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Special Review
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Korean J Med. 2014;87(1):1-8. Published online July 1, 2014.
DOI: https://doi.org/10.3904/kjm.2014.87.1.1
- Dipeptidyl Peptidase-4 (DPP-4) 억제제
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이대호
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원광대학교 의과대학 내과학교실
- Dipeptidyl Peptidase-4 Inhibitor
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Dae Ho Lee
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Department of Internal Medicine, Wonkwang University School of Medicine and Hospital, Iksan, Korea
- Corresponding author: Dae Ho Lee ,Tel: +82-63-859-2602, Fax: +82-63-855-2025, Email: drhormone@naver.com
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- Abstract
- Recent advances in incretin biology have led to the development of a new class of oral anti-diabetic drugs. To date, there are two
known incretin hormones, glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), of which the
former is a more important therapeutic target for type 2 diabetes. GLP-1 is secreted by intestinal L-cells in response to oral nutrient
intake, and it stimulates insulin secretion and suppresses glucagon secretion in a glucose-dependent manner. However, both GLP-1
and GIP are rapidly degraded by dipeptidyl peptidase-4 (DPP-4), a multifunctional type II transmembrane glycoprotein. Thus,
several DPP-4 inhibitors with different pharmacologic features are now available and can be used either as monotherapy or in
combination with other anti-diabetic agents for the treatment of type 2 diabetes. In both therapeutic regimens, DPP-4 inhibitors
have been shown to reduce hemoglobin A1c levels by approximately 0.5-0.8%. In clinical trials, DPP-4 inhibitors were generally
well-tolerated, posed a low risk of hypoglycemia, and did not increase body weight. Despite some reports of a possible increased
risk of pancreatitis with GLP-1 receptor agonists and DPP-4 inhibitors, no causal associations have been found. Recent randomized
controlled clinical trials have shown that DPP-4 inhibitors did not increase or decrease the rates of major adverse cardiovascular
events in patients with type 2 diabetes at high risk of cardiovascular disease, even though this class of anti-diabetic agents had
various salutary effects in many studies involving animals or healthy and diabetic humans. Additional studies will be required to
resolve these disparate conclusions.
Keywords :Incretin, Glucagon-like peptide-1, Glucose-dependent insulinotropic polypeptide, Dipeptidyl peptidase-4 inhibitor,
Type 2 diabetes
