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Dipeptidyl Peptidase 4 Inhibitors

Dipeptidyl Peptidase 4 Inhibitors

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...

Glucagon-like Receptor Agonists

Glucagon-like Receptor Agonists

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...

Oral Hypoglycemic Agents: Glinides

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Oral Hypoglycemic Agents: Biguanides and Glitazones

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Oral Hypoglycemic Agents: Sulfonylureas

Oral Hypoglycemic Agents: Sulfonylureas

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Related Experiment Video

Updated: Jun 1, 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 enhancer: sitagliptin].

Manabu Kondo¹, Yukio Tanizawa

¹Division of Endocrinology, Metabolism, Hematological Science and Therapeutics, Department of Bio-Signal Analysis, Yamaguchi University Graduate School of Medicine.

Nihon Rinsho. Japanese Journal of Clinical Medicine

|May 21, 2011

Summary

Sitagliptin, a DPP-4 inhibitor, increases active GLP-1 in type 2 diabetes patients. Long-term effectiveness and safety, especially with sulfonylureas, require further evaluation in Japan.

Area of Science:

Endocrinology
Pharmacology

Context:

Incretin-based therapies, including dipeptidyl peptidase-4 (DPP-4) inhibitors like sitagliptin, are now available for type 2 diabetes management in Japan.
Sitagliptin enhances the action of endogenous glucagon-like peptide-1 (GLP-1), a key incretin hormone.

Purpose:

To evaluate the efficacy and safety profile of sitagliptin in the Japanese type 2 diabetes population.
To assess the impact of sitagliptin on active GLP-1 levels and its effectiveness in monotherapy and combination treatments.

Summary:

Sitagliptin treatment approximately doubles active endogenous GLP-1 concentrations post-oral glucose tolerance test (OGTT).
Clinical trials indicate sitagliptin is effective as monotherapy and in combination with other oral antidiabetic agents.
While monotherapy with sitagliptin did not increase hypoglycemia, caution is advised in Japan due to reported severe events with sulfonylureas, particularly in elderly patients.

Related Experiment Videos

Last Updated: Jun 1, 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

Impact:

Sitagliptin represents a novel therapeutic option for Japanese patients with type 2 diabetes, offering potential glycemic control benefits.
Further long-term studies are necessary to fully establish the sustained efficacy and safety of sitagliptin in this specific demographic, considering potential drug interactions.