Exenatide: clinical aspects of the first incretin-mimetic for the treatment of type 2 diabetes mellitus

Background: Exenatide is the first-in-class incretin mimetic for the treatment of type 2 diabetes. Objective: To assess exenatide's mechanism of action, therapeutic and adverse effects. Methods: Pharmacokinetics and pharmacodynamics of exenatide were reviewed, as well Phase I, II and III clinical trials, and postmarket reports. Results/conclusion: Exenatide improves fasting plasma glucose and HbA1c in type 2 diabetic patients not controlled on other antidiabetic drugs, due to its effects on glucose-dependent stimulation on insulin secretion, suppression elevated glucagon secretion, slowing the accelerated rate of gastric emptying, reduction of food intake and possible beta-cell preservation. Nausea and vomiting were the most common and dose-related side effects. Rare reports of acute pancreatitis do not appear greater than the rate in the general population of patients with type 2 diabetes.