Pharmacological Insights into Dipeptidyl Peptidase-4 Inhibitors: Therapeutic Applications and Future Perspectives

Document Type : Review Article

Authors

1 Minia University Hospital, Minia, Egypt

2 Department of Pharmacology and Toxicology, Faculty of Pharmacy, Minia University, El-Minia, Egypt

Abstract

Dipeptidyl peptidase-4 inhibitors (DPP-4Is) are considered a fundamental group of oral hypoglycemic drugs that are extensively utilized in type 2 diabetes mellitus (T2DM) treatment, primarily by modulating incretin hormones to enhance glycemic control, a process that described as the incretin effect.
Accumulating experimental and clinical data suggest that these drugs have the ability to extend benefits beyond glucose lowering effect, exhibiting potential positive feedback on cardiovascular health, kidneys, and liver. It also possesses an interesting role in COVID-19 management and Alzheimer's disease. Beyond their well-established role in glycemic control, DPP-4 inhibitors may help to modulate other risk factors by offering organ protection, highlighting the importance of continued rigorous research in this area.
This review summarizes the published preclinical and clinical research discussing the pharmacological features of DPP-4Is, along with their safety profiles and potential side effects. Moreover, pharmacokinetic properties, mechanisms of action, and therapeutic applications of approved DPP-4Is, including Saxagliptin, Sitagliptin, Vildagliptin, Alogliptin and Linagliptin were also discussed in this review.

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International Journal of Applied Biochemistry and Molecular Biology
Volume 2, Issue 2
June 2025
Pages 104-125

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