Type 2 diabetes mellitus (T2DM) has become a worldwide concern in recent
years, primarily in highly developed Western societies. T2DM causes systemic complications, such as atherosclerotic heart disease, ischemic stroke, peripheral artery disease,
kidney failure, and diabetes-related maculopathy and retinopathy. The growing number
of T2DM patients and the treatment of long-term T2DM-related complications pressurize and exhaust public healthcare systems. As a result, strategies for combating T2DM
and developing novel drugs are critical global public health requirements. Aside from
preventive measures, which are still the most effective way to prevent T2DM, novel and
highly effective therapies are emerging. In the spotlight of next-generation T2DM treatment, sodium-glucose co-transporter 2 (SGLT-2) inhibitors are promoted as the most efficient perspective therapy. SGLT-2 inhibitors (SGLT2i) include phlorizin derivatives,
such as canagliflozin, dapagliflozin, empagliflozin, and ertugliflozin. SGLT-2, along
with SGLT-1, is a member of the SGLT family of proteins that play a role in glucose absorption via active transport mediated by Na+
/K+
ATPase. SGLT-2 is only found in the
kidney, specifically the proximal tubule, and is responsible for more than 90% glucose
absorption. Inhibition of SGLT-2 reduces glucose absorption, and consequently increases urinary glucose excretion, decreasing blood glucose levels. Thus, the inhibition of
SGLT-2 activity ultimately alleviates T2DM-related symptoms and prevents or delays
systemic T2DM-associated chronic complications. This review aimed to provide a more
detailed understanding of the effects of SGLT2i responsible for the acute improvement
in blood glucose regulation, a prerequisite for T2DM-associated cardiovascular complications control.