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Glucagon-like Receptor Agonists

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Incretins include glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which stimulate insulin secretion post-meals. In type 2 diabetes, GIP's efficacy is reduced, making GLP-1 a viable drug target. GIP originates from preproGIP.
GLP-1, when administered in high doses intravenously, triggers insulin secretion, inhibits glucagon release, slows gastric emptying, reduces food intake, and restores normal insulin secretion. However, its rapid inactivation by the...

Dipeptidyl Peptidase 4 Inhibitors

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Dipeptidyl peptidase 4 (DPP-4) is a serine protease widely distributed in the body. It's involved in the inactivation of GLP-1 and GIP hormones, which are crucial for insulin regulation. DPP-4 inhibitors, such as sitagliptin (Januvia), saxagliptin (Onglyza), linagliptin (Tradjenta), alogliptin (Nesina), and vildagliptin (Galvus), help increase the proportion of active GLP-1, enhancing insulin secretion. These inhibitors work by competitively binding to DPP-4. This binding causes a significant...

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Updated: Jun 10, 2026

Homogeneous Time-resolved Förster Resonance Energy Transfer-based Assay for Detection of Insulin Secretion

Homogeneous Time-resolved Förster Resonance Energy Transfer-based Assay for Detection of Insulin Secretion

Published on: May 10, 2018

Incretin agents in type 2 diabetes.

Stuart A Ross¹, Jean-Marie Ekoé

¹University Of Calgary, AB, Canada. drross@telus.net

Canadian Family Physician Medecin De Famille Canadien

|July 16, 2010

Summary

Incretin pathway agents, including glucagon-like peptide 1 (GLP1) receptor agonists and dipeptidyl peptidase 4 (DPP4) inhibitors, effectively lower blood sugar in type 2 diabetes patients without increasing hypoglycemia risk.

Area of Science:

Endocrinology and Metabolism
Pharmacology
Diabetes Research

Background:

Type 2 diabetes mellitus (T2DM) management requires effective antihyperglycemic agents.
The incretin pathway plays a crucial role in glucose homeostasis.
Emerging therapies targeting the incretin pathway offer new treatment avenues.

Purpose of the Study:

To evaluate the therapeutic efficacy and side effect profiles of incretin pathway agents.
To determine the optimal place of these agents in T2DM treatment algorithms.
To compare glucagon-like peptide 1 (GLP1) receptor agonists and dipeptidyl peptidase 4 (DPP4) inhibitors.

Main Methods:

Systematic literature search of MEDLINE, EMBASE, and Cochrane Database of Systematic Reviews.
Analysis of evidence primarily from Level I and II studies.

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Hyperinsulinemic-euglycemic Clamps in Conscious, Unrestrained Mice

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Homogeneous Time-resolved Förster Resonance Energy Transfer-based Assay for Detection of Insulin Secretion

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Published on: May 10, 2018

Hyperinsulinemic-euglycemic Clamps in Conscious, Unrestrained Mice

Hyperinsulinemic-euglycemic Clamps in Conscious, Unrestrained Mice

Published on: November 16, 2011

Evaluation of clinical trial data on incretin-based therapies.

Main Results:

GLP1 receptor agonists and DPP4 inhibitors significantly reduce hyperglycemia without increasing hypoglycemia risk.
GLP1 receptor agonists demonstrate greater glycated hemoglobin A1c reduction and promote weight loss.
DPP4 inhibitors are weight-neutral.

Conclusions:

Incretin agents (GLP1 receptor agonists and DPP4 inhibitors) are valuable additions to T2DM treatment.
These agents can be used as add-on therapy to metformin or as initial treatment when metformin is contraindicated.
Their distinct profiles allow for tailored patient management.