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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 |
| Eliminationhalf-life | ~24 hours |
| Excretion | Feces (80%),urine (5%)[6] |
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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 nameTradjenta among others, is amedication used to treattype 2 diabetes (but not type 1) in conjunction with exercise and diet.[8][9] Linagliptin is adipeptidyl peptidase-4 inhibitor[8] that works by increasing the production ofinsulin and decreasing the production ofglucagon by thepancreas.[8] It is generally less preferred thanmetformin andsulfonylureas as an initial treatment.[8][10] It is takenby mouth.[8]
Commonside effects include inflammation of the nose and throat.[8] Serious side effects may includeangioedema,pancreatitis,joint pain.[10][8] Use inpregnancy andbreastfeeding is not recommended.[10]
Linagliptin was approved for medical use in the United States,[11] Japan, the European Union, Canada, and Australia in 2011.[8][12] In 2020, it was the 293rd most commonly prescribed medication in the United States, with more than 1 million prescriptions.[13][14] From August 2021 linagliptin became available as ageneric medicine in the US.[15]
Linagliptin isindicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes.[6]
Linagliptin may cause severe joint pain.[6][16]
Linagliptin belongs to a class of drugs calledDPP-4 inhibitors.[6]
Linagliptin is theinternational nonproprietary name (INN).[17] Brand names: Trajenta,[18] Tradjenta.
