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
- 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.
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- Contraindications & Blackbox Warnings
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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.
Target Actions Organism AGlucagon-like peptide 1 receptor agonistHumans - 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
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data.- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAcarbose The risk or severity of hypoglycemia can be increased when Acarbose is combined with Albiglutide. Acebutolol The therapeutic efficacy of Albiglutide can be increased when used in combination with Acebutolol. Acetazolamide The therapeutic efficacy of Albiglutide can be increased when used in combination with Acetazolamide. Acetohexamide Albiglutide may increase the hypoglycemic activities of Acetohexamide. Acetyl sulfisoxazole The therapeutic efficacy of Albiglutide can be increased when used in combination with Acetyl sulfisoxazole. Acetylsalicylic acid The risk or severity of hypoglycemia can be increased when Acetylsalicylic acid is combined with Albiglutide. Alclometasone The risk or severity of hyperglycemia can be increased when Alclometasone is combined with Albiglutide. Alogliptin The risk or severity of hypoglycemia can be increased when Alogliptin is combined with Albiglutide. Amcinonide The risk or severity of hyperglycemia can be increased when Amcinonide is combined with Albiglutide. Aminosalicylic acid Aminosalicylic acid may increase the hypoglycemic activities of Albiglutide. 
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- Not Available
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Eperzan Powder, for solution 30 mg / 0.5 mL Subcutaneous Glaxosmithkline Inc Not applicable Not applicable Canada 
Eperzan Injection, powder, for solution 30 mg Subcutaneous Glaxo Smith Kline Trading Services 2021-01-12 2019-02-20 EU 
Eperzan Injection, powder, for solution 50 mg Subcutaneous Glaxo Smith Kline Trading Services 2021-01-12 2019-02-20 EU Eperzan Powder, for solution 50 mg / 0.5 mL Subcutaneous Glaxosmithkline Inc Not applicable Not applicable Canada Eperzan Injection, powder, for solution 30 mg Subcutaneous Glaxo Smith Kline Trading Services 2021-01-12 2019-02-20 EU Eperzan Injection, powder, for solution 50 mg Subcutaneous Glaxo Smith Kline Trading Services 2021-01-12 2019-02-20 EU Tanzeum Injection, powder, lyophilized, for solution 30 mg/0.5mL Subcutaneous GlaxoSmithKline LLC 2014-04-15 2020-09-30 US 
Tanzeum Injection, powder, lyophilized, for solution 50 mg/0.5mL Subcutaneous GlaxoSmithKline LLC 2014-04-15 2020-08-31 US
Categories
- ATC Codes
- A10BJ04 — Albiglutide
- Drug Categories
- Alimentary Tract and Metabolism
- Amino Acids, Peptides, and Proteins
- Blood Glucose Lowering Agents
- Drugs Used in Diabetes
- Gastrointestinal Hormones
- GLP-1 Agonists
- Glucagon-like peptide-1 (GLP-1) analogues
- Glucagon-Like Peptides
- Hormones
- Hormones, Hormone Substitutes, and Hormone Antagonists
- Incretins
- Pancreatic Hormones
- Peptide Hormones
- Peptides
- Proglucagon
- Protein Precursors
- Proteins
- Recombinant Proteins
- 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
- 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]
- External Links
- KEGG Drug
- D08843
- PubChem Substance
- 347910396
- 1534763
- Wikipedia
- Albiglutide
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Treatment Diabetes Mellitus 1 4 Completed Treatment Type 2 Diabetes Mellitus 1 4 Terminated Treatment Diabetes Mellitus 1 4 Terminated Treatment Type 2 Diabetes Mellitus 2 3 Completed Treatment Diabetes Mellitus 1 3 Completed Treatment Type 2 Diabetes Mellitus 12 3 Withdrawn Treatment Type 2 Diabetes Mellitus 2 2 Completed Basic Science Congestive Heart Failure (CHF) 1 2 Completed Treatment Type 1 Diabetes Mellitus 1 2 Completed Treatment Type 2 Diabetes Mellitus 5
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, powder, for solution Subcutaneous 30 MG Injection, powder, for solution Subcutaneous 50 MG Powder, for solution Subcutaneous 30 mg / 0.5 mL Powder, for solution Subcutaneous 50 mg / 0.5 mL Injection, powder, lyophilized, for solution Subcutaneous 30 mg/0.5mL Injection, powder, lyophilized, for solution Subcutaneous 50 mg/0.5mL - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
Targets
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- 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
- 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]
- 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]
- 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