Small molecule
PubChem CID 10096344
Linagliptin
Tradjenta
- Mechanism of action
- DPP-4 inhibitor, increases active incretin hormone levels
- In plain language
- Blocks an enzyme called DPP-4 that normally breaks down the body's own after-meal, insulin-boosting hormones, so those hormones stick around longer and help the pancreas release more insulin when blood sugar is high.
- How it works
- Linagliptin (Tradjenta) is a dipeptidyl peptidase-4 (DPP-4) inhibitor. Per the FDA label, it inhibits DPP-4, the enzyme that normally degrades the incretin hormones GLP-1 and GIP, increasing the concentrations of these active incretin hormones. This stimulates insulin release from pancreatic beta cells in a glucose-dependent manner and decreases glucagon secretion from pancreatic alpha cells, reducing hepatic glucose output. Linagliptin binds to DPP-4 reversibly and selectively, without significant activity against the related enzymes DPP-8 or DPP-9 at therapeutic exposures.
- Therapeutic applications
- Linagliptin is FDA-indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. It is not recommended for patients with type 1 diabetes mellitus and has not been studied in patients with a history of pancreatitis.
- Class
- Small molecule
- Therapeutic area
- Metabolic / Diabetes
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