Identification

Name
Albiglutide
Accession Number
DB09043  (DB05162)
Type
Biotech
Groups
Approved
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
Not Available
External IDs
GSK-716155 / GSK716155
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
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.

Structured Indications
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
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
AlaproclateAlaproclate may increase the hypoglycemic activities of Albiglutide.Experimental
AloxiprinAloxiprin may increase the hypoglycemic activities of Albiglutide.Experimental
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
BrofaromineBrofaromine may increase the hypoglycemic activities of Albiglutide.Experimental
Carbaspirin calciumCarbaspirin calcium may increase the hypoglycemic activities of Albiglutide.Experimental
CarbutamideAlbiglutide may increase the hypoglycemic activities of Carbutamide.Experimental
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
CitalopramCitalopram may increase the hypoglycemic activities of Albiglutide.Approved
DapoxetineDapoxetine may increase the hypoglycemic activities of Albiglutide.Investigational
dersalazinedersalazine 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
GarenoxacinGarenoxacin may increase the hypoglycemic activities of Albiglutide.Investigational
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
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
GLPG-0492GLPG-0492 may increase the hypoglycemic activities of Albiglutide.Investigational
GlyburideAlbiglutide may increase the hypoglycemic activities of Glyburide.Approved
GrepafloxacinGrepafloxacin may increase the hypoglycemic activities of Albiglutide.Withdrawn
GuacetisalGuacetisal may increase the hypoglycemic activities of Albiglutide.Experimental
HarmalineHarmaline may increase the hypoglycemic activities of Albiglutide.Experimental
Hemoglobin crosfumarilHemoglobin crosfumaril may increase the hypoglycemic activities of Albiglutide.Experimental
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
MebanazineMebanazine may increase the hypoglycemic activities of Albiglutide.Withdrawn
MesalazineMesalazine may increase the hypoglycemic activities of Albiglutide.Approved
MesteroloneMesterolone may increase the hypoglycemic activities of Albiglutide.Experimental
MetahexamideAlbiglutide may increase the hypoglycemic activities of Metahexamide.Experimental
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
Nalidixic AcidNalidixic Acid may increase the hypoglycemic activities of Albiglutide.Approved
NandroloneNandrolone may increase the hypoglycemic activities of Albiglutide.Experimental
NefazodoneNefazodone may increase the hypoglycemic activities of Albiglutide.Approved, Withdrawn
NemonoxacinNemonoxacin may increase the hypoglycemic activities of Albiglutide.Investigational
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
OlsalazineOlsalazine may increase the hypoglycemic activities of Albiglutide.Approved
OxandroloneOxandrolone may increase the hypoglycemic activities of Albiglutide.Approved, Investigational
Oxolinic acidOxolinic acid may increase the hypoglycemic activities of Albiglutide.Experimental
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
Pipemidic acidPipemidic acid may increase the hypoglycemic activities of Albiglutide.Experimental
PirlindolePirlindole may increase the hypoglycemic activities of Albiglutide.Approved
Piromidic acidPiromidic acid may increase the hypoglycemic activities of Albiglutide.Experimental
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
RufloxacinRufloxacin may increase the hypoglycemic activities of Albiglutide.Experimental
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
SitafloxacinSitafloxacin may increase the hypoglycemic activities of Albiglutide.Experimental
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
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 Interactions
Not Available

References

Synthesis Reference
Not 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
KEGG Drug
D08843
Wikipedia
Albiglutide
ATC Codes
A10BX13 — Albiglutide
AHFS Codes
Not Available
PDB Entries
Not Available
FDA label
Not Available
MSDS
Not 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
3RecruitingTreatmentType 2 Diabetes Mellitus1
3WithdrawnTreatmentType 2 Diabetes Mellitus2
4Active Not RecruitingTreatmentDiabetes Mellitus (DM)2
4CompletedTreatmentType 2 Diabetes Mellitus2
4TerminatedTreatmentType 2 Diabetes Mellitus1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not 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
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 May 31, 2017 16:27