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

Sequences

>Protein sequence for teduglutide
HGDGSFSDEMNTILDNLAARDFINWLIQTKITD

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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

Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
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Gattex	Injection, powder, lyophilized, for solution	5 mg/0.5mL	Subcutaneous	Shire-NPS Pharmaceuticals, Inc.	2012-12-21	Not applicable
Revestive	Kit; Powder, for solution		Subcutaneous	Shire Pharmaceuticals Ireland Limited	2015-10-28	Not applicable
Revestive	Injection, powder, for solution	5 mg	Subcutaneous	Shire	2012-08-30	Not applicable

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Application Number

A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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Product Code

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Mixture Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End
Gattex	Teduglutide (5 mg/0.5mL) + Ethanol (0.7 mL/1mL)	Kit	Topical	Shire-NPS Pharmaceuticals, Inc.	2012-12-21	Not applicable
Gattex	Teduglutide (5 mg/0.5mL) + Ethanol (0.7 mL/1mL)	Kit	Topical	Shire-NPS Pharmaceuticals, Inc.	2012-12-21	Not applicable

Categories

UNII

7M19191IKG

CAS number

197922-42-2

Pharmacology

Indication

Treatment of short bowel syndrome (SBS), malabsorption associated with the removal of the intestine, in adults patients who are dependent on parenteral support.

Associated Conditions

Short Bowel Syndrome (SBS)

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

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Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

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Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

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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.

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%.

Affected organisms

Humans and other mammals

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
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Abacavir	Abacavir may decrease the excretion rate of Teduglutide which could result in a higher serum level.
Acarbose	Acarbose 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.
Acetazolamide	Acetazolamide may increase the excretion rate of Teduglutide which could result in a lower serum level and potentially a reduction in efficacy.
Acetylsalicylic acid	Acetylsalicylic acid may decrease the excretion rate of Teduglutide which could result in a higher serum level.
Aclidinium	Aclidinium may decrease the excretion rate of Teduglutide which could result in a higher serum level.
Acrivastine	Teduglutide may decrease the excretion rate of Acrivastine which could result in a higher serum level.
Acyclovir	Acyclovir may decrease the excretion rate of Teduglutide which could result in a higher serum level.

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Extended Description

Extended description of the mechanism of action and particular properties of each drug interaction.

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Severity

A severity rating for each drug interaction, from minor to major.

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Evidence Level

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Action

An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions

Not Available

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. [PubMed:23729002]
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]
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

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

ATC Codes

A16AX08 — Teduglutide

AHFS Codes

56:92.00 — Miscellaneous GI Drugs

FDA label

Download (410 KB)

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
1	Completed	Not Available	Healthy Volunteers	1
1	Completed	Not Available	Pharmacokinetics and Safety of Elevated Doses	1
1	Completed	Not Available	Impaired kidney function	1
1	Completed	Other	Hepatic Impairment	1
1	Completed	Treatment	Healthy Volunteers	1
1	Recruiting	Treatment	Postoperative Fistula	1
2	Completed	Treatment	Crohn's Disease (CD)	2
2	Not Yet Recruiting	Treatment	Severe Acute Malnutrition	1
2	Recruiting	Treatment	Human Immunodeficiency Virus (HIV)	1
2, 3	Not Yet Recruiting	Basic Science	Hyperlipidemias	1
2, 3	Recruiting	Basic Science	Hyperlipidemias	3
3	Active Not Recruiting	Treatment	Short Bowel Syndrome (SBS)	4
3	Completed	Treatment	Short Bowel Syndrome (SBS)	9
3	Enrolling by Invitation	Treatment	Short Bowel Syndrome (SBS)	1
3	Not Yet Recruiting	Treatment	Ileostomy - Stoma	1
3	Recruiting	Treatment	Short Bowel Syndrome (SBS)	1
4	Completed	Treatment	Short Bowel Syndrome (SBS)	1
4	Recruiting	Treatment	Short Bowel Syndrome (SBS)	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage forms

Form	Route	Strength
Injection, powder, lyophilized, for solution	Subcutaneous	5 mg/0.5mL
Kit	Topical
Injection, powder, for solution	Subcutaneous	5 mg
Kit; powder, for solution	Subcutaneous

Prices

Not Available

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)
Unlock Additional Data
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

Additional Data Available

Filed On

The date on which a patent was filed with the relevant government.

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Properties

State: Liquid
Experimental Properties: Not Available

Taxonomy

Description: Not Available
Kingdom: Organic Compounds
Super Class: Organic Acids
Class: Carboxylic Acids and Derivatives
Sub Class: Amino Acids, Peptides, and Analogues
Direct Parent: Peptides
Alternative Parents: Not Available
Substituents: Not Available
Molecular Framework: Not Available
External Descriptors: Not Available

Targets

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. [PubMed:23729002]

Drug created on June 05, 2013 23:11 / Updated on December 08, 2019 20:10