Identification

Name
Albiglutide
Accession Number
DB09043  (DB05162)
Type
Biotech
Groups
Approved
Biologic Classification
Protein Based Therapies
Fusion proteins
Description

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.

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
External IDs
GSK-716155 / GSK716155
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
EperzanPowder, for solution30 mgSubcutaneousGlaxosmithkline IncNot applicableNot applicableCanada
EperzanPowder, for solution50 mgSubcutaneousGlaxosmithkline IncNot applicableNot applicableCanada
TanzeumInjection, powder, lyophilized, for solution50 mg/0.5mLSubcutaneousGlaxoSmithKline LLC2014-04-152020-08-31Us
TanzeumInjection, powder, lyophilized, for solution30 mg/0.5mLSubcutaneousGlaxoSmithKline LLC2014-04-152020-09-30Us
Categories
UNII
5E7U48495E
CAS number
782500-75-8

Pharmacology

Indication

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

Associated Conditions
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
Human
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.

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.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
2,4-thiazolidinedioneThe risk or severity of hypoglycemia can be increased when Albiglutide is combined with 2,4-thiazolidinedione.
5-(2-methylpiperazine-1-sulfonyl)isoquinolineThe therapeutic efficacy of Albiglutide can be increased when used in combination with 5-(2-methylpiperazine-1-sulfonyl)isoquinoline.
AcarboseThe risk or severity of hypoglycemia can be increased when Acarbose is combined with Albiglutide.
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 acidAcetylsalicylic acid may increase the hypoglycemic activities of Albiglutide.
AgmatineThe risk or severity of hypoglycemia can be increased when Agmatine is combined with Albiglutide.
AICA ribonucleotideThe risk or severity of hypoglycemia can be increased when AICA ribonucleotide is combined with Albiglutide.
AlaproclateThe risk or severity of hypoglycemia can be increased when Alaproclate is combined with Albiglutide.
Food Interactions
Not Available

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. [PubMed:25136065]
External Links
KEGG Drug
D08843
PubChem Substance
347910396
Wikipedia
Albiglutide
ATC Codes
A10BX13 — Albiglutide
AHFS Codes
  • 68:20.92 — Miscellaneous Antidiabetic Agents

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedBasic ScienceHealthy Volunteers / Type 2 Diabetes Mellitus1
1CompletedOtherHealthy Female Volunteers / Type 2 Diabetes Mellitus1
1CompletedTreatmentHealthy Volunteers / Type 2 Diabetes Mellitus1
1CompletedTreatmentImpaired Renal Function / Type 2 Diabetes Mellitus1
1CompletedTreatmentType 2 Diabetes Mellitus1
2CompletedBasic ScienceCongestive Heart Failure (CHF)1
2CompletedTreatmentType 2 Diabetes Mellitus4
3Active Not RecruitingTreatmentType 2 Diabetes Mellitus1
3CompletedTreatmentDiabetes Mellitus (DM)1
3CompletedTreatmentDiabetes Mellitus (DM) / Type 2 Diabetes Mellitus1
3CompletedTreatmentType 2 Diabetes Mellitus7
3WithdrawnTreatmentType 2 Diabetes Mellitus2
4CompletedTreatmentDiabetes Mellitus (DM)1
4CompletedTreatmentType 2 Diabetes Mellitus1
4TerminatedTreatmentDiabetes Mellitus (DM)1
4TerminatedTreatmentType 2 Diabetes Mellitus2

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
Powder, for solutionSubcutaneous30 mg
Powder, for solutionSubcutaneous50 mg
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

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

Kind
Protein
Organism
Human
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. [PubMed:25136065]

Drug created on April 28, 2015 15:08 / Updated on November 18, 2018 13:32