MOL_WEIGHT:NUMBER(CALCULATED) | CHEMICAL |
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