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Synonyms: Eperzan® | GSK716155 | Tanzeum®
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.
Ligand Activity Visualisation ChartsThese 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. ✖ |
| Bioactivity Comments |
| In a study investigating the pharmacodynamics, pharmacokinetics, safety and tolerability of albiglutide, the drug was reported to improve fasting plasma glucose and postprandial glucose in type 2 diabetes patients [4]. The only affinity data for this compound (called albugon in the article) was generated using cells expressing the rat GLP-1 receptor, where the EC50 was reported as 20nM [1]. |
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