Sitagliptin works to competitively inhibit the enzyme dipeptidyl peptidase 4 (DPP-4). This enzyme breaks down the incretins GLP-1 and GIP, gastrointestinal hormones released in response to a meal. [ 28 ]

Mechanism of action. Inhibition of DPP-4 by sitagliptin slows DPP-4 mediated inactivation of incretins like GLP-1 and GIP Label,2. Incretins are released throughout the day and upregulated in response to meals as part of glucose homeostasis Label,4.

May 22, 2023 · Mechanism of Action. DPP-4 is a ubiquitous enzyme that acts on incretin hormones, mainly GLP-1 (glucagon-like peptide-1) and GIP (gastric inhibitory peptide), which maintain glucose homeostasis by increasing insulin secretion and decreasing glucagon secretion.

Feb 10, 2020 · Mechanism of Action. Sitagliptin inhibits dipeptidyl peptidase-4 (DPP-4) enzyme resulting in prolonged active incretin levels.

Mar 2, 2007 · It stimulates insulin secretion when hyperglycemia is present and inhibits glucagon secretion. In clinical studies it is weight neutral. This article gives an overview of the mechanism of action, the pharmacology, and the clinical efficacy and safety of sitagliptin in …

In the current issue of the JCEM, Muscelli et al. (17) reexamine the mechanisms by which sitagliptin, a DPP-4 inhibitor, achieves its glucose-lowering effect. To do so, 50 subjects with type 2 diabetes were randomized to drug or placebo in a double-blind fashion after a 4-wk washout of other antihyperglycemic medication.

Sitagliptin (PubChem CID: 4369359) is a dipeptidyl peptidase-4 (DPP-4) inhibitor, while exendin-4 (PubChem CID: 56927919) is a glucagon-like peptide-1 (GLP-1) receptor agonist [173, 174]. The mechanism of action for both drugs is based on enhancing insulin secretion by the pancreatic beta cells, resulting in reduced blood glucose levels.

Apr 5, 2010 · Sitagliptin is a member of the gliptin class of antidiabetic medications. Its mechanism of action is through inhibition of dipeptidyl peptidase-4 (DPP-4), an enzyme that acts to degrade and inactivate glucagon-like peptide-1 (GLP-1).

Its mechanism of action involves inhibiting DPP-4, leading to increased levels of active incretins (GLP-1 and GIP). As a result, sitagliptin enhances glucose-dependent insulin secretion and suppresses glucagon release, thus improving glycemic control without causing hypoglycemia.

Mechanism of Action Sitagliptin inhibits dipeptidyl peptidase IV (DPP-IV) enzymes resulting in prolonged active incretin levels. Incretin hormones [eg, glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP)] regulate glucose homeostasis by increasing insulin synthesis and release from pancreatic beta cells and ...