DPP‐4 inhibitors and their potential role in the management of type 2 diabetes

  title={DPP‐4 inhibitors and their potential role in the management of type 2 diabetes},
  author={Anthony H. Barnett},
  journal={International Journal of Clinical Practice},
  • A. Barnett
  • Published 1 November 2006
  • Medicine, Biology
  • International Journal of Clinical Practice
The dipeptidyl peptidase 4 (DPP‐4) inhibitors enhance the body's own ability to control blood glucose by increasing the active levels of incretin hormones in the body. Their mechanism of action is distinct from any existing class of oral glucose‐lowering agents. They control elevated blood glucose by triggering pancreatic insulin secretion, suppressing pancreatic glucagon secretion, and signalling the liver to reduce glucose production. The leading DPP‐4 inhibitors have shown clinically… 

DPP4 Inhibitors: a new approach in diabetes treatment

This review article focuses on the two leading agents of this category (sitagli leptin and vildagliptin), providing an overview of their function along with the latest data regarding their clinical efficacy as antidiabetic agents.

DPP-4 İnhibitörleri ve Diabetes Mellitus Tedavisi

Results of the recent studies show that DPP-4 inhibitors stimulate insulin secretion and inhibit glucagon secretion, and in the light of studies pancreatic β-cell mass can be increased by both proliferation and inhibition of apoptosis.

DPP-4 inhibitors.

  • B. Ahrén
  • Medicine, Biology
    Best practice & research. Clinical endocrinology & metabolism
  • 2007

Dipeptidyl Peptidase (DPP)-IV Inhibitors with Antioxidant Potential Isolated from Natural Sources: A Novel Approach for the Management of Diabetes

DPP-IV inhibitors improve hyperglycemic conditions by stabilizing the postprandial level of gut hormones such as glucagon-like peptide-1, and glucose-dependent insulinotropic polypeptides, which function as incretins to help upregulate insulin secretion and β-cell mass.

Dipeptidyl peptidase-4 inhibitors and the management of type 2 diabetes mellitus

Dipeptidyl peptidase-4 inhibitors appear to improve islet function and may modify the course of diabetes; this, however, must be confirmed with long-term controlled studies to demonstrate sustained glycemic control that translates into β-cell preservation.

Type 2 Diabetes Comorbidities and Treatment Challenges: Rationale for DPP-4 Inhibitors

On the basis of their clinical profiles, the DPP-4 inhibitors are emerging as an attractive option for improving glycemic control in patients with type 2 diabetes with a lower risk of hypoglycemia, weight-neutral effects, and a low propensity for drug-drug interactions.

Saxagliptin: a dipeptidyl peptidase-4 inhibitor for the treatment of type 2 diabetes mellitus.

  • Joshua J. NeumillerR. Campbell
  • Medicine, Biology
    American journal of health-system pharmacy : AJHP : official journal of the American Society of Health-System Pharmacists
  • 2010
Saxagliptin, a DPP-4 inhibitor approved for the treatment of type 2 diabetes, demonstrated safety and efficacy in lowering HbA(1c), FPG, and PPG levels as both monotherapy and in combination with other oral antidiabetic medications.


The production of glucagon-like peptide 1 (GLP-1), an incretin hormone, has been shown to be abnormally low in patients with type 2 diabetes, suggesting that GLP-1 may be a contributor in the

Saxagliptin: a new DPP-4 inhibitor for the treatment of type 2 diabetes mellitus

Saxagliptin is a novel DPP-4 inhibitor that has recently completed phase 3 studies and will be a new effective drug in the currently available variety of antidiabetic medications for patients with T2DM.

DPP-4 Inhibitors in Clinical Practice

The scientific background for incretin-based therapy and the available evidence regarding the role and efficacy of DPP-4 inhibitors in the treatment of patients with type 2 diabetes are reviewed.



Enhancing incretin action for the treatment of type 2 diabetes.

The need for daily injections of potentially immunogenic GLP-1-derived peptides and the potential for unanticipated side effects with chronic use of DPP-IV inhibitors will require ongoing scrutiny of the risk-benefit ratio for these new therapies as they are evaluated in the clinic.

Applications of dipeptidyl peptidase IV inhibitors in diabetes mellitus.

Effect of single oral doses of sitagliptin, a dipeptidyl peptidase-4 inhibitor, on incretin and plasma glucose levels after an oral glucose tolerance test in patients with type 2 diabetes.

In patients with type 2 diabetes, near maximal glucose-lowering efficacy of sitagliptin after single oral doses was associated with inhibition of plasma DPP-4 activity of 80% or greater, corresponding to a plasma sitgliptin concentration of 100 nm or greater and an augmentation of active GLP-1 and GIP levels of 2-fold or higher after an OGTT.

Dipeptidyl peptidase IV inhibitor treatment stimulates β-cell survival and islet neogenesis in streptozotocin-induced diabetic rats

In vitro studies using a β-(INS-1) cell line showed a dose-dependent prevention of STZ-induced apoptotic cell-death by both GIP and GLP-1, supporting a role for the incretins in eliciting the in vivo results.

Inhibition of dipeptidyl peptidase IV with NVP-DPP728 increases plasma GLP-1 (7–36 amide) concentrations and improves oral glucose tolerance in obese Zucker rats

The improvement observed in prandial glucose homeostasis during DPP-IV inhibition suggests that inhibition of this enzyme is a promising treatment for Type II diabetes.

Inhibition of dipeptidyl peptidase-4 reduces glycemia, sustains insulin levels, and reduces glucagon levels in type 2 diabetes.

Improved metabolic control by DPP-4 inhibition in type 2 diabetes is seen in association with reduced glucagon levels and, despite the lower glycemia, unaltered insulin levels.

Pharmacokinetics and Pharmacodynamic Effects of the Oral DPP‐4 Inhibitor Sitagliptin in Middle‐Aged Obese Subjects

In nondiabetic obese subjects, treatment with sitagliptin 200 mg bid was generally well tolerated without associated hypoglycemia and led to maximal inhibition of plasma DPP‐4 activity, increased active GLP‐1, and reduced glycemic excursion.

Twelve-week monotherapy with the DPP-4 inhibitor vildagliptin improves glycemic control in subjects with type 2 diabetes.

Monotherapy with vildagliptin is well tolerated and improves glycemic control in diet-treated subjects with type 2 diabetes, and concurrent improvements in beta-cell function were also observed.

Vildagliptin, a dipeptidyl peptidase-IV inhibitor, improves model-assessed beta-cell function in patients with type 2 diabetes.

Vildagliptin is an incretin degradation inhibitor that improves beta-cell function in diabetic patients by increasing the insulin secretory tone.

Improved glycaemic control with dipeptidyl peptidase‐4 inhibition in patients with type 2 diabetes: vildagliptin (LAF237) dose response

This study was designed to establish a dose of the DPP‐4‐inhibitor vildagliptin (LAF237) that was effective in reducing HbA1c levels and was safe and well tolerated in patients with type 2 diabetes.