Pharmacokinetics and pharmacodynamics of liraglutide, a long-acting, potent glucagon-like peptide-1 analog

Pharmacotherapy. 2009 Dec;29(12 Pt 2):33S-42S. doi: 10.1592/phco.29.pt2.33S.

Abstract

Despite the continued development of new pharmacologic agents, and the use of several existing drug therapies, almost two thirds of patients with type 2 diabetes mellitus do not reach the American Diabetes Association-targeted hemoglobin A(1c) level of less than 7.0%. Therefore, maintaining adequate metabolic control remains a primary concern for many clinicians and patients. It is now well recognized that in addition to defective secretion and action of insulin, other hormones also potentially play a role in the development and progression of type 2 diabetes. Glucagon-like peptide-1 (GLP-1) is a gastrointestinal hormone from the incretin family, which stimulates insulin secretion and plays an important role in regulating the enteroinsular axis. Incretin-based therapies are the newest class of glucose-lowering drugs for the treatment of type 2 diabetes and may help address some of the unmet needs in this therapeutic area. Liraglutide is a once-daily GLP-1 analog that has been recently approved by the European Union regulatory agency and is in late-stage review by the United States Food and Drug Administration for the treatment of type 2 diabetes. The pharmacokinetic and pharmacodynamic properties of liraglutide and mechanisms behind its protracted action, which in turn enables enhanced glycemic control, are reviewed.

Publication types

  • Review

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Delayed-Action Preparations / chemistry
  • Delayed-Action Preparations / pharmacokinetics
  • Delayed-Action Preparations / pharmacology
  • Diabetes Mellitus, Type 2 / metabolism
  • Glucagon-Like Peptide 1 / analogs & derivatives*
  • Glucagon-Like Peptide 1 / chemistry
  • Glucagon-Like Peptide 1 / pharmacokinetics*
  • Glucagon-Like Peptide 1 / pharmacology
  • Humans
  • Liraglutide
  • Molecular Sequence Data
  • Time Factors

Substances

  • Delayed-Action Preparations
  • Liraglutide
  • Glucagon-Like Peptide 1