Albiglutide

Identification

Summary

Albiglutide is a GLP-1 agonist used to manage type 2 diabetes mellitus.

Generic Name

Albiglutide

DrugBank Accession Number

DB09043

Background

Albiglutide is a glucagon-like peptide-1 agonist (GLP-1) biologic drug indicated in the treatment of type 2 diabetes. It is marketed under the brands Eperzan and Tanzeum by GSK (GlaxoSmithKline). It is a dipeptidyl peptidase-4-resistant glucagon-like peptide-1 dimer fused to human albumin. Albiglutide was approved on April 15, 2014 by the FDA.

Type

Biotech

Groups

Approved

Biologic Classification

Protein Based Therapies
Fusion proteins

Protein Structure

Protein Chemical Formula

C₃₂₃₂H₅₀₃₂N₈₆₄O₉₇₉S₄₁

Protein Average Weight

72970.0 Da

Sequences

> Albiglutide sequence
HGEGTFTSDVSSYLEGQAAKEFIAWLVKGRHGEGTFTSDVSSYLEGQAAKEFIAWLVKGR
DAHKSEVAHRFKDLGEENFKALVLIAFAQYLQQCPFEDHVKLVNEVTEFAKTCVADESAE
NCDKSLHTLFGDKLCTVATLRETYGEMADCCAKQEPERNECFLQHKDDNPNLPRLVRPEV
DVMCTAFHDNEETFLKKYLYEIARRHPYFYAPELLFFAKRYKAAFTECCQAADKAACLLP
KLDELRDEGKASSAKQRLKCASLQKFGERAFKAWAVARLSQRFPKAEFAEVSKLVTDLTK
VHTECCHGDLLECADDRADLAKYICENQDSISSKLKECCEKPLLEKSHCIAEVENDEMPA
DLPSLAADFVESKDVCKNYAEAKDVFLGMFLYEYARRHPDYSVVLLLRLAKTYETTLEKC
CAAADPHECYAKVFDEFKPLVEEPQNLIKQNCELFEQLGEYKFQNALLVRYTKKVPQVST
PTLVEVSRNLGKVGSKCCKHPEAKRMPCAEDYLSVVLNQLCVLHEKTPVSDRVTKCCTES
LVNRRPCFSALEVDETYVPKEFNAETFTFHADICTLSEKERQIKKQTALVELVKHKPKAT
KEQLKAVMDDFAAFVEKCCKADDKETCFAEEGKKLVAASQAALGL

Download FASTA Format

Synonyms

• Albiglutida
• Albiglutide

External IDs

• GSK-716155
• GSK716155

Pharmacology

Indication

Indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.

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Associated Conditions

• Type 2 Diabetes Mellitus

Contraindications & Blackbox Warnings

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Pharmacodynamics

Not Available

Mechanism of action

Albiglutide is an agonist of the GLP-1 (glucagon-like peptide 1) receptor and augments glucose-dependent insulin secretion. Albiglutide also slows gastric emptying.

Target	Actions	Organism
AGlucagon-like peptide 1 receptor	agonist	Humans

Absorption

Maximum concentrations of albiglutide were reached at 3 to 5 days post-dosing following a single 30mg dose. The mean peak concentration (Cmax) and mean area under the time-concentration curve (AUC) of albiglutide were 1.74 mcg/mL and 465 mcg.h/mL, respectively

Volume of distribution

11 L.

Protein binding

Not Available

Metabolism

Biotransformation studies have not been performed. Because albiglutide is an albumin fusion protein, it likely follows a metabolic pathway similar to native human serum albumin, which is catabolized primarily in the vascular endothelium.

Route of elimination

Not Available

Half-life

4-7 days.

Clearance

67 mL/h.

Adverse Effects

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Toxicity

-RISK OF THYROID C-CELL TUMORS -Albiglutide is contraindicated in patients with a personal or family history of MTC or in patients with Multiple Endocrine Neoplasia syndrome type 2 (MEN2). Routine serum calcitonin or thyroid ultrasound monitoring is of uncertain value in patients treated with Albiglutide.

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.

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drug	Interaction
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Acarbose	The risk or severity of hypoglycemia can be increased when Acarbose is combined with Albiglutide.
Acebutolol	The therapeutic efficacy of Albiglutide can be increased when used in combination with Acebutolol.
Acetazolamide	The therapeutic efficacy of Albiglutide can be increased when used in combination with Acetazolamide.
Acetohexamide	Albiglutide may increase the hypoglycemic activities of Acetohexamide.
Acetyl sulfisoxazole	The therapeutic efficacy of Albiglutide can be increased when used in combination with Acetyl sulfisoxazole.
Acetylsalicylic acid	The risk or severity of hypoglycemia can be increased when Acetylsalicylic acid is combined with Albiglutide.
Alclometasone	The risk or severity of hyperglycemia can be increased when Alclometasone is combined with Albiglutide.
Alogliptin	The risk or severity of hypoglycemia can be increased when Alogliptin is combined with Albiglutide.
Amcinonide	The risk or severity of hyperglycemia can be increased when Amcinonide is combined with Albiglutide.
Aminosalicylic acid	Aminosalicylic acid may increase the hypoglycemic activities of Albiglutide.

