Canagliflozin (Invokana™), an oral selective sodium-glucose co-transporter 2 
(SGLT2) inhibitor, is under global development with Mitsubishi Tanabe Pharma and 
Janssen Pharmaceuticals, a subsidiary of Johnson and Johnson, for the treatment 
of type 2 diabetes mellitus. SGLT2 are mainly located in the proximal tubule of 
the kidney and are involved in the reabsorption of filtered glucose from the 
glomeruli into the body. Inhibition of SGLT2 lowers blood glucose in an insulin 
independent manner as a consequence of blocking reabsorption of filtered glucose 
in the glomeruli, thereby increasing urinary excretion of glucose and, in turn, 
potentially reducing bodyweight. Canagliflozin is the first SGLT2 inhibitor to 
be approved in the USA and is under regulatory review in the EU. This article 
summarizes the milestones in the development of canagliflozin, leading to its 
first approval for use in adults with type 2 diabetes.