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Identification
NameAlbiglutide
Accession NumberDB09043
TypeBiotech
GroupsApproved
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 structureDb09043
Related Articles
Protein chemical formulaC3232H5032N864O979S41
Protein average weight72970.0 Da
Sequences
> Albiglutide sequence
HGEGTFTSDVSSYLEGQAAKEFIAWLVKGRHGEGTFTSDVSSYLEGQAAKEFIAWLVKGR
DAHKSEVAHRFKDLGEENFKALVLIAFAQYLQQCPFEDHVKLVNEVTEFAKTCVADESAE
NCDKSLHTLFGDKLCTVATLRETYGEMADCCAKQEPERNECFLQHKDDNPNLPRLVRPEV
DVMCTAFHDNEETFLKKYLYEIARRHPYFYAPELLFFAKRYKAAFTECCQAADKAACLLP
KLDELRDEGKASSAKQRLKCASLQKFGERAFKAWAVARLSQRFPKAEFAEVSKLVTDLTK
VHTECCHGDLLECADDRADLAKYICENQDSISSKLKECCEKPLLEKSHCIAEVENDEMPA
DLPSLAADFVESKDVCKNYAEAKDVFLGMFLYEYARRHPDYSVVLLLRLAKTYETTLEKC
CAAADPHECYAKVFDEFKPLVEEPQNLIKQNCELFEQLGEYKFQNALLVRYTKKVPQVST
PTLVEVSRNLGKVGSKCCKHPEAKRMPCAEDYLSVVLNQLCVLHEKTPVSDRVTKCCTES
LVNRRPCFSALEVDETYVPKEFNAETFTFHADICTLSEKERQIKKQTALVELVKHKPKAT
KEQLKAVMDDFAAFVEKCCKADDKETCFAEEGKKLVAASQAALGL
Download FASTA Format
SynonymsNot Available
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Eperzanpowder for solution50 mgsubcutaneousGlaxosmithkline IncNot applicableNot applicableCanada
Eperzanpowder for solution30 mgsubcutaneousGlaxosmithkline IncNot applicableNot applicableCanada
Tanzeuminjection, powder, lyophilized, for solution30 mg/.5mLsubcutaneousGlaxo Smith Kline Llc2014-04-15Not applicableUs
Tanzeuminjection, powder, lyophilized, for solution50 mg/.5mLsubcutaneousGlaxo Smith Kline Llc2014-04-15Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIINot Available
CAS number782500-75-8
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available
Pharmacology
IndicationIndicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.
PharmacodynamicsNot Available
Mechanism of actionAlbiglutide is an agonist of the GLP-1 (glucagon-like peptide 1) receptor and augments glucose-dependent insulin secretion. Albiglutide also slows gastric emptying.
Related Articles
AbsorptionMaximum 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 bindingNot 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 eliminationNot Available
Half life4-7 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
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Powder for solutionsubcutaneous30 mg
Powder for solutionsubcutaneous50 mg
Injection, powder, lyophilized, for solutionsubcutaneous30 mg/.5mL
Injection, powder, lyophilized, for solutionsubcutaneous50 mg/.5mL
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental PropertiesNot Available
References
Synthesis ReferenceNot Available
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
ATC CodesA10BX13
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
Acetylsalicylic acidAcetylsalicylic acid may increase the hypoglycemic activities of Albiglutide.
ChlorpropamideAlbiglutide may increase the hypoglycemic activities of Chlorpropamide.
DihydrotestosteroneDihydrotestosterone may increase the hypoglycemic activities of Albiglutide.
Insulin HumanAlbiglutide may increase the hypoglycemic activities of Insulin Regular.
Insulin LisproAlbiglutide may increase the hypoglycemic activities of Insulin Lispro.
LeuprolideThe therapeutic efficacy of Albiglutide can be decreased when used in combination with Leuprolide.
Lipoic AcidLipoic Acid may increase the hypoglycemic activities of Albiglutide.
OxandroloneOxandrolone may increase the hypoglycemic activities of Albiglutide.
ParoxetineParoxetine may increase the hypoglycemic activities of Albiglutide.
PegvisomantPegvisomant may increase the hypoglycemic activities of Albiglutide.
PhenelzinePhenelzine may increase the hypoglycemic activities of Albiglutide.
SparfloxacinSparfloxacin may increase the hypoglycemic activities of Albiglutide.
TestosteroneTestosterone may increase the hypoglycemic activities of Albiglutide.
TranylcypromineTranylcypromine may increase the hypoglycemic activities of Albiglutide.
TrichlormethiazideThe therapeutic efficacy of Albiglutide can be decreased when used in combination with Trichlormethiazide.
Food InteractionsNot 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
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 ]
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Drug created on April 28, 2015 15:08 / Updated on August 17, 2016 12:24