Exenatide is the first in a new class of therapeutic agents known as incretin mimetics. It exhibits glucose-lowering activity similar to the naturally occurring incretin hormone glucagon-like peptide-1 (GLP-1). Exenatide is under development for improving glucose control in patients with type 2 diabetes who are not achieving adequate control through diet and oral medications alone. In rodent models, exenatide has been shown to significantly reduce fasting and postprandial glucose excursions and plasma glucagon levels. A direct effect upon beta-cell mass was also demonstrated. Early phase II studies confirmed the antidiabetic effects of exenatide in patients with type 2 diabetes. Clinical studies have included a program of 3 pivotal studies in patients who had not achieved adequate glycemic control with oral antidiabetic agents. The results of these studies have shown that patients treated with exenatide had reduced average glucose levels and improved glycemic control. A New Drug Application (NDA) is planned for mid-2004.