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Synonyms: BI-1356 | Tradjenta®
linagliptin is an approved drug (EMA & FDA (2011))
Compound class: Synthetic organic
Comment: Linagliptin is a once-daily, oral dipeptidyl peptidase-4 (DPP-4) inhibitor class anti-diabetic drug.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
View more information in the IUPHAR Pharmacology Education Project: linagliptin
|No information available.|
|Summary of Clinical Use|
|Used in the management of type 2 diabetes.
Linagliptin was assessed in a combination therapy with the SGLT-2 inhibitor, empagliflozin with ClinicalTrials.gov ID NCT01734785. In February 2015, this translated to US FDA approval for the fixed dose formulation Glyxambi® (empagliflozin and linagliptin) for the treatment of type 2 diabetes.
In July 2016, the FDA approved a once-daily, extended release DPP-4 inhibitor/biguanide combination (Jentadueto XR®: linagliptin and metformin hydrochloride) as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes.
|Mechanism Of Action and Pharmacodynamic Effects|
|Competitively and reversibly inhibits dipeptidyl peptidase, the enzyme which catalyses the breakdown of GLP-1. The resulting elevation of GLP-1 levels leads to increased production and release of insulin from pancreatic beta cells and decreased release of glucagon from pancreatic alpha cell. This leads to a decrease in glucose production in the liver and an increase of insulin.|
For extended ADME data see the following:
Electronic Medicines Compendium (eMC)
European Medicines Agency (EMA)