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Exenatide: a novel treatment of Type 2 diabetes

Bo Ahren

Glucagon-like peptide-1 is an incretin hormone with antidiabetic action due to stimulation of insulin secretion, and potentially also to an increase in -cell mass, inhibition of glucagon secretion, delay in gastric emptying and induction of satiety. A problem in developing glucagon-like peptide-1 as a therapeutic compound is that the hormone is rapidly inactivated by dipeptidyl peptidase-4. To overcome this, long-acting dipeptidyl peptidase-4, resistant receptor agonists have been explored. One such promising agonist is exenatide, which was isolated as exendin-4 from the lizard Gila monster. Exenatide, administered twice daily subcutaneously, improves metabolic control in subjects with Type 2 diabetes, both when given alone and together with other treatments. The durability is good – a 30-week study showed that HbA1c was reduced by 1.0%. This observation is also seen in association with weight loss. Furthermore, clinical studies have shown that exenatide is safe and tolerable. Mild-to-moderate nausea and vomiting are the most consistent adverse events – it is seen in the early phases of treatment in approximately 30% of subjects given exenatide. The experience so far shows that exenatide offers a promising novel therapy for Type 2 diabetes, based on an interaction with glucagon-like peptide-1 receptors.