albiglutide   Click here for help

GtoPdb Ligand ID: 7386

Synonyms: Eperzan® | GSK716155 | Tanzeum®
Approved drug
albiglutide is an approved drug (FDA and EMA (2014))
Compound class: Peptide or derivative
Comment: Albiglutide is recombinant protein engineered by fusing the gene for glucagon-like peptide 1 (GLP-1; an incretin secreted in the gut) with the gene for human albumin. In this case the GLP-1 appears to contain an amino acid substitution (Ala to Glu at the C-terminal) directly adjacent to the dipeptidyl peptidase-4 (DPP-4; the enzyme responsible for in vivo degradation of GLP-1) hydrolysis site, which renders the peptide resistant to cleavage by this enzyme [3,5]. In conjunction with the fusion to albumin [2] this drug has an extended half-life compared to other approved drug GLP-1 mimetics.
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Ligand Activity Visualisation Charts

These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.

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View interactive charts of activity data across species
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Summary of Clinical Use Click here for help
Albiglutide is approved to treat type 2 diabetes mellitus in conjunction with diet and excercise.
Mechanism Of Action and Pharmacodynamic Effects Click here for help
Albiglutide mimics the effects of endogenous GLP-1 on insulin secretion from pancreatic β-cells, reduction of food intake and induction of satiety at the central nervous system level. Due to it's extended half-life, meaning it only has to be injected once per week, this drug should be more patient friendly than the current GLP-1 analogs that require once or twice daily injections. Although this drug binds to the GLP1R, we have been unable to find affinity data for this drug at the human GLP1R to substantiate its MMOA. Therefore we have not tagged a primary target for this drug.
External links Click here for help
For extended ADME data see the following:

Drugs.com
European Medicines Agency (EMA)