Identification
NameAlbiglutide
Accession NumberDB09043  (DB05162)
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 IDs GSK-716155 / GSK716155
Product Ingredients 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/.5mLSubcutaneousGlaxosmithkline Inc2014-04-15Not applicableUs
TanzeumInjection, powder, lyophilized, for solution50 mg/.5mLSubcutaneousGlaxosmithkline Inc2014-04-15Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Categories
UNII5E7U48495E
CAS number782500-75-8
Pharmacology
Indication

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

Structured Indications
PharmacodynamicsNot 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.

TargetKindPharmacological actionActionsOrganismUniProt ID
Glucagon-like peptide 1 receptorProteinyes
agonist
HumanP43220 details
Related Articles
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 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 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
PathwaysNot Available
Pharmacogenomic Effects/ADRs Not Available
Interactions
Drug Interactions
DrugInteractionDrug group
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE may increase the hypoglycemic activities of Albiglutide.Experimental
AcetohexamideAlbiglutide may increase the hypoglycemic activities of Acetohexamide.Withdrawn
Acetylsalicylic acidAcetylsalicylic acid may increase the hypoglycemic activities of Albiglutide.Approved, Vet Approved
Aminosalicylic AcidAminosalicylic Acid may increase the hypoglycemic activities of Albiglutide.Approved
BalsalazideBalsalazide may increase the hypoglycemic activities of Albiglutide.Approved, Investigational
BenmoxinBenmoxin may increase the hypoglycemic activities of Albiglutide.Withdrawn
CaroxazoneCaroxazone may increase the hypoglycemic activities of Albiglutide.Withdrawn
ChlorpropamideAlbiglutide may increase the hypoglycemic activities of Chlorpropamide.Approved
CinoxacinCinoxacin may increase the hypoglycemic activities of Albiglutide.Approved, Withdrawn
CiprofloxacinCiprofloxacin may increase the hypoglycemic activities of Albiglutide.Approved, Investigational
CitalopramCitalopram may increase the hypoglycemic activities of Albiglutide.Approved
DapoxetineDapoxetine may increase the hypoglycemic activities of Albiglutide.Investigational
DesvenlafaxineDesvenlafaxine may increase the hypoglycemic activities of Albiglutide.Approved
DiflunisalDiflunisal may increase the hypoglycemic activities of Albiglutide.Approved
DihydrotestosteroneDihydrotestosterone may increase the hypoglycemic activities of Albiglutide.Illicit
DuloxetineDuloxetine may increase the hypoglycemic activities of Albiglutide.Approved
EnoxacinEnoxacin may increase the hypoglycemic activities of Albiglutide.Approved
EscitalopramEscitalopram may increase the hypoglycemic activities of Albiglutide.Approved, Investigational
EtoperidoneEtoperidone may increase the hypoglycemic activities of Albiglutide.Approved
FleroxacinFleroxacin may increase the hypoglycemic activities of Albiglutide.Approved
FlumequineFlumequine may increase the hypoglycemic activities of Albiglutide.Withdrawn
FluoxetineFluoxetine may increase the hypoglycemic activities of Albiglutide.Approved, Vet Approved
FluoxymesteroneFluoxymesterone may increase the hypoglycemic activities of Albiglutide.Approved, Illicit
FluvoxamineFluvoxamine may increase the hypoglycemic activities of Albiglutide.Approved, Investigational
FurazolidoneFurazolidone may increase the hypoglycemic activities of Albiglutide.Approved, Vet Approved
GatifloxacinGatifloxacin may increase the hypoglycemic activities of Albiglutide.Approved, Investigational
GemifloxacinGemifloxacin may increase the hypoglycemic activities of Albiglutide.Approved, Investigational
GlibornurideAlbiglutide may increase the hypoglycemic activities of Glibornuride.Withdrawn
GliclazideAlbiglutide may increase the hypoglycemic activities of Gliclazide.Approved
GlimepirideAlbiglutide may increase the hypoglycemic activities of Glimepiride.Approved
GlipizideAlbiglutide may increase the hypoglycemic activities of Glipizide.Approved
GliquidoneAlbiglutide may increase the hypoglycemic activities of Gliquidone.Approved
GlisoxepideAlbiglutide may increase the hypoglycemic activities of Glisoxepide.Approved
GlyburideAlbiglutide may increase the hypoglycemic activities of Glyburide.Approved
GrepafloxacinGrepafloxacin may increase the hypoglycemic activities of Albiglutide.Withdrawn
HydracarbazineHydracarbazine may increase the hypoglycemic activities of Albiglutide.Experimental
IndalpineIndalpine may increase the hypoglycemic activities of Albiglutide.Investigational, Withdrawn
Insulin PorkAlbiglutide may increase the hypoglycemic activities of Insulin Pork.Approved
IproclozideIproclozide may increase the hypoglycemic activities of Albiglutide.Withdrawn
IproniazidIproniazid may increase the hypoglycemic activities of Albiglutide.Withdrawn
IsocarboxazidIsocarboxazid may increase the hypoglycemic activities of Albiglutide.Approved
LevofloxacinLevofloxacin may increase the hypoglycemic activities of Albiglutide.Approved, Investigational
LevomilnacipranLevomilnacipran may increase the hypoglycemic activities of Albiglutide.Approved
