Pitavastatin is the last marketed statin. Different studies have shown that pitavastatin is more potent than pravastatin and simvastatin in reducing LDL-cholesterol levels, and equivalent to atorvastatin and rosuvastatin. Moreover, pitavastatin provides a significant and sustained increase of HDL-cholesterol levels. Remarkably, as pitavastatin is minimally metabolized by CYP, the risk of interactions with other drugs is low. Additionally, pitavastatin does not interfere with glucose metabolism in diabetics and non-diabetics, and exerts a beneficial effect in patients with renal dysfunction. However, although available information may suggest that pitavastatin can improve cardiovascular prognosis, data coming from specifically designed clinical trials are still warranted. The aim of this review was to update the available evidence about efficacy and safety of pitavastatin, and to analyze the place of pitavastatin in the current armamentarium for the treatment of patients with hypercholesterolemia.