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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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]