Statin therapy has became the most important advance in stroke prevention since the introduction of aspirin and blood pressure-lowering therapies. Other lipid-modifying drugs have been less successful in reducing the incidence of stroke, but because of evidence for the use of triglyceride-lowering drugs and treatments that raise concentrations of high-density lipoprotein (HDL) cholesterol, further investigations are needed, particularly in patients with an atherogenic dyslipidemia profile (high triglycerides and low HDL cholesterol levels). Furthermore, beyond reducing low-density lipoprotein cholesterol and possibly improving other lipids fractions in patients who are at high risk of stroke, the present review shoes that lipid-modifying drugs might have neuroprotective effects that should also be further explored.