albiglutide   Click here for help

GtoPdb Ligand ID: 7386

Synonyms: Eperzan® | GSK716155 | Tanzeum®
Approved drug
albiglutide is an approved drug (FDA and EMA (2014))
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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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].
Selectivity at GPCRs
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Target Sp. Type Action Value Parameter Concentration range (M) Reference
GLP-1 receptor Rn Agonist Agonist 7.7 pEC50 - 1
pEC50 7.7 (EC50 2x10-8 M) [1]