Products
Albiglutide was approved in many countries, in the EU, and in the United States in 2014 in the form of an injectable (Eperzan).
Structure and properties
Albiglutide is a GLP-1 dimer (fragment of 30 amino acids, 7-36) fused to the human protein albumin. The amino acid alanine at position 8 has been replaced by a glycine, resulting in reduced degradation via DPP-4. Compared with GLP-1, this results in a much longer half-life of 6 to 8 days.
Effects
Albiglutide (ATC A10BX13) has blood glucose-lowering and antidiabetic properties. The effects are due to binding to the GLP-1 receptor, a GPCR (G protein-coupled receptor). This receptor is also activated by the incretin GLP-1. GLP-1 receptor agonists:
- Promote insulin secretion from pancreatic beta cells.
- Decrease glucagon secretion from alpha cells, resulting in decreased glucose release by the liver (lowering gluconeogenesis).
- Increase insulin sensitivity.
- Slow gastric emptying, reducing the rate at which glucose enters the bloodstream.
- Increase satiety (central), reduce the feeling of hunger and may contribute to weight loss.
GLP-1 receptor agonists tend to cause less hypoglycemia because their effect does not occur until glucose levels are elevated. The orally available gliptins (see there) inhibit the breakdown of GLP-1, thereby enhancing its effects.
Indications
For the treatment of type 2 diabetes mellitus.
Dosage
According to the SmPC. The drug is administered subcutaneously once a week.
Contraindications
Albiglutide is contraindicated in case of hypersensitivity. For complete precautions, see the drug label.
Adverse Effects
The most common possible adverse effects include nausea, diarrhea, and injection site reactions.
