Exenatide LAR: a sustained-release formulation of exenatide for the treatment of type 2 diabetes

Despite the availability of multiple classes of glucose-lowering agents to treat type 2 diabetes mellitus, glycemic control often remains inadequate, with hemoglobin (Hb) A^sub 1c^ values above the treatment goal of 7%. One newer class of agents, the glucagon-like peptide (GLP-1) receptor agonists, targets the incretin system to increase insulin secretion in response to glucose stimuli, while also inhibiting glucagon secretion, slowing gastric emptying and inducing satiety. Currently, exenatide is one of the few FDA-approved GLP-1 receptor agonists and its use is limited by the need for twice-daily injections. A long-acting release (LAR) formulation of exenatide is being evaluated in clinical trials to assess effects on glucose control and patient quality of life. Data from published clinical trials of exenatide LAR show that a dose of 2 mg given by subcutaneous injection once weekly is associated with reductions in HbA^sub 1c^ fasting plasma glucose and body weight. When compared to twice-daily exenatide, the LAR formulation appears to offer slightly increased efficacy. Exenatide LAR has been well tolerated in phase 2 and 3 clinical trials. Mild-to-moderate nausea is the most commonly reported adverse drug event. Long-term safety and efficacy data have not yet been published and more information is needed before exenatide LAR finds its place in therapy. Currently, once-weekly exenatide LAR is awaiting approval by FDA. [PUBLICATION ABSTRACT]