The SGLT2 inhibitors represent a class of antidiabetic agents that facilitates elimination of glucose through the urine. These agents selectively inhibit the SGLT2. The SGLT2 transporter is located specifically in the proximal convoluted tubules of the kidneys and facilitates the reabsorption of glucose from the ultrafiltrate. In T2DM, the activity of SGLT2 transporter is upregulated, resulting in increased tubular reabsorption of glucose. Clinically, the SGLT2 transporter plays a more important role in the renal reabsorption of glucose. Sodium–glucose cotransporter type-1 (SGLT1) transporter is present more ubiquitously in the body, having a predominant role in the gut, skeletal, and cardiac muscle cells. SGLT1 transporter also has a minor role in the kidneys, accounting for a small fraction of glucose reabsorption.