Teduglutide

Identification

Summary

Teduglutide is a glucagon-like peptide-2 (GLP-2) analog used to treat patients with Short Bowel Syndrome (SBS) who require parenteral nutritional support.

Brand Names

Gattex, Revestive

Generic Name

Teduglutide

DrugBank Accession Number

DB08900

Background

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.

Type

Biotech

Groups

Approved

Biologic Classification

Protein Based Therapies
Other protein based therapies

Protein Chemical Formula

C₁₆₄H₂₅₂N₄₄O₅₅S

Protein Average Weight

3752.0 Da

Sequences

>Protein sequence for teduglutide
HGDGSFSDEMNTILDNLAARDFINWLIQTKITD

Download FASTA Format

Synonyms

(Gly2)GLP-2
Glucagon-like peptide II (2-glycine) (human)
Gly(2)-GLP-2
Teduglutida
Teduglutide
Teduglutide [rDNA origin]
Teduglutide Recombinant

External IDs

ALX 0600
ALX-0600

Poor quality drug data slowing you down?

Unlock 38% more drug discovery time and eliminate decision-making doubts with this one-stop guide to quality drug data.

Download eBook

Poor quality drug data slowing you down?

Download eBook

Pharmacology

Indication

Teduglutide is indicated for the treatment of adults and pediatric patients 1 year of age and older with Short Bowel Syndrome (SBS) who are dependent on parenteral support.⁴

Reduce drug development failure rates

Build, train, & validate machine-learning models
with evidence-based and structured datasets.

See how

Build, train, & validate predictive machine-learning models with structured datasets.

See how

Associated Conditions

Indication Type	Indication	Combined Product Details	Approval Level	Age Group	Patient Characteristics	Dose Form
Management of	Short bowel syndrome		••••••••••••	•••••• •••••••••	•••••••••• •••••••••	•••••••••

Contraindications & Blackbox Warnings

Prevent Adverse Drug Events Today

Tap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.

Learn more

Avoid life-threatening adverse drug events with our Clinical API

Learn more

Pharmacodynamics

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.

Target	Actions	Organism
AGlucagon-like peptide 2 receptor	agonist	Humans

Absorption

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;
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 binding

Not 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 elimination

Urine

Half-life

Terminal 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.

Adverse Effects

Improve decision support & research outcomes

With structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!

See the data

Improve decision support & research outcomes with our structured adverse effects data.

See a data sample

Toxicity

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%.

Pathways

Not Available

Pharmacogenomic Effects/ADRs

Not Available

Interactions

Drug Interactions

This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.

Drug	Interaction
Integrate drug-drug interactions in your software
1,2-Benzodiazepine	The serum concentration of 1,2-Benzodiazepine can be increased when it is combined with Teduglutide.
Abacavir	Abacavir may decrease the excretion rate of Teduglutide which could result in a higher serum level.
Aceclofenac	Aceclofenac may decrease the excretion rate of Teduglutide which could result in a higher serum level.
Acemetacin	Acemetacin may decrease the excretion rate of Teduglutide which could result in a higher serum level.
Acetaminophen	Acetaminophen may decrease the excretion rate of Teduglutide which could result in a higher serum level.

Food Interactions

No interactions found.

Products

Drug product information from 10+ global regions

Our datasets provide approved product information including:
dosage, form, labeller, route of administration, and marketing period.

Access now

Access drug product information from over 10 global regions.

Access now

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Gattex	Injection, powder, lyophilized, for solution	5 mg/0.5mL	Subcutaneous	Takeda Pharmaceuticals America, Inc.	2012-12-21	Not applicable
Revestive	Injection, powder, for solution	5 mg	Subcutaneous	Takeda Pharmaceuticals International Ag Ireland Branch	2016-09-08	Not applicable
Revestive	Injection, powder, for solution	1.25 mg	Subcutaneous	Takeda Pharmaceuticals International Ag Ireland Branch	2020-12-22	Not applicable
Revestive	Kit; Powder, for solution	5 mg / vial	Subcutaneous	Takeda	2015-10-28	Not applicable
Revestive	Injection, powder, for solution	5 mg	Subcutaneous	Takeda Pharmaceuticals International Ag Ireland Branch	2020-12-22	Not applicable

