Linagliptin

Linagliptin

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
AHFS/Drugs.com	Consumer Drug Information
MedlinePlus	a611036
Licence data	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 Y
KEGG	D09566 Y
Chemical data
Formula	C25H26N8O2
Mol. mass	472.54 g/mol
Y(what is this?)  (verify)

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.

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.

Clinical trials

Results in 2010 from a Phase III clinical trial of linagliptin showed that the drug can effectively reduce blood sugar.^[2]

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. 

1. ^ "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/. 
2. ^ "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/. 

This drug article relating to the gastrointestinal system is a stub. You can help Wikipedia by expanding it.v · Categories: Dipeptidyl peptidase-4 inhibitors Alkynes Piperidines Quinazolines Purines Gastrointestinal system drug stubs Wikimedia Foundation. 2010. Игры ⚽ Нужно сделать НИР? Gellért Hill Calvary Stavropol (disambiguation) Look at other dictionaries: Linagliptin —   Strukturformel Allgemeines Freiname Linagliptin Andere Namen …   Deutsch Wikipedia Development of dipeptidyl peptidase-4 inhibitors — Dipeptidyl peptidase 4 inhibitors (DPP 4 inhibitors) are enzyme inhibitors that inhibit the enzyme dipeptidyl peptidase 4 (DPP 4) and are a potent treatment for type 2 diabetes. Inhibition of the DPP 4 enzyme prolongs and enhances the activity of …   Wikipedia Dipeptidyl peptidase-4 inhibitor — DPP 4 inhibitors and GLP 1 Inhibitors of dipeptidyl peptidase 4, also DPP 4 inhibitors or gliptins, are a class of oral hypoglycemics that block DPP 4. They can be used to treat diabetes mellitus type 2. The first agent of the class sitagliptin… …   Wikipedia Anti-diabetic medication — Anti diabetic medications treat diabetes mellitus by lowering glucose levels in the blood. With the exceptions of insulin, exenatide, and pramlintide, all are administered orally and are thus also called oral hypoglycemic agents or oral… …   Wikipedia Glipizide — Not to be confused with gliclazide or glyburide. Glipizide Systematic (IUPAC) name N (4 [N (cyclohexylcarbamoyl)sulfamoyl]phenethyl) 5 methylpyrazine 2 carboxamide …   Wikipedia Glimepiride — Systematic (IUPAC) name 3 ethyl 4 methyl N (4 [N ((1r,4r) 4 methylcyclohexylcarbamoyl)sulfamoyl]phenethyl) 2 oxo 2,5 dihydro 1H pyrrole 1 carboxamide Clinical …   Wikipedia Metformin — Chemical structure (top) and ball and stick model (bottom) of metformin System …   Wikipedia Troglitazone — Systematic (IUPAC) name (RS) 5 (4 [(6 hydroxy 2,5,7,8 tetramethylchroman 2 yl)methoxy]benzyl)thiazolidine 2,4 dione Clinical data Pre …   Wikipedia Pioglitazone — Systematic (IUPAC) name (RS) 5 (4 [2 (5 ethylpyridin 2 yl)ethoxy]benzyl)thiazolidine 2,4 dione Clinical data …   Wikipedia Chlorpropamide — Systematic (IUPAC) name 4 chloro N (propylcarbamoyl)benzenesulfonamide Clinical data Trade names Diabin …   Wikipedia 18+ © Academic, 2000-2024 Contact us: Technical Support, Advertising Dictionaries export, created on PHP, Joomla, Drupal, WordPress, MODx. Mark and share Search through all dictionaries Translate… Search Internet Share the article and excerpts Direct link … Do a right-click on the link above and select “Copy Link”