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Rosuvastatin represents one of the latest inhibitors of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase introduced in clinical practice for the treatment of hypercholesterolaemia. In comparative trials, across dose ranges this statin reduced low-density lipoprotein (LDL) cholesterol and total cholesterol significantly more than atorvastatin, simvastatin, and pravastatin, and triglycerides significantly more than simvastatin and pravastatin. In healthy subjects with normal LDL cholesterol and elevated C-reactive protein, rosuvastatin treatment produced a significant decrease in the incidence of cardiovascular events.Its chemical and pharmacokinetic properties suggest a very limited penetration in extrahepatic tissues with a lower risk of muscle toxicity and metabolically mediated drug-drug interactions, suggesting a low risk of pharmacokinetic interactions with antiretroviral drugs in patients with HIV infection. We describe a case of protease inhibitor-associated hypercholesterolaemia in a male HIV-infected patient with high cardiovascular risk. Treatment with rosuvastatin leaded to a significant reduction in total and LDL cholesterol levels, with a good tolerability profile after 15 months of follow-up.