Liraglutide is the first human glucagon-like peptide-1 receptor analog, based on the structure of native glucagon-like peptide-1 with pharmacokinetic properties suitable for once-daily dosing. In the Phase II studies and the Phase III Liraglutide Effect and Action in Diabetes (LEAD™) program, liraglutide has been shown to lower glycated hemoglobin A1c to the same degree or more than other oral antidiabetic drugs. Liraglutide also induces weight loss and improves β-cell function, blood pressure and some cardiovascular risk markers. Liraglutide is well tolerated; the adverse effect most frequently reported being transient nausea. This article reviews the Phase II studies and the Phase III LEAD™ program. In May 2008, Novo Nordisk submitted a new drug application for liraglutide to the US FDA and the EMEA.
Keywords: GLP-1; Type 2 diabetes; glucagon-like peptide-1 mimetic; glucagon-like peptide-1 receptor analog; glycemic control; weight loss; β-cell function.