SGLT2 Inhibitors: Complete List
The four FDA-approved SGLT2 inhibitors currently available in the United States are empagliflozin, dapagliflozin, canagliflozin, and ertugliflozin. 1, 2, 3, 4
Available SGLT2 Inhibitors
The following agents are approved and commonly used in clinical practice:
- Empagliflozin - Available as JARDIANCE in 10 mg and 25 mg tablets 3
- Dapagliflozin - Available in 5 mg and 10 mg film-coated tablets 2
- Canagliflozin - Approved SGLT2 inhibitor with documented cardiovascular and renal benefits 4, 5, 6
- Ertugliflozin - Fourth FDA-approved agent in this class 4, 5, 7
Selectivity Profiles
- Dapagliflozin, empagliflozin, and ertugliflozin are the most selective inhibitors for SGLT2 compared to SGLT1 8
- Canagliflozin has greater SGLT1 inhibition and affects intestinal glucose absorption in addition to renal effects 8
- Sotagliflozin is a dual SGLT1/SGLT2 inhibitor that has been studied in cardiovascular outcome trials but has different selectivity characteristics 8, 9
Mechanism of Action
All SGLT2 inhibitors work through the same primary mechanism:
- Block sodium-glucose co-transporter 2 proteins in the S1 and S2 segments of the proximal renal tubules 8, 1
- Reduce renal glucose reabsorption and increase urinary glucose excretion (glucosuria) 8, 2, 3
- Function independently of insulin secretion or action, making them effective regardless of diabetes duration 1
- Lower the renal threshold for glucose to approximately 180 mg/dL 1
Clinical Efficacy
- Reduce HbA1c by approximately 0.5% to 1.0% 1, 6
- Promote weight loss of 1.5 to 3.5 kg 1
- Lower systolic blood pressure by 3 to 5 mmHg 1
- Reduce risk of major cardiovascular adverse events and hospitalization for heart failure 1, 4, 5
- Provide renoprotective effects with reduced progression of diabetic kidney disease 1, 6
- Low risk of hypoglycemia when used as monotherapy 1