linagliptin

Ligand id: 6318

Name: linagliptin

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 10
Hydrogen bond donors 1
Rotatable bonds 4
Topological polar surface area 113.48
Molecular weight 472.23
XLogP 2.6
No. Lipinski's rules broken 0

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.