- Advanced search
- Guide to IMMUNOPHARMACOLOGY Portal
Ligand id: 6318
View more information in the IUPHAR Pharmacology Education Project: linagliptin
Molecular properties generated using the CDK
|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)