Albiglutide

General Description

Albiglutide (also known as naliglutide, GSK 716155) isa sequential dimer of GLP-1(7–36)(Ala8→Gly) covalentlylinked to modified human serum albumin (i.e., it is a “fusionprotein” with modified HSA). This molecule is currentlywell into phase III clinical trials. Although albiglutide,if marketed (Syncria, GlaxoSmithKline), will—likeexenatide—be administered by injection, the half-life andduration of 6 to 7 days would allow for weekly administration.

Clinical Use

GLP-1 receptor agonist:
Treatment of type 2 diabetes mellitus

Enzyme inhibitor

This GLP-1 agonist and anti-diabetic drug (MW = 72.9 kDa; CAS 782500- 75-8), marketed as Eperzan? and Tanzeum?, by GlaxoSmithKline (GSK) is a dipeptidyl peptidase-4-resistant glucagon-like peptide-1 dimer fused to human albumin. Albiglutide has a half-life of 4-7 days, commending it for biweekly or weekly administration in the treatment of Type 2 diabetes. The half-life is considerably longer than exenatide (Byetta?) and liraglutide (Victoza?).

Metabolism

Albiglutide is a protein for which the expected metabolic pathway is degradation to small peptides and individual amino acids by ubiquitous proteolytic enzymes.