Products
Lixisenatide was approved as a subcutaneous solution for injection in the EU in 2012, in the United States in 2016, and in many countries in 2017 (Lyxumia). Lixisenatide is also combined with insulin glargine; see iGlarLixi (Suliqua).
Structure and properties
Lixisenatide is a peptide and GLP1 analog of 44 amino acids that, like exenatide, was developed starting from exendin-4, a polypeptide from the saliva of the North American Gila lizard . Lixisenatide has a longer half-life of about three hours and a higher binding affinity than the natural substrate GLP-1.
Effects
Lixisenatide (ATC A10BX10) 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 injected subcutaneously once daily.
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Adverse effects
The most common possible adverse effects include nausea, vomiting, diarrhea, and headache. Hypoglycemia is common only in combination with sulfonylureas or insulins.
