Liraglutide: First Once-Daily Human GLP-1 Analogue

Abstract

The gastrointestinal hormones glucose- dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1), termed incretins, are essential regulators of normal glucose homeostasis. The drug substance, Liraglutide, is a long acting analogue of the naturally occurring human GLP-1 (7-37) with 97% homology and a lipophilic substituent for prolongation of half life.

Liraglutide is available in a pre-filled, multi-dose pen-injector containing $6.0~mg/ml$ of the drug substance in solution presented for subcutaneous injection.

Liraglutide provided significantly better glycemic control than Rosglitazone or insulin glargine in combination trials. Liraglutide improved pancreatic beta-cell function, consistently led to weight loss, and was associated with a low risk of hypoglycaemia. Liraglutide was generally well tolerated, with the most common adverse events being gastrointestinal events, such as nausea, which decreased over time.