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Description
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

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.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: O95838
Gene ID: 9340.0
Gene Symbol: GLP2R
Target Organism: Homo sapiens (Human)
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
GATTEX KIT

Approved Use

GATTEX® (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 Date

2012
PubMed

PubMed

TitleDatePubMed
Teduglutide: a review of its use in the treatment of patients with short bowel syndrome.
2013 Jun
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
Patents

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
Proliferation was assessed using a colorimetric MTS assay after Caco-2 cells were incubated with 0 to 1000 nM teduglutide.
Name Type Language
TEDUGLUTIDE
DASH   INN   MART.   MI   USAN   VANDF   WHO-DD  
INN   USAN  
Official Name English
ALX 0600 (2-GLYCINE-1-33-GLUCAGON-LIKE PEPTIDE II (HUMAN))
Common Name English
TEDUGLUTIDE [USAN]
Common Name English
TEDUGLUTIDE [MI]
Common Name English
2-GLYCINE-1-33-GLUCAGON-LIKE PEPTIDE II (HUMAN)
Common Name English
ALX-0600
Code English
TEDUGLUTIDE [JAN]
Common Name English
TEDUGLUTIDE (RDNA ORIGIN)
Common Name English
ALX 0600
Code English
TEDUGLUTIDE RECOMBINANT [ORANGE BOOK]
Common Name English
Teduglutide [WHO-DD]
Common Name English
GATTEX
Brand Name English
TEDUGLUTIDE [MART.]
Common Name English
teduglutide [INN]
Common Name English
REVESTIVE
Brand Name English
TEDUGLUTIDE RECOMBINANT
ORANGE BOOK  
Common Name English
TEDUGLUTIDE [VANDF]
Common Name English
Classification Tree Code System Code
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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Code System Code Type Description
DRUG CENTRAL
4718
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PRIMARY
MERCK INDEX
m10518
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PRIMARY Merck Index
ChEMBL
CHEMBL2104987
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PRIMARY
DRUG BANK
DB08900
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PRIMARY
NCI_THESAURUS
C66582
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PRIMARY
NDF-RT
N0000175140
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PRIMARY Glucagon-Like Peptide 2 [Chemical/Ingredient]
SMS_ID
100000124173
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PRIMARY
MESH
C494910
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PRIMARY
CHEBI
72305
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PRIMARY
RXCUI
1364468
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PRIMARY RxNorm
DAILYMED
7M19191IKG
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PRIMARY
WIKIPEDIA
TEDUGLUTIDE
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PRIMARY
NDF-RT
N0000190990
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PRIMARY Glucagon-like Peptide-2 (GLP-2) Agonists [MoA]
HSDB
8337
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PRIMARY
CAS
197922-42-2
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PRIMARY
NDF-RT
N0000175452
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PRIMARY Analogs/Derivatives [Chemical/Ingredient]
FDA UNII
7M19191IKG
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PRIMARY
USAN
PP-09
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PRIMARY
EVMPD
SUB31909
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PRIMARY
INN
8444
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PRIMARY
IUPHAR
7049
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PRIMARY
EPA CompTox
DTXSID501027767
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PRIMARY