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2000
Volume 24, Issue 10
  • ISSN: 1871-5273
  • E-ISSN: 1996-3181

Abstract

Sitagliptin is a dipeptidyl peptidase-IV inhibitor approved for treating type 2 diabetes mellitus. It increases the active form of incretin Glucagon-like Peptide-1 (GLP-1). The GLP-1 peptide prevents damage to neurons due to its anti-inflammatory and anti-apoptotic activities. This article summarizes the studies assessing the neuroprotective properties of sitagliptin, especially through the GLP-1 pathway. The outcomes of experimental research indicate that sitagliptin has a decreasing effect on inflammation response. Sitagliptin decreases proinflammatory factors, such as Glial Fibrillary Acidic Protein (GFAP), Nuclear factor kappa B (NF-κB), Tumor Necrosis Factor-α (TNF-α), and Interleukin-6 (IL-6). It also decreases glutamate levels, the primary excitatory neurotransmitter. Furthermore, sitagliptin shows antioxidative and antiapoptotic effects. Lastly, sitagliptin may provide a novel agent for the management of neurological disease.

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2025-04-14
2025-09-30

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/content/journals/cnsnddt/10.2174/0118715273367858250321124131
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Neuroprotective Effect of Sitagliptin beyond the Incretin Effect: A Narrative Review
CNS & Neurological Disorders - Drug Targets (Formerly Current Drug Targets - CNS & Neurological Disorders) 24, 743 (2025); https://doi.org/10.2174/0118715273367858250321124131
/content/journals/cnsnddt/10.2174/0118715273367858250321124131
/content/journals/cnsnddt/10.2174/0118715273367858250321124131
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  • Article Type:     Review Article
Keyword(s): Alzheimer's disease; glucagon-like peptide-1; inflammation; neuroprotection; oxidative stress; Sitagliptin

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