Mixture Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End	Region	Image
Gattex	Teduglutide (5 mg/0.5mL) + Ethanol (0.7 mL/1mL)	Injection, powder, lyophilized, for solution; Kit	Subcutaneous; Topical	Takeda Pharmaceuticals America, Inc.	2012-12-21	Not applicable
Gattex	Teduglutide (5 mg/0.5mL) + Ethanol (0.7 mL/1mL)	Injection, powder, lyophilized, for solution; Kit	Subcutaneous; Topical	Takeda Pharmaceuticals America, Inc.	2012-12-21	Not applicable

Chemical Identifiers

UNII: 7M19191IKG
CAS number: 197922-42-2

References

General References

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. [Article]
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. [Article]
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. [Article]
FDA Approved Drug Products: Gattex (teduglutide) for subcutaneous injection [Link]

External Links

KEGG Drug: D06053
KEGG Compound: C16049
PubChem Substance: 347910383
RxNav: 1364468
ChEBI: 72305
ChEMBL: CHEMBL2104987
RxList: RxList Drug Page
Drugs.com: Drugs.com Drug Page
Wikipedia: Teduglutide

FDA label

Download (410 KB)

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
4	Completed	Treatment	Short Bowel Syndrome (SBS)	2
3	Completed	Treatment	Short Bowel Syndrome (SBS)	16
3	Withdrawn	Treatment	Stoma Ileostomy	1
2	Completed	Treatment	Acute Malnutrition, Severe Acute Malnutrition	1
2	Completed	Treatment	Crohn's Disease (CD)	2

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage Forms

Form	Route	Strength
Injection, powder, lyophilized, for solution	Subcutaneous	5 mg/0.5mL
Injection, powder, lyophilized, for solution; kit	Subcutaneous; Topical
Injection, powder, for solution	Parenteral; Subcutaneous	1.25 MG
Injection, powder, for solution	Parenteral; Subcutaneous	5 MG
Injection, powder, for solution	Subcutaneous	1.25 mg
Kit; powder, for solution	Subcutaneous	5 mg / vial
Injection, powder, for solution	Subcutaneous	5 mg

Prices

Not Available

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)
US5789379	Yes	1998-08-04	2020-10-14
US7056886	Yes	2006-06-06	2023-03-18
US7847061	Yes	2010-12-07	2026-05-01
US9060992	Yes	2015-06-23	2026-05-01
US9555079	Yes	2017-01-31	2026-05-01
US9545434	Yes	2017-01-17	2026-05-01
US9539310	Yes	2017-01-10	2026-05-01
US9545435	Yes	2017-01-17	2026-05-01
US9592273	Yes	2017-03-14	2026-05-01
US9592274	Yes	2017-03-14	2026-05-01
US9572867	Yes	2017-02-21	2026-05-01
US9987334	Yes	2018-06-05	2026-05-01
US9968658	Yes	2018-05-15	2026-05-01
US9981016	Yes	2018-05-29	2026-05-01
US9974837	Yes	2018-05-22	2026-05-01
US9974835	Yes	2018-05-22	2026-05-01
US9981014	Yes	2018-05-29	2026-05-01
US9968656	Yes	2018-05-15	2026-05-01
US9968655	Yes	2018-05-15	2026-05-01
US9987335	Yes	2018-06-05	2026-05-01
US9993528	Yes	2018-06-12	2026-05-01

Properties

State: Liquid
Experimental Properties: Not Available

Targets

Build, predict & validate machine-learning models

Use our structured and evidence-based datasets to unlock new
insights and accelerate drug research.

Learn more

Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.

Learn more

Details1. Glucagon-like peptide 2 receptor

Kind: Protein
Organism: Humans
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
Uniprot Name: Glucagon-like peptide 2 receptor
Molecular Weight: 63000.84 Da

References

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. [Article]

Drug created at June 06, 2013 05:11 / Updated at June 03, 2022 07:24

Teduglutide

Identification

Pharmacology

Interactions

Products

Categories

Chemical Identifiers

References

Clinical Trials

Pharmacoeconomics

Properties

Targets

References