Farxiga (Dapagliflozin) as an SGLT2 Inhibitor
Yes, Farxiga (dapagliflozin) is definitively an SGLT2 (sodium-glucose cotransporter 2) inhibitor that works by blocking glucose reabsorption in the kidneys, promoting urinary glucose excretion and thereby lowering blood glucose levels. 1
Mechanism of Action
Dapagliflozin specifically targets the SGLT2 protein expressed in the proximal renal tubules, which is responsible for the majority of glucose reabsorption from the tubular lumen. By inhibiting this transporter:
- It reduces reabsorption of filtered glucose, promoting urinary glucose excretion
- It reduces sodium reabsorption and increases sodium delivery to the distal tubule
- These effects influence several physiological functions including lowering pre- and afterload of the heart, downregulating sympathetic activity, and decreasing intraglomerular pressure 1
The FDA label clearly identifies dapagliflozin as an "inhibitor of SGLT2" that works through this specific mechanism 1.
Pharmacodynamic Effects
When administered to patients with type 2 diabetes:
- Dapagliflozin doses of 5-10 mg daily result in excretion of approximately 70 grams of glucose in urine per day at Week 12
- This urinary glucose excretion leads to increases in urinary volume
- The effect is dose-dependent, with near maximum glucose excretion observed at 20 mg daily 1
Classification Among SGLT2 Inhibitors
Dapagliflozin is classified as a highly selective SGLT2 inhibitor, similar to empagliflozin and ertugliflozin, in contrast to:
- Canagliflozin, which has lower selectivity for SGLT2
- Sotagliflozin, which is a dual SGLT1/SGLT2 inhibitor with significant affinity for both receptors 2
Clinical Applications
As an SGLT2 inhibitor, dapagliflozin (Farxiga) is FDA-approved for:
- Reducing the risk of sustained eGFR decline, end-stage kidney disease, cardiovascular death, and hospitalization for heart failure in adults with chronic kidney disease
- Reducing the risk of cardiovascular death, hospitalization for heart failure, and urgent heart failure visits in adults with heart failure
- Reducing the risk of hospitalization for heart failure in adults with type 2 diabetes and established cardiovascular disease or multiple risk factors
- Improving glycemic control in adults and pediatric patients aged 10 years and older with type 2 diabetes mellitus 1
The American Diabetes Association and American College of Cardiology recognize dapagliflozin as part of the SGLT2 inhibitor class, which has demonstrated significant benefits beyond glucose control, including cardiovascular and renal protection 3, 2.