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. FDA approved on December 21, 2012.
|Protein chemical formula||C164H252N44O55S|
|Protein average weight||3752.0 Da|
>Protein sequence for teduglutide HGDGSFSDEMNTILDNLAARDFINWLIQTKITDDownload FASTA Format
|External IDs||Not Available|
|Product Ingredients||Not Available|
|Approved Prescription Products|
|Approved Generic Prescription Products||Not Available|
|Approved Over the Counter Products||Not Available|
|Unapproved/Other Products||Not Available|
|Brand mixtures||Not Available|
Treatment of short bowel syndrome (SBS), malabsorption associated with the removal of the intestine, in adults patients who are dependent on parenteral support.
An enhancement of gastrointestinal fluid absorption (750-1000 mL/day) was observed following daily administrations of teduglutide. An increase in villus height and crypt depth of the intestinal mucosa was also noted. A decrease in fecal weight has also been observed. Teduglutide does not prolong the QTc interval.
|Mechanism of action|
Teduglutide is an analog of naturally occurring human glucagon-like peptide-2 (GLP-2), a peptide secreted by L-cells of the distal intestine in response to meals. GLP-2 increases intestinal and portal blood flow and inhibit gastric acid secretion. Teduglutide binds to the glucagon-like peptide-2 receptors located in enteroendocrine cells, subepithelial myofibroblasts and enteric neurons of the submucosal and myenteric plexus. This causes the release of insulin-like growth factor (IGF)-1, nitric oxide and keratinocyte growth factor (KGF). These growth factors may contribute to the increase in crypt cell growth and surface area of the gastric mucosa. Ultimately, absorption through the intestine is enhanced.
The pharmacokinetic profile of teduglutide (when administered subcutaneously) is described by a one-compartment model with first order absorption in the abdomen, arm, and thigh. With escalating doses, teduglutide demonstrates linear pharmacokinetics.
Absolute bioavailability, SubQ = 88%;
Tmax, SubQ = 3-5 hours;
|Volume of distribution|
Vd, healthy subjects = 103 mL/kg
|Protein binding||Not Available|
Although a formal investigation has not been conducted, it is expected because teduglutide is a peptide-based drug, it will be degraded into smaller peptides and amino acids via catabolic pathways. The cytochrome P450 enzyme system is not involved in the metabolism of this drug.
|Route of elimination|
Terminal half-life, healthy subjects = 2 hours; Terminal half-life, SBS patients = 1.3 hours
Plasma clearance, healthy subjects = 123 mL/hr/kg; This value indicates that teduglutide is primarily cleared by the kidney.
The most common adverse reactions (≥ 10%) across all studies with GATTEX are abdominal pain, injection site reactions, nausea, headaches, abdominal distension, upper respiratory tract infection. In addition, vomiting and fluid overload were reported in the SBS studies (1 and 3) at rates ≥ 10%.
|Pharmacogenomic Effects/ADRs||Not Available|
|Food Interactions||Not Available|
|Synthesis Reference||Not Available|
|ATC Codes||A16AX08 — Teduglutide|
|PDB Entries||Not Available|
|FDA label||Download (410 KB)|
|Experimental Properties||Not Available|
|Super Class||Organic Acids|
|Class||Carboxylic Acids and Derivatives|
|Sub Class||Amino Acids, Peptides, and Analogues|
|Alternative Parents||Not Available|
|Molecular Framework||Not Available|
|External Descriptors||Not Available|
- Pharmacological action
- General Function:
- Glucagon receptor activity
- Specific Function:
- This is a receptor for glucagon-like peptide 2. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.
- Gene Name:
- Uniprot ID:
- Uniprot Name:
- Glucagon-like peptide 2 receptor
- Molecular Weight:
- 63000.84 Da
- Burness CB, McCormack PL: Teduglutide: a review of its use in the treatment of patients with short bowel syndrome. Drugs. 2013 Jun;73(9):935-47. doi: 10.1007/s40265-013-0070-y. [PubMed:23729002 ]