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
Db09043
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.

Pharmacology
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
Contraindications & Blackbox Warnings
Contraindications
Avoid life-threatening adverse drug events
Improve clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.
Learn more
Avoid life-threatening adverse drug events & improve clinical decision support.
Learn more
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.

TargetActionsOrganism
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
Adverseeffects
Improve decision support & research outcomes
With structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.
Learn more
Improve decision support & research outcomes with our structured adverse effects data.
Learn more
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.
DrugInteraction
AcarboseThe risk or severity of hypoglycemia can be increased when Acarbose is combined with Albiglutide.
AcebutololThe therapeutic efficacy of Albiglutide can be increased when used in combination with Acebutolol.
AcetazolamideThe therapeutic efficacy of Albiglutide can be increased when used in combination with Acetazolamide.
AcetohexamideAlbiglutide may increase the hypoglycemic activities of Acetohexamide.
Acetyl sulfisoxazoleThe therapeutic efficacy of Albiglutide can be increased when used in combination with Acetyl sulfisoxazole.
Acetylsalicylic acidThe risk or severity of hypoglycemia can be increased when Acetylsalicylic acid is combined with Albiglutide.
AlclometasoneThe risk or severity of hyperglycemia can be increased when Alclometasone is combined with Albiglutide.
AlogliptinThe risk or severity of hypoglycemia can be increased when Alogliptin is combined with Albiglutide.
AmcinonideThe risk or severity of hyperglycemia can be increased when Amcinonide is combined with Albiglutide.
Aminosalicylic acidAminosalicylic acid may increase the hypoglycemic activities of Albiglutide.
Interactions
Identify potential medication risks
Easily compare up to 40 drugs with our drug interaction checker.
Get severity rating, description, and management advice.
Learn more
Food Interactions
Not Available

Products

Products2
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
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
EperzanPowder, for solution30 mg / 0.5 mLSubcutaneousGlaxosmithkline IncNot applicableNot applicableCanada flag
EperzanInjection, powder, for solution30 mgSubcutaneousGlaxo Smith Kline Trading Services2021-01-122019-02-20EU flag
EperzanInjection, powder, for solution50 mgSubcutaneousGlaxo Smith Kline Trading Services2021-01-122019-02-20EU flag
EperzanPowder, for solution50 mg / 0.5 mLSubcutaneousGlaxosmithkline IncNot applicableNot applicableCanada flag
EperzanInjection, powder, for solution30 mgSubcutaneousGlaxo Smith Kline Trading Services2021-01-122019-02-20EU flag
EperzanInjection, powder, for solution50 mgSubcutaneousGlaxo Smith Kline Trading Services2021-01-122019-02-20EU flag
TanzeumInjection, powder, lyophilized, for solution30 mg/0.5mLSubcutaneousGlaxoSmithKline LLC2014-04-152020-09-30US flag
TanzeumInjection, powder, lyophilized, for solution50 mg/0.5mLSubcutaneousGlaxoSmithKline LLC2014-04-152020-08-31US flag

Categories

ATC Codes
A10BJ04 — Albiglutide
Drug Categories
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]
KEGG Drug
D08843
PubChem Substance
347910396
RxNav
1534763
Wikipedia
Albiglutide

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentDiabetes Mellitus1
4CompletedTreatmentType 2 Diabetes Mellitus1
4TerminatedTreatmentDiabetes Mellitus1
4TerminatedTreatmentType 2 Diabetes Mellitus2
3CompletedTreatmentDiabetes Mellitus1
3CompletedTreatmentType 2 Diabetes Mellitus12
3WithdrawnTreatmentType 2 Diabetes Mellitus2
2CompletedBasic ScienceCongestive Heart Failure (CHF)1
2CompletedTreatmentType 1 Diabetes Mellitus1
2CompletedTreatmentType 2 Diabetes Mellitus5

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Injection, powder, for solutionSubcutaneous30 MG
Injection, powder, for solutionSubcutaneous50 MG
Powder, for solutionSubcutaneous30 mg / 0.5 mL
Powder, for solutionSubcutaneous50 mg / 0.5 mL
Injection, powder, lyophilized, for solutionSubcutaneous30 mg/0.5mL
Injection, powder, lyophilized, for solutionSubcutaneous50 mg/0.5mL
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available

Targets

Drugtargets2
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
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]

Drug created at April 28, 2015 21:08 / Updated at October 26, 2021 21:40