Haworth projection (bottom)
|Trade names||Forxiga, Farxiga, others|
|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)|
|Elimination half-life||~12.9 hours|
|Excretion||Urine (75%), feces (21%):5|
|Chemical and physical data|
|Molar mass||408.873 g/mol g·mol−1|
|3D model (JSmol)|
|(what is this?)|
Dapagliflozin, sold under the brand name Farxiga among others, is a medication used to treat type 2 diabetes. It is of the gliflozin class. It was developed by Bristol-Myers Squibb in partnership with AstraZeneca.
Dapagliflozin used to improve glycemic control, along with diet and exercise, in adults with type 2 diabetes. SGLT2 inhibitors, including dapagliflozin, reduce the likelihood of hospitalization for congestive heart failure or progression of renal disease in persons with diabetes mellitus type 2 and reduce the likelihood of stroke and heart attack in persons with diabetes mellitus type 2 who have known atherosclerotic vascular disease.
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). Rarely, use of a SGLT2 drug, including dapagliflozin, is associated with necrotizing fasciitis of the perineum, also called Fournier gangrene.
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.
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