GLP1 Receptor Agonist

Glucagon-like peptide(GLP)-1 is an incretin hormone displaying glucose-dependent stimulation of insulin secretion and able to restore the normal profile of insulin release in response to glucose (which is highly defective in type 2 diabetic patients). It displays as well trophic effects on the pancreatic ß-cells so preserving ß-cell mass, and inhibitory effects on gastrointestinal motility, which has been shown to ameliorate hyperglycemia and reduce glycemic excursions.

GLP-1 Receptor Agonists Mechanism of Action

Because it restores an important defective pathway in type 2 diabetes and induces only a glucose dependent insulin secretion, the targeting of GLP-1 pathway displays numerous advantages versus other anti diabetic therapeutic approaches currently available:

• This is an insulin secretagogue with no hypoglycemic risk as insulin secretion is glucose-dependent only
• By contrast to many other antidiabetic treatments, it has some weight lowering properties.

A non peptide GLP-1 receptor agonist, such as the one currently developed by Poxel, comes with numerous advantages. As opposed to peptidic GLP-1 receptor agonists, a non peptide compound can be developed as an orally active product, more convenient to use than injectable ones, and thus improving compliance for the patients as well as potentially benefiting from an earlier prescription in the treatment guidelines.

The Poxel project is currently in lead optimization, and has already demonstrated positive effects on insulin secretion in preclinical diabetic animal models.