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Identification
NameTeduglutide
Accession NumberDB08900
TypeBiotech
GroupsApproved
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. FDA approved on December 21, 2012.

Protein structureNo structure small
Related Articles
Protein chemical formulaC164H252N44O55S
Protein average weight3752.0 Da
Sequences
>Protein sequence for teduglutide
HGDGSFSDEMNTILDNLAARDFINWLIQTKITD
Download FASTA Format
Synonyms
(Gly2)glp-2
ALX 0600
ALX-0600
Gattex
Glucagon-like peptide ii (2-glycine) (human)
Gly(2)-glp-2
HGDGSFSDEMNTILDNLAARDFINWLIQTKITD
His-gly-asp-gly-ser-phe-ser-asp-glu-met-asn-thr-ile-leu-asp-asn-leu-ala-ala-arg-asp-phe-ile-asn-trp-leu-ile-gln-thr-lys-ile-thr-asp
Teduglutide [rDNA origin]
Teduglutide Recombinant
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Gattexinjection, powder, for solution5 mg/1subcutaneousNPS Pharmaceuticals2012-12-21Not applicableUs
GattexkitNPS Pharmaceuticals2012-12-21Not applicableUs
GattexkitNPS Pharmaceuticals2012-12-21Not applicableUs
Revestivekit; powder for solution5 mgsubcutaneousNps Pharma Holdings Limited2015-10-28Not applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
RevestiveNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNII7M19191IKG
CAS number197922-42-2
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available
Pharmacology
IndicationTreatment of short bowel syndrome (SBS), malabsorption associated with the removal of the intestine, in adults patients who are dependent on parenteral support.
PharmacodynamicsAn 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 actionTeduglutide 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.
Related Articles
AbsorptionThe 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; Cmax, 0.05 mg/kg SubQ, SBS patients = 36 ng/mL; AUC, 0.05 mg/kg SubQ, SBS patients = 0.15 µg•hr/mL; Teduglutide does not accumulate following multiple subcutaneous administrations.
Volume of distribution

Vd, healthy subjects = 103 mL/kg

Protein bindingNot Available
Metabolism

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 eliminationUrine
Half lifeTerminal half-life, healthy subjects = 2 hours; Terminal half-life, SBS patients = 1.3 hours
Clearance

Plasma clearance, healthy subjects = 123 mL/hr/kg;
This value indicates that teduglutide is primarily cleared by the kidney.

ToxicityThe 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%.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Injection, powder, for solutionsubcutaneous5 mg/1
Kit
Kit; powder for solutionsubcutaneous5 mg
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5789379 No1996-04-142016-04-14Us
US7056886 No2002-09-182022-09-18Us
US7847061 No2005-11-012025-11-01Us
US9060992 No2005-11-012025-11-01Us
Properties
StateLiquid
Experimental PropertiesNot Available
References
Synthesis ReferenceNot Available
General References
  1. 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 ]
  2. Semrad CE: The long road to a new short-bowel therapy: teduglutide for clinical use. Clin Gastroenterol Hepatol. 2013 Jul;11(7):824-5. doi: 10.1016/j.cgh.2013.03.030. Epub 2013 Apr 13. [PubMed:23591284 ]
  3. Jeppesen PB: Teduglutide, a novel glucagon-like peptide 2 analog, in the treatment of patients with short bowel syndrome. Therap Adv Gastroenterol. 2012 May;5(3):159-71. doi: 10.1177/1756283X11436318. [PubMed:22570676 ]
External Links
ATC CodesA16AX08
AHFS Codes
  • 56:92
PDB EntriesNot Available
FDA labelDownload (410 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AlprazolamThe serum concentration of Alprazolam can be increased when it is combined with Teduglutide.
BromazepamThe serum concentration of Bromazepam can be increased when it is combined with Teduglutide.
CamazepamThe serum concentration of Camazepam can be increased when it is combined with Teduglutide.
ChlordiazepoxideThe serum concentration of Chlordiazepoxide can be increased when it is combined with Teduglutide.
ChlormezanoneThe serum concentration of Chlormezanone can be increased when it is combined with Teduglutide.
CinolazepamThe serum concentration of Cinolazepam can be increased when it is combined with Teduglutide.
ClobazamThe serum concentration of Clobazam can be increased when it is combined with Teduglutide.
ClonazepamThe serum concentration of Clonazepam can be increased when it is combined with Teduglutide.
ClorazepateThe serum concentration of Clorazepate can be increased when it is combined with Teduglutide.
ClotiazepamThe serum concentration of Clotiazepam can be increased when it is combined with Teduglutide.
CloxazolamThe serum concentration of Cloxazolam can be increased when it is combined with Teduglutide.
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Teduglutide.
EstazolamThe serum concentration of Estazolam can be increased when it is combined with Teduglutide.
FludiazepamThe serum concentration of Fludiazepam can be increased when it is combined with Teduglutide.
FlunitrazepamThe serum concentration of Flunitrazepam can be increased when it is combined with Teduglutide.
FlurazepamThe serum concentration of Flurazepam can be increased when it is combined with Teduglutide.
HalazepamThe serum concentration of Halazepam can be increased when it is combined with Teduglutide.
KetazolamThe serum concentration of Ketazolam can be increased when it is combined with Teduglutide.
LorazepamThe serum concentration of Lorazepam can be increased when it is combined with Teduglutide.
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Teduglutide.
NitrazepamThe serum concentration of Nitrazepam can be increased when it is combined with Teduglutide.
OxazepamThe serum concentration of Oxazepam can be increased when it is combined with Teduglutide.
QuazepamThe serum concentration of Quazepam can be increased when it is combined with Teduglutide.
TemazepamThe serum concentration of Temazepam can be increased when it is combined with Teduglutide.
TofisopamThe serum concentration of Tofisopam can be increased when it is combined with Teduglutide.
TriazolamThe serum concentration of Triazolam can be increased when it is combined with Teduglutide.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
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:
GLP2R
Uniprot ID:
O95838
Molecular Weight:
63000.84 Da
References
  1. 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 ]
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Drug created on June 05, 2013 23:11 / Updated on May 31, 2016 02:13