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Ligand id: 4594
View more information in the IUPHAR Pharmacology Education Project: dapagliflozin
Molecular properties generated using the CDK
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.✖
|No information available.|
|Summary of Clinical Use|
|Approved to treat diabetes mellitus, type 2.
The fixed-dose drug Xigduo XR® contains dapagliflozin (as dapagliflozin propanediol monohydrate PubChem CID 56841155) and metformin hydrochloride.
Results have been published for trial NCT03036124 and these conclude that dapagliflozin reduced worsening heart failure or death from cardiovascular causes irrespective of diabetes status, in patients with heart failure and a reduced ejection fraction . Clinical trial NCT03619213 is evaluating whether this efficacy is retained in patients with heart failure and preserved ejection fraction.
|Mechanism Of Action and Pharmacodynamic Effects|
|Dapagliflozin inhibits sodium-glucose transport protein subtype 2 (SGLT2), which accounts for >90% of glucose reabsorption from the kidneys. Inhibition of this transporter leads to excretion of blood glucose into urine. Dapagliflozin is >1000 times more inhibitory at SGLT2 than SGLT1, meaning that its effects on intestinal glucose absorption are negligible. Although this drug could be equally effective in treating type 1 diabetes, its approval restricts use to type 2 disease.|
|Clinical Trial ID||Title||Type||Source||Comment||References|
|NCT03036124||Study to Evaluate the Effect of Dapagliflozin on the Incidence of Worsening Heart Failure or Cardiovascular Death in Patients With Chronic Heart Failure||Phase 3 Interventional||AstraZeneca|
|NCT03619213||Dapagliflozin Evaluation to Improve the LIVEs of Patients With PReserved Ejection Fraction Heart Failure.||Phase 3 Interventional||AstraZeneca|
For extended ADME data see the following:
Electronic Medicines Compendium (eMC)
European Medicines Agency (EMA)