Why choose Invokana (canagliflozin) - After first line, take a firm line
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Mode of Action

How Invokana works

  • Invokana is an SGLT2 inhibitor.
  • SGLT2 is a glucose cotransporter expressed in the proximal renal tubules, and is responsible for 90% of glucose reabsorption. 1,2
  • SGLT2 inhibitors act independently of β-cell function or insulin sensitivity – removing excess blood glucose by increasing urinary glucose excretion. 3
  • This also results in a loss of excess calories and water – which is why Invokana also reduces both weight and blood pressure. 4

SGLT2i: a novel method to achieve glycaemic control

Invokana (canagliflozin) Mode of Action Diagram

Adapted from Rothenberg PL, et al. Presented at the European Association for the Study of Diabetes. September 20–24, 2010; Stockholm, Sweden 4

Click diagram to enlarge

  • SGLT2 is responsible for 90% of glucose reabsorption, making it an attractive target for inhibition. 5
  • SGLT2 inhibitors act independently of β-cell function or insulin sensitivity – removing excess blood glucose by increasing urinary glucose secretion. 3 This also results in a loss of excess calories and water – which is why Invokana also reduces both weight and blood pressure – with approximately two thirds of weight reduction coming from a loss of fat mass. 4,6
  • Invokana increases estimated urinary glucose secretion ranging from 77–119g per day. This translates to an equivalent loss of 308-476Kcal/day. 2 [Results from Phase I studies of urinary glucose excretion in patients with type 2 diabetes.]

    This leads to:
     Improved glycaemic control and a reduction in HbA1c 2
     A loss of calories and therefore a reduction in body weight 2
     A mild osmotic diuresis, with the diuretic effect leading to a reduction in systolic blood pressure 2

How can Invokana deliver long-term renal benefits?

Invokana (canagliflozin) Mode of Action Diagram

Click diagram to enlarge

  • In type 2 diabetes, SGLT2 is overexpressed – leading to glomerular hyperfiltration. Inhibiting SGLT2 may, therefore, reduce hyperfiltration and lead to decreases in intraglomerular pressure.

Improvements in renal outcomes with Invokana are additional benefits only and not licensed indications.

References
  1. Bays H. Curr Med Res Opin 2009;25(3):671-81
  2. Reference 1(6)
  3. Bailey CD et al. BMC Med 2013;11:43
  4. Rothenberg PL et al. European Association for the Study of Diabetes (EASD) Annual Meeting. Stockholm, Sweden 2016. Abstract No. 876 (poster).
  5. Dokken NP. Diabetes Spectrum 2012;25(8):29-36
  6. Lavalle-Gonzáles FJ, et al. Diabetologia 2013;56(12):2582-92