The FDA has approved a once-weekly extended-release formulation of exenatide (Bydureon – Amylin), an injectable glucagon-like peptide-1 (GLP-1) receptor agonist, for treatment of type 2 diabetes.

MECHANISM OF ACTION — GLP-1 is released from cells in the gastrointestinal tract in response to food. It potentiates insulin secretion, lowers serum glucagon concentrations, slows gastric emptying and promotes satiety. In patients with diabetes, administration of a GLP-1 agonist results in lowering of fasting blood glucose and reduction of postprandial glucose levels.1,2

PHARMACOKINETICS — The extended-release (ER) formulation releases exenatide from microspheres over a period of about 10 weeks. The initial release is from the surface of the microspheres, followed by a more gradual release from the microspheres themselves, resulting in 2 peaks ... more      

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