Exenatide was authorized for use in the treatment of type 2 diabetes mellitus by the FDA (Food and Drug Administration) in the USA in April 2005 and in Europe early in 2007. Exenatide has proven safe in both experimental and preclinical trials.
Clinical studies have shown exenatide to be generally well tolerated. As the first member of a new class of antidiabetic agents called incretin mimetics it is intended for use in the treatment of type 2 diabetes mellitus.
Subcutaneous exenatide is as effective in the management of type 2 diabetes as the human incretin hormone, glucagon-like peptide-1 (GLP-1), and has four clinically significant advantages over other available oral antidiabetic drugs and insulin: a) it does not cause hypoglycemia; b) it enhances insulin secretion even in patients nonresponsive to sulfonylurea -based therapy; c) reduces elevated glucagon levels; d) significantly prevents weight gain in obese diabetic patients. By inhibiting gast ric and small intestine motility as well as secretion of gastric acid, exenatide reduces the uptake of nutrients from the gastrointestinal tract and postprandial blood glucose fluctuations.
The subcutaneous GLP-1 analogue exenatide with a half life of 2.4 hours has the disadvantage of inducing a short lasting hypoglycemic effect (6-8 hours) and therefore needs to be given twice daily.