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
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.
Click here for help

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.

✖

View interactive charts of activity data across species
References
1. Baggio LL, Huang Q, Brown TJ, Drucker DJ. (2004)
A recombinant human glucagon-like peptide (GLP)-1-albumin protein (albugon) mimics peptidergic activation of GLP-1 receptor-dependent pathways coupled with satiety, gastrointestinal motility, and glucose homeostasis.
Diabetes, 53 (9): 2492-500. [PMID:15331566]
2. Chuang VT, Kragh-Hansen U, Otagiri M. (2002)
Pharmaceutical strategies utilizing recombinant human serum albumin.
Pharm Res, 19 (5): 569-77. [PMID:12069157]
3. Heard KR, Wu W, Li Y, Zhao P, Woznica I, Lai JH, Beinborn M, Sanford DG, Dimare MT, Chiluwal AK et al.. (2013)
A general method for making peptide therapeutics resistant to serine protease degradation: application to dipeptidyl peptidase IV substrates.
J Med Chem, 56 (21): 8339-51. [PMID:24044354]
4. Matthews JE, Stewart MW, De Boever EH, Dobbins RL, Hodge RJ, Walker SE, Holland MC, Bush MA, Albiglutide Study Group. (2008)
Pharmacodynamics, pharmacokinetics, safety, and tolerability of albiglutide, a long-acting glucagon-like peptide-1 mimetic, in patients with type 2 diabetes.
J Clin Endocrinol Metab, 93 (12): 4810-7. [PMID:18812476]
5. Tomkin GH. (2009)
Albiglutide, an albumin-based fusion of glucagon-like peptide 1 for the potential treatment of type 2 diabetes.
Curr Opin Mol Ther, 11 (5): 579-88. [PMID:19806507]