Linagliptin
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| Systematic (IUPAC) name | |
| 8-[(3R)-3-aminopiperidin-1-yl]-7-(but-2-yn-1-yl)-3- methyl-1-[(4-methylquinazolin-2-yl)methyl]-3,7-dihydro-1H-purine-2,6-dione | |
| Clinical data | |
| Trade names | Tradjenta, Trajenta |
| AHFS/Drugs.com | Consumer Drug Information |
| MedlinePlus | a611036 |
| Licence data | EMA:Link, US FDA:link |
| Pregnancy cat. | B (US) |
| Legal status | ℞-only (US) |
| Routes | Oral |
| Identifiers | |
| CAS number | 668270-12-0  |
| ATC code | A10BH05 |
| PubChem | CID 10096344 |
| UNII | 3X29ZEJ4R2 |
| KEGG | D09566 |
| ChEMBL | CHEMBL237500  |
| Chemical data | |
| Formula | C25H26N8O2 |
| Mol. mass | 472.54 g/mol |
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Linagliptin (BI-1356, trade names Tradjenta and Trajenta) is a DPP-4 inhibitor developed by Boehringer Ingelheim for treatment of type II diabetes.
Linagliptin (once-daily) was approved by the US FDA on 2 May 2011 for treatment of type II diabetes.[1] It is being marketed by Boehringer Ingelheim and Lilly.
[edit] Mechanism of action
Linagliptin is an inhibitor of DPP-4, an enzyme that degrades the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). Both GLP-1 and GIP increase insulin biosynthesis and secretion from pancreatic beta cells in the presence of normal and elevated blood glucose levels. GLP-1 also reduces glucagon secretion from pancreatic alpha cells, resulting in a reduction in hepatic glucose output. Thus, linagliptin stimulates the release of insulin in a glucose-dependent manner and decreases the levels of glucagon in the circulation.
[edit] Clinical trials
Results in 2010 from a Phase III clinical trial of linagliptin showed that the drug can effectively reduce blood sugar.[2]
[edit] References
- H. Spreitzer (September 1, 2008). "Neue Wirkstoffe - BI-1356" (in German). Österreichische Apothekerzeitung (18/2008): 918.
- Wang, Y, Serradell, N, Rosa, E, Castaner, R (2008). "BI-1356". Drugs of the Future 33 (6): 473–477. doi:10.1358/dof.2008.033.06.1215244.
- ^ "FDA Approves Type 2 Diabetes Drug from Boehringer Ingelheim and Lilly". 3 May 2011. http://www.genengnews.com/gen-news-highlights/fda-approves-type-2-diabetes-drug-from-boehringer-ingelheim-and-lilly/81245092/.
- ^ "Four Phase III Trials Confirm Benefits of BI’s Oral, Once-Daily Type 2 Diabetes Therapy". Genetic Engineering & Biotechnology News. 28 June 2010. http://www.genengnews.com/gen-news-highlights/four-phase-iii-trials-confirm-benefits-of-bi-s-oral-once-daily-type-2-diabetes-therapy/81243585/.
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