This thesis examines how sodium–glucose cotransporter-2 (SGLT2) inhibitors have evolved from purely glucose-lowering drugs into agents with important cardiovascular and renal benefits. It outlines the main biological mechanisms underlying these effects, such as changes in renal hemodynamics, energy metabolism, and inflammatory pathways. The work reviews evidence from large clinical trials showing reduced rates of heart failure hospitalization and slower progression of chronic kidney disease. Special attention is given to the clinical impact of these findings in both diabetic and non-diabetic populations. In conclusion, the thesis highlights the growing importance of SGLT2 inhibitors in contemporary cardio-renal-metabolic therapy.