Rosuvastatin is a potent statin with pharmacologic and pharmacokinetic advantages. Its high degree of liver selectivity results in high hepatic concentration leading to superior efficacy at lowering low density lipoprotein cholesterol and triglycerides as well as improving high density lipoprotein cholesterol compared to other statins. Rosuvastatin has relatively low lipophilicity when compared with other statins and has minimal entry into peripheral cells. This along with its minimal cytochrome P450 metabolism presents relatively better tolerability, safety and drug interaction profile. Consistent with these features, rosuvastatin represents a step forward in the statin therapy. We conducted a literature search to identify rosuvastatin papers published in English. In this review, we have outlined the pharmacodynamics, pharmacokinetics of rosuvastatin, focusingits efficacy and safety. We have also emphasized on the major clinical trials involving rosuvastatin.