LomefloxacinLomefloxacin may increase the hypoglycemic activities of Albiglutide.Approved
MebanazineMebanazine may increase the hypoglycemic activities of Albiglutide.Withdrawn
MesalazineMesalazine may increase the hypoglycemic activities of Albiglutide.Approved
Methylene blueMethylene blue may increase the hypoglycemic activities of Albiglutide.Investigational
MethyltestosteroneMethyltestosterone may increase the hypoglycemic activities of Albiglutide.Approved
MilnacipranMilnacipran may increase the hypoglycemic activities of Albiglutide.Approved
MinaprineMinaprine may increase the hypoglycemic activities of Albiglutide.Approved
MoclobemideMoclobemide may increase the hypoglycemic activities of Albiglutide.Approved
MoxifloxacinMoxifloxacin may increase the hypoglycemic activities of Albiglutide.Approved, Investigational
Nalidixic AcidNalidixic Acid may increase the hypoglycemic activities of Albiglutide.Approved
NCX 4016NCX 4016 may increase the hypoglycemic activities of Albiglutide.Investigational
NefazodoneNefazodone may increase the hypoglycemic activities of Albiglutide.Approved, Withdrawn
NialamideNialamide may increase the hypoglycemic activities of Albiglutide.Withdrawn
NitroaspirinNitroaspirin may increase the hypoglycemic activities of Albiglutide.Investigational
NorfloxacinNorfloxacin may increase the hypoglycemic activities of Albiglutide.Approved
OctamoxinOctamoxin may increase the hypoglycemic activities of Albiglutide.Withdrawn
OfloxacinOfloxacin may increase the hypoglycemic activities of Albiglutide.Approved
OlsalazineOlsalazine may increase the hypoglycemic activities of Albiglutide.Approved
OxandroloneOxandrolone may increase the hypoglycemic activities of Albiglutide.Approved, Investigational
OxymetholoneOxymetholone may increase the hypoglycemic activities of Albiglutide.Approved, Illicit
PargylinePargyline may increase the hypoglycemic activities of Albiglutide.Approved
ParoxetineParoxetine may increase the hypoglycemic activities of Albiglutide.Approved, Investigational
PazufloxacinPazufloxacin may increase the hypoglycemic activities of Albiglutide.Investigational
PefloxacinPefloxacin may increase the hypoglycemic activities of Albiglutide.Approved
PegvisomantPegvisomant may increase the hypoglycemic activities of Albiglutide.Approved
PhenelzinePhenelzine may increase the hypoglycemic activities of Albiglutide.Approved
PheniprazinePheniprazine may increase the hypoglycemic activities of Albiglutide.Withdrawn
PhenoxypropazinePhenoxypropazine may increase the hypoglycemic activities of Albiglutide.Withdrawn
PirlindolePirlindole may increase the hypoglycemic activities of Albiglutide.Approved
PivhydrazinePivhydrazine may increase the hypoglycemic activities of Albiglutide.Withdrawn
PrulifloxacinPrulifloxacin may increase the hypoglycemic activities of Albiglutide.Investigational
RasagilineRasagiline may increase the hypoglycemic activities of Albiglutide.Approved
RosoxacinRosoxacin may increase the hypoglycemic activities of Albiglutide.Approved
SafrazineSafrazine may increase the hypoglycemic activities of Albiglutide.Withdrawn
Salicylic acidSalicylic acid may increase the hypoglycemic activities of Albiglutide.Approved, Vet Approved
SelegilineSelegiline may increase the hypoglycemic activities of Albiglutide.Approved, Investigational, Vet Approved
SertralineSertraline may increase the hypoglycemic activities of Albiglutide.Approved
SparfloxacinSparfloxacin may increase the hypoglycemic activities of Albiglutide.Approved
StanozololStanozolol may increase the hypoglycemic activities of Albiglutide.Approved, Vet Approved
TemafloxacinTemafloxacin may increase the hypoglycemic activities of Albiglutide.Withdrawn
TestosteroneTestosterone may increase the hypoglycemic activities of Albiglutide.Approved, Investigational
TolazamideAlbiglutide may increase the hypoglycemic activities of Tolazamide.Approved
TolbutamideAlbiglutide may increase the hypoglycemic activities of Tolbutamide.Approved
ToloxatoneToloxatone may increase the hypoglycemic activities of Albiglutide.Approved
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypoglycemic activities of Albiglutide.Experimental
TranylcypromineTranylcypromine may increase the hypoglycemic activities of Albiglutide.Approved
TrovafloxacinTrovafloxacin may increase the hypoglycemic activities of Albiglutide.Approved, Withdrawn
VenlafaxineVenlafaxine may increase the hypoglycemic activities of Albiglutide.Approved
ZimelidineZimelidine may increase the hypoglycemic activities of Albiglutide.Withdrawn
Food InteractionsNot 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 — Albiglutide
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
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 Mellitus6
3Not Yet RecruitingTreatmentType 2 Diabetes Mellitus1
3RecruitingTreatmentType 2 Diabetes Mellitus1
3WithdrawnTreatmentType 2 Diabetes Mellitus1
4Active Not RecruitingTreatmentDiabetes Mellitus (DM)2
4CompletedTreatmentType 2 Diabetes Mellitus2
4TerminatedTreatmentType 2 Diabetes Mellitus1
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
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

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 May 31, 2017 16:27