Liraglutide: A Review of its Use in Type 2 Diabetes Mellitus
Summary Liraglutide (Victoza®) is an acylated analogue of glucagon-like peptide-1 (GLP-1) indicated for the treatment of type 2 diabetes mellitus. In phase III studies, once-daily subcutaneous liraglutide improved glycaemic control compared with placebo or active comparator in adult patients with ty...
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Veröffentlicht in: | Drugs (New York, N.Y.) N.Y.), 2009-10, Vol.69 (14), p.1985-2004 |
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Sprache: | eng |
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Zusammenfassung: | Summary
Liraglutide (Victoza®) is an acylated analogue of glucagon-like peptide-1 (GLP-1) indicated for the treatment of type 2 diabetes mellitus. In phase III studies, once-daily subcutaneous liraglutide improved glycaemic control compared with placebo or active comparator in adult patients with type 2 diabetes, both as monotherapy and in combination with one or two oral antidiabetic drugs such as metformin, sulfonylureas or thiazolidinediones. Liraglutide provided significantly better glycaemic control than rosiglitazone or insulin glargine in combination trials. At appropriate dosages, liraglutide was noninferior to glimepiride with respect to glycaemic control in a combination trial, but provided significantly better control than glimepiride or glibenclamide in monotherapy trials. Liraglutide improved pancreatic b-cell function, generally 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. Thus, liraglutide is an effective treatment option for use in patients with type 2 diabetes mellitus.
Pharmacological Properties
Liraglutide is an acylated GLP-1 analogue that shares 97% amino acid sequence identity with native GLP-1. Liraglutide reduces both fasting and postprandial plasma glucose levels, with its effect lasting throughout a 24-hour dosing interval. It increases insulin secretion, reduces postprandial glucagon secretion, delays gastric emptying and improves b-cell function. It is also associated with a reduction in bodyweight.
Liraglutide self-associates into a heptameric structure that delays absorption from the subcutaneous injection site and slows its metabolism, giving it a prolonged elimination half-life compared with native GLP-1. The resulting pharmacokinetic profile allows for once-daily administration. The delay in gastric emptying associated with liraglutide does not cause clinically significant changes in the overall exposure to coadministered oral drugs.
Therapeutic Efficacy
In a well designed, 52-week, monotherapy trial in 746 patients with early-stage type 2 diabetes (LEAD-3), subcutaneous liraglutide 1.2 or 1.8 mg once daily improved glycaemic control (in terms of reduction from baseline in glycosylated haemoglobin [HbA
lc
] level) to a significantly greater extent than seen with oral glimepiride 8 mg once daily. These improvements in glycaemic control were sustain |
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ISSN: | 0012-6667 1179-1950 |
DOI: | 10.2165/11201060-000000000-00000 |