An update on exenatide, a novel therapeutic option for patients with type 2 diabetes.
ABSTRACT Exenatide, a synthetic glucagon GLP-1 receptor agonist, belongs to a new class of agents approved as a treatment option in patients with poorly controlled type 2 diabetes not adequately controlled on oral antidiabetic agents. The principal mode of drug action includes enhanced glucose-dependent insulin secretion --the so called "incretin effect"-- suppression of glucagon and inhibition of endogenous glucose production. The potential to address these dysregulated pathways allows exenatide to be a valuable adjunct to existing treatment options for patients with poorly controlled type 2 diabetes. Clinical trials with twice-daily exenatide have shown significant improvements in glycemic control (HbA(1c) reductions of 0.8-1% across studies), progressive weight loss and low incidence of hypoglycemia. Common side effects include nausea and vomiting which usually subside after a few days of therapy and do not usually necessitate withdrawal of the drug. In recent months, a longer-acting, once-weekly preparation of exenatide, which is currently approved for use in Europe, has shown promise and phase III studies indicate that it may be more potent and efficacious than existing twice-daily preparations. Meanwhile, the results from long-term studies to assess cardiovascular benefits with exenatide therapy are eagerly awaited.