Linagliptin
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| Pronunciation | LIN-a-GLIP-tin |
| Trade names | Tradjenta, Trajenta |
| AHFS/Drugs.com | Consumer Drug Information |
| MedlinePlus | a611036 |
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| Routes of administration |
By mouth (tablets) |
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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 |
| Biological half-life | ~12 hours |
| Excretion | Feces (80%), urine (5%) |
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| Formula | C25H28N8O2 |
| Molar mass | 472.54 g/mol |
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Linagliptin (INN, previously known as BI-1356, marketed under trade names Tradjenta (U.S.) and Trajenta (worldwide)) is a dipeptidyl peptidase-4 inhibitor developed by Boehringer Ingelheim for treatment of diabetes mellitus type 2.
Once-daily linagliptin was approved by the U.S. Food and Drug Administration (FDA) on 2 May 2011 for treatment of type 2 diabetes. It is being marketed by Boehringer Ingelheim and Lilly.
Results in 2010 from a Phase III clinical trial of linagliptin showed that the drug can effectively reduce blood sugar.
Linagliptin may cause severe joint pain.
Linagliptin belongs to a class of drugs called DPP-4 inhibitors. They work by increasing hormones that stimulate pancreas to produce more insulin and stimulate your liver to produce less glucose. In other words, linagliptin, along with diet and exercise, can help the body produce more insulin and less sugar. Managing blood sugar can mean a lower HbA1c, a primary treatment goal in type 2 diabetes.
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