The Pharmacokinetic Properties of Glucagon-like Peptide-1 Receptor Agonists and Their Mode and Mechanism of Action in Patients with Type 2 Diabetes

J Fam Pract. 2018 Jun;67(6 suppl):S8-S13.

Abstract

Once-weekly (OW) glucagon-like peptide-1 receptor agonists (GLP-1 RAs) have demonstrated improved glycemic control in patients with type 2 diabetes (T2D), and some have a number of other benefits, including weight loss, improvements in blood pressure and lipid profiles, and cardiovascular protection. They also provide a therapy option with a low risk of hypoglycemia, an attractive choice for many patients. Molecular structure and pharmacokinetic properties vary among GLP-1 RAs, with some more closely related than others to native glucagon-like peptide-1 (GLP-1). OW GLP-1 RAs have various modifications to their molecular structure that make the molecules resistant to degradation by dipeptidyl peptidase-4 (DPP-4), increasing the half-life of these drugs and making them suitable for OW administration. These differences in the molecular structures and pharmacokinetic properties between the various OW GLP-1 RAs help to explain the differences in efficacy, mechanisms, and safety profiles among the drugs, and these considerations can help primary care physicians to optimize prescribing practices.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Delayed-Action Preparations / pharmacokinetics
  • Diabetes Mellitus, Type 2 / drug therapy*
  • Drug Administration Schedule
  • Drug Monitoring / methods
  • Glucagon-Like Peptide 1 / administration & dosage
  • Glucagon-Like Peptide 1 / analogs & derivatives*
  • Glucagon-Like Peptide 1 / pharmacokinetics
  • Humans
  • Hypoglycemia / prevention & control
  • Hypoglycemic Agents / administration & dosage
  • Hypoglycemic Agents / pharmacokinetics*
  • Randomized Controlled Trials as Topic

Substances

  • Delayed-Action Preparations
  • Hypoglycemic Agents
  • rGLP-1 protein
  • Glucagon-Like Peptide 1