This review updates the pharmacology, efficacy, safety, and tolerability of
liraglutide, a
glucagon-like peptide 1 (GLP-1) analog approved for the treatment of
type 2 diabetes (T2DM) in January 2010. MEDLINE was searched (May 2009-January 1, 2011) for articles in English, using the terms
liraglutide,
NN2211,
incretin mimetic,
glucagon-like peptide (GLP)-1, and
GLP-1 receptor agonist. Abstracts from key meetings (ADA 2009 and 2010, AACE 2010, EASD 2009, and EASD 2010) were also searched for relevant data. A
GLP-1 analog with pharmacokinetic properties allowing once-daily administration via
subcutaneous injection,
liraglutide has shown clinical benefits when used as monotherapy or in combination.
Liraglutide monotherapy has demonstrated efficacy in reducing
hemoglobin A1c (A1C) and
body weight, with low risk for
hypoglycemic events.
Liraglutide has also been studied in combination with
metformin,
glimepiride, and
rosiglitazone for the treatment of T2DM. Extension studies within the
Liraglutide Effects and Action in Diabetes clinical program have demonstrated the efficacy of
liraglutide over 2 years of treatment. Overall,
liraglutide has been shown to be well tolerated, with dose-dependent
nausea,
vomiting, and
diarrhea being the most commonly reported adverse events in clinical trials. Extended dosing periods have demonstrated the durability of response of
liraglutide with respect to
glycemic control, lack of
weight gain, and blood pressure benefits. Compared with
exenatide and
sitagliptin,
liraglutide seems to offer greater improvements in A1C, fasting plasma
glucose, and
body weight. Adverse events commonly associated with
liraglutide in clinical trials included
nausea and
hypoglycemia. Emerging data suggest that
liraglutide may be a useful option for patients with T2DM.