Ipragliflozin (Suglat® [Japan]), an orally active, next-generation sodium-glucose transporter 2 (SGLT2) inhibitor, has been developed by Astellas Pharma and Kotobuki Pharmaceutical for the treatment of type 2 diabetes mellitus. Ipragliflozin has received its first global approval in this indication in Japan, for use as monotherapy or in combination with another antihyperglycaemic agent (metformin, pioglitazone, a sulfonylurea, an α-glucosidase inhibitor, a dipeptidylpeptidase-4 inhibitor or nateglinide). Ipragliflozin is the first SGLT2 inhibitor to be approved in Japan. This article summarizes the milestones in the development of ipragliflozin leading to this first approval for the treatment of type 2 diabetes mellitus.