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Food Interactions

Not Available

Products

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Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Eperzan	Powder, for solution	50 mg / 0.5 mL	Subcutaneous	Glaxosmithkline Inc	Not applicable	Not applicable
Eperzan	Injection, powder, for solution	50 mg	Subcutaneous	Glaxo Smith Kline Trading Services	2021-01-12	2019-02-20
Eperzan	Injection, powder, for solution	50 mg	Subcutaneous	Glaxo Smith Kline Trading Services	2021-01-12	2019-02-20
Eperzan	Powder, for solution	30 mg / 0.5 mL	Subcutaneous	Glaxosmithkline Inc	Not applicable	Not applicable
Eperzan	Injection, powder, for solution	30 mg	Subcutaneous	Glaxo Smith Kline Trading Services	2021-01-12	2019-02-20
Eperzan	Injection, powder, for solution	30 mg	Subcutaneous	Glaxo Smith Kline Trading Services	2021-01-12	2019-02-20
Tanzeum	Injection, powder, lyophilized, for solution	30 mg/0.5mL	Subcutaneous	GlaxoSmithKline LLC	2014-04-15	2020-09-30
Tanzeum	Injection, powder, lyophilized, for solution	50 mg/0.5mL	Subcutaneous	GlaxoSmithKline LLC	2014-04-15	2020-08-31

Categories

ATC Codes

A10BJ04 — Albiglutide

• A10BJ — Glucagon-like peptide-1 (GLP-1) analogues
• A10B — BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
• A10 — DRUGS USED IN DIABETES
• A — ALIMENTARY TRACT AND METABOLISM

Drug Categories

• Alimentary Tract and Metabolism
• Blood Glucose Lowering Agents
• Drugs Used in Diabetes
• Gastrointestinal Hormones
• GLP-1 Agonists
• Glucagon-like peptide-1 (GLP-1) analogues
• Glucagon-Like Peptides
• Hormones
• Hormones, Hormone Substitutes, and Hormone Antagonists
• Incretins
• Proglucagon
• Recombinant Proteins

Chemical TaxonomyProvided by Classyfire

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

Affected organisms

• Humans and other mammals

Chemical Identifiers

UNII

5E7U48495E

CAS number

782500-75-8

References

General References

1. Trujillo JM, Nuffer W: Albiglutide: a new GLP-1 receptor agonist for the treatment of type 2 diabetes. Ann Pharmacother. 2014 Nov;48(11):1494-501. doi: 10.1177/1060028014545807. Epub 2014 Aug 18. [Article]

External Links

KEGG Drug

D08843

PubChem Substance

347910396

RxNav

1534763

Wikipedia

Albiglutide

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
4	Completed	Treatment	Diabetes Mellitus	1
4	Completed	Treatment	Type 2 Diabetes Mellitus	1
4	Terminated	Treatment	Diabetes Mellitus	1
4	Terminated	Treatment	Type 2 Diabetes Mellitus	2
3	Completed	Treatment	Diabetes Mellitus	1
3	Completed	Treatment	Type 2 Diabetes Mellitus	12
3	Withdrawn	Treatment	Type 2 Diabetes Mellitus	2
2	Completed	Basic Science	Congestive Heart Failure (CHF)	1
2	Completed	Treatment	Type 1 Diabetes Mellitus	1
2	Completed	Treatment	Type 2 Diabetes Mellitus	5

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage Forms

Form	Route	Strength
Injection, powder, for solution	Subcutaneous	30 MG
Injection, powder, for solution	Subcutaneous	50 MG
Powder, for solution	Subcutaneous	30 mg / 0.5 mL
Powder, for solution	Subcutaneous	50 mg / 0.5 mL
Injection, powder, lyophilized, for solution	Subcutaneous	30 mg/0.5mL
Injection, powder, lyophilized, for solution	Subcutaneous	50 mg/0.5mL

Prices

Not Available

Patents

Not Available

Properties

State

Solid

Experimental Properties

Not Available

Targets

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Details1. Glucagon-like peptide 1 receptor

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Agonist

General Function

Transmembrane signaling receptor activity

Specific Function

This is a receptor for glucagon-like peptide 1. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.

Gene Name

GLP1R

Uniprot ID

P43220

Uniprot Name

Glucagon-like peptide 1 receptor

Molecular Weight

53025.22 Da

References

1. Trujillo JM, Nuffer W: Albiglutide: a new GLP-1 receptor agonist for the treatment of type 2 diabetes. Ann Pharmacother. 2014 Nov;48(11):1494-501. doi: 10.1177/1060028014545807. Epub 2014 Aug 18. [Article]
2. Lorenz M, Lawson F, Owens D, Raccah D, Roy-Duval C, Lehmann A, Perfetti R, Blonde L: Differential effects of glucagon-like peptide-1 receptor agonists on heart rate. Cardiovasc Diabetol. 2017 Jan 13;16(1):6. doi: 10.1186/s12933-016-0490-6. [Article]
3. Htike ZZ, Zaccardi F, Papamargaritis D, Webb DR, Khunti K, Davies MJ: Efficacy and safety of glucagon-like peptide-1 receptor agonists in type 2 diabetes: A systematic review and mixed-treatment comparison analysis. Diabetes Obes Metab. 2017 Apr;19(4):524-536. doi: 10.1111/dom.12849. Epub 2017 Feb 17. [Article]
4. Nadkarni P, Chepurny OG, Holz GG: Regulation of glucose homeostasis by GLP-1. Prog Mol Biol Transl Sci. 2014;121:23-65. doi: 10.1016/B978-0-12-800101-1.00002-8. [Article]
5. Gallwitz B: Novel Therapeutic Approaches in Diabetes. Endocr Dev. 2016;31:43-56. doi: 10.1159/000439372. Epub 2016 Jan 19. [Article]
6. Rendell MS: Albiglutide: a unique GLP-1 receptor agonist. Expert Opin Biol Ther. 2016 Dec;16(12):1557-1569. doi: 10.1080/14712598.2016.1240780. Epub 2016 Oct 3. [Article]

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Drug created at April 28, 2015 21:08 / Updated at March 22, 2023 23:54