Synonyms: BMS-512148 | Farxiga® | Forxiga®
dapagliflozin is an approved drug (EMA (2012), FDA (2014))
Compound class:
Synthetic organic
Comment: Dapagliflozin is a derivative of naturally occurring dihydrocholine glucoside. It acts as a sodium-glucose cotransporter 2 (SGLT-2) inhibitor. In addition to clinical efficacy in type 2 diabetes, evidence from clinical trial suggests that dapagliflozin is of benefit in treating heart failure with or without type 2 diabetes as a comorbidity [7].
SARS-CoV-2 and COVID-19: Based on the cardio- and renoprotective benefits of dapagliflozin in T2DM patients, it was evaluated vs. placebo in 1250 hospitalised COVID-19 patients (NCT04350593) [4], to determine if it would provide similar protection from organ damage caused by SARS-CoV-2 infection. The drug treatment effected a non-significant reduction in the risk of organ failure or death [5]. Subsequent to this finding, another approved SGLT2 inhibitor empagliflozin was added to the RECOVERY trial. Ligand Activity Visualisation ChartsThese 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: dapagliflozin |
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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 [7]. Clinical trial NCT03619213 is evaluating whether this efficacy is retained in patients with heart failure and preserved ejection fraction. In July 2021, the FDA approved dapagliflozin as a therapy for chronic kidney disease [1-2], based on evidence from the DAPA-CKD trial (NCT03036150) [8]. |
Clinical Trials | |||||
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 | ||
NCT04350593 | Dapagliflozin in Respiratory Failure in Patients With COVID-19 | Phase 3 Interventional | Saint Luke's Health System | 5 | |
NCT03036150 | A Study to Evaluate the Effect of Dapagliflozin on Renal Outcomes and Cardiovascular Mortality in Patients With Chronic Kidney Disease | Phase 3 Interventional | AstraZeneca | 8 |
External links |
For extended ADME data see the following: Electronic Medicines Compendium (eMC) Drugs.com European Medicines Agency (EMA) |