Sitagliptin

Sitagliptin is an oral dipeptidyl peptidase-4 inhibitor used to improve blood sugar control in adults with type 2 diabetes. It prolongs the activity of incretin hormones that stimulate glucose-dependent insulin release.

Dipeptidyl peptidase-4: Dipeptidyl peptidase-4 is an enzyme that rapidly inactivates incretin hormones and other signaling peptides. Sitagliptin inhibits this enzyme, slowing the breakdown of GLP-1 and GIP.
Type 2 diabetes: Type 2 diabetes is a chronic metabolic disease characterized by insulin resistance and insufficient insulin secretion. Sitagliptin is prescribed to improve glycemic control in this condition.
GLP-1 receptor agonist: A GLP-1 receptor agonist is a medicine that activates the receptor for glucagon-like peptide-1. Unlike sitagliptin, these drugs directly activate the receptor and often produce greater weight loss.
Incretin: An incretin is a gut-derived hormone that enhances insulin secretion in response to nutrient intake. Sitagliptin was developed to preserve the body's naturally produced incretins.
TECOS: TECOS was a randomized trial assessing cardiovascular outcomes with sitagliptin in people with type 2 diabetes and cardiovascular disease. The trial found cardiovascular safety without demonstrating cardiovascular risk reduction.
Incretin effect: The incretin effect is the greater insulin response to oral glucose than to an equivalent amount of intravenous glucose. Sitagliptin strengthens this meal-linked hormonal amplification of insulin release.
Metformin: Metformin is an oral glucose-lowering medicine that reduces hepatic glucose production and improves insulin sensitivity. It is a common first-line treatment that may be continued when sitagliptin is added.
Sodium-glucose cotransporter 2 inhibitor: A sodium-glucose cotransporter 2 inhibitor lowers blood glucose by increasing urinary glucose excretion. This class lowers glucose through the kidneys rather than by preserving incretin hormones.
DPP-4 inhibitor: A DPP-4 inhibitor is a medicine that slows enzymatic degradation of incretin hormones. Sitagliptin was the first widely marketed member of this oral drug class.
Cardiovascular safety of diabetes medications: Cardiovascular safety of diabetes medications concerns their effects on cardiovascular events and mortality. Sitagliptin was studied under regulatory requirements for cardiovascular risk assessment.

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