Abstract

The glucagon-like peptide-1 receptor (GLP-1R) agonists and dipeptidyl peptidase-4 (DPP-4) inhibitors have become important options for the management of patients with type 2 diabetes mellitus. While the GLP-1R agonists and DPP-4 inhibitors act on the incretin system to regulate glucose homeostasis, there are important clinical differences among the five agents currently available in the U.S. For example, the GLP-1R agonists require subcutaneous administration, produce pharmacological levels of GLP-1 activity, promote weight loss, have a more robust glucose-lowering effect, and have a higher incidence of adverse gastrointestinal effects. In contrast, the DPP-4 inhibitors are taken orally, increase the half-life of endogenous GLP-1, are weight neutral, and are more commonly associated with nasopharyngitis. Differences in efficacy, safety, tolerability, and cost among the incretin-based therapies are important to consider in the primary care management of patients with type 2 diabetes mellitus.

Highlights

  • Treating patients with type 2 diabetes mellitus (T2DM) can be very challenging

  • Were considered by the American Diabetes Association/ European Society for the Study of Diabetes (ADA/EASD) [2] and by the American Association of Clinical Endocrinologists/American College of Endocrinology (AACE/ ACE) [3] when developing their 2009 guideline recommendations. Both groups concluded that, based upon their unique physiologic activity, efficacy, nonglycemic benefits, and safety profiles, agents which act on the incretin system–the glucagon-like peptide-1 (GLP-1R) agonists and dipeptidyl peptidase-4 (DPP-4) inhibitors– are important options for the management of patients with T2DM

  • Postprandial glucose Reduction in the A1C level observed with the glucagon-like peptide-1 receptor (GLP-1R) agonists and DPP-4 inhibitors appears to result primarily from the generally greater reduction of the postprandial glucose (PPG) level compared to the Fasting plasma glucose (FPG) level (Table 1) [23,26,37,45,52]

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Summary

Introduction

Treating patients with type 2 diabetes mellitus (T2DM) can be very challenging. new treatment options for T2DM, such as incretin-based agents, provide new opportunities to bring the disease under control, and perhaps slow its progression. When administered as monotherapy or in combination with metformin or other glucose-lowering therapy, the GLP-1R agonists reduce the A1C level by 0.5% to 1.5% [29,36,37,38,39,40,41] and the DPP-4 inhibitors by 0.5% to 0.9% [22,23,24,26,42,43,44,45].

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