Linagliptin
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| Pronunciation | /ˌlɪnəˈɡlɪptɪn/ LIN-ə-GLIP-tin |
| Trade names | Tradjenta, Trajenta, Trazenta |
| Other names | BI-1356 |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a611036 |
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| Routes of administration | By mouth |
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| Pharmacokinetic data | |
| Bioavailability | ~30% (Tmax = 1.5 hours) |
| Protein binding | 75–99% (concentration-dependent) |
| Metabolism | Minimal (~10% metabolized) |
| Metabolites | Pharmacologically inactive |
| Elimination half-life | ~24 hours |
| Excretion | Feces (80%), urine (5%) |
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| Chemical and physical data | |
| Formula | C25H28N8O2 |
| Molar mass | 472.553 g·mol−1 |
| 3D model (JSmol) | |
| Melting point | 202 °C (396 °F) |
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Linagliptin, sold under the brand name Tradjenta among others, is a medication used to treat type 2 diabetes (but not type 1) in conjunction with exercise and diet. Linagliptin is a dipeptidyl peptidase-4 inhibitor that works by increasing the production of insulin and decreasing the production of glucagon by the pancreas. It is generally less preferred than metformin and sulfonylureas as an initial treatment. It is taken by mouth.
Common side effects include inflammation of the nose and throat. Serious side effects may include angioedema, pancreatitis, joint pain. Use in pregnancy and breastfeeding is not recommended.
Linagliptin was approved for medical use in the United States, Japan, the European Union, Canada, and Australia in 2011. In 2020, it was the 293rd most commonly prescribed medication in the United States, with more than 1 million prescriptions. From August 2021 linagliptin became available as a generic medicine in the US.