Haworth projection (bottom)
|Trade names||Forxiga, Farxiga|
|AHFS/Drugs.com||UK Drug Information|
|By mouth (tablets)|
|Bioavailability||78% (after 10 mg dose)|
|Metabolism||UGT1A9 (major), CYP (minor)|
|Metabolites||Dapagliflozin 3-O-glucuronide (inactive)|
|Biological half-life||~12.9 hours|
|Excretion||Urine (75%), feces (21%):5|
|Chemical and physical data|
|Molar mass||408.873 g/mol|
|3D model (JSmol)|
|(what is this?)|
Dapagliflozin (INN, USAN, trade name Farxiga // far-SEE-gə in the U.S. and Forxiga in the EU and Russia) is a drug of the gliflozin class, used to treat type 2 diabetes. It was developed by Bristol-Myers Squibb in partnership with AstraZeneca.
The FDA approved dapagliflozin on January 8, 2014 for glycemic control, along with diet and exercise, in adults with type 2 diabetes.
Since dapagliflozin leads to heavy glycosuria (sometimes up to about 70 grams per day) it can lead to rapid weight loss and tiredness. The glucose acts as an osmotic diuretic (this effect is the cause of polyuria in diabetes) which can lead to dehydration. The increased amount of glucose in the urine can also worsen the infections already associated with diabetes, particularly urinary tract infections and thrush (candidiasis). Dapagliflozin is also associated with hypotensive reactions. There are concerns it may increase the risk of diabetic ketoacidosis.
Mechanism of action
Dapagliflozin inhibits subtype 2 of the sodium-glucose transport proteins (SGLT2) which are responsible for at least 90% of the glucose reabsorption in the kidney. Blocking this transporter mechanism causes blood glucose to be eliminated through the urine. In clinical trials, dapagliflozin lowered HbA1c by 0.6 versus placebo percentage points when added to metformin.
- "Farxiga (dapagliflozin) Tablets, for Oral Use. Full Prescribing Information" (PDF). AstraZeneca Pharmaceuticals. Retrieved 15 November 2016.
- "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names: List 59" (PDF). World Health Organization. 2008. p. 50. Retrieved 15 November 2016.
- "Statement on a Nonproprietary Name Adopted by the USAN Council" (PDF). American Medical Association. Archived from the original (PDF) on 7 February 2012. Retrieved 15 November 2016.
- "FDA Panel Advises Against Approval of Dapagliflozin". Healio. 19 July 2011.
- "FDA Approves Farxiga to Treat Type 2 Diabetes". Food and Drug Administration. 8 January 2014. Retrieved 15 November 2016.
- "Forxiga EPAR summary for the public" (PDF). European Medicines Agency. 12 November 2012.
- Drugs.com: International Drug Names for Forxiga.
- "US FDA Approves Once-Daily Xigduo™ XR Tablets for Adults with Type 2 Diabetes". www.astrazeneca.com. AstraZeneca. 30 October 2014.
- "Safety Alerts for Human Medical Products — SGLT2 inhibitors: Drug Safety Communication — FDA Warns Medicines May Result in a Serious Condition of Too Much Acid in the Blood". Food and Drug Administration. 15 May 2015. Retrieved 15 November 2016.
- Prous Science: Molecule of the Month November 2007
- UEndocrine: Internet Endocrinology Community
- Schubert-Zsilavecz, M, Wurglics, M, Neue Arzneimittel 2008/2009
- Efficacy and Safety of Dapagliflozin, Added to Therapy of Patients With Type 2 Diabetes With Inadequate Glycemic Control on Insulin, ClinicalTrials.gov, April 2009
- Trial Details for Trial MB102-020, Bristol-Myers Squibb, May 2009