empagliflozin

Ligand id: 4754

Name: empagliflozin

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Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 6
Hydrogen bond donors 4
Rotatable bonds 6
Topological polar surface area 108.61
Molecular weight 450.14
XLogP 2.9
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
After being assessed in clinical trials for the treatment of type 2 diabetes mellitus (T2DM) [1], either as mono- or combination therapy (with linagliptin or metformin for example), empagliflozin was approved in August 2014 for the improvement of glycemic control in adult patients alongside diet and exercise.
In February 2015 the US FDA approved the fixed dose formulation Glyxambi® (empagliflozin and linagliptin) for the treatment of T2DM. The EMA has granted marketing authorisation for the fixed-dose combination of empagliflozin plus metformin (Synjardy®) for the treatment of T2DM.
A postmarket clinical trial of more than 7,000 patients with T2DM and CV disease showed that empagliflozin reduces the risk of CV death (compared to placebo) as an add-on to standard of care diabetes and atherosclerotic CV disease therapies [5]. These findings led to FDA approval in Dec 2016 for empagliflozin to be used to reduce the risk of CV death in T2DM patients with CV disease.
Mechanism Of Action and Pharmacodynamic Effects
Empagliflozin is an inhibitor of the sodium glucose co-transporter-2 (gene symbol SLC5A2), a protein responsible for renal reabsorption of blood glucose. Inhibition of the transporter promotes urinary excretion of glucose [2,4].
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