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Both antiretroviral agents and statins are well known for their independent roles in causing drug–drug interactions.Not surprisingly, combined use of statins and antiretroviral agents may lead to a variety of clinically relevant drug–drug interactions, including reduced lipid-lowering effects (as a result from increased metabolism of statins) as well as an increased risk of potentially fatal rhabdomyolysis (as a result of reduced metabolism of the statin or impaired hepatic uptake). Initially, attention has focused on the cytochrome P450 system as being the source of the observed drug–drug interactions, but nowadays it is clear that other pathways, such as UDP-glucuronosyltransferase and the organic anion polypeptide B transporter, may also be involved. Here we review current literature on statin–antiretroviral interactions. The review is preceded by a brief overview of pharmacokinetic properties of antiretroviral agents and statins.Clinically relevant interactions between statins and antiretroviral agents do occur. The clinical relevance relates to an increased risk of statin-induced toxicity or reduced lipid-lowering activity of the statin. The information listed in this review should help the clinician to select the most appropriate combination. Whenever needed it is recommended to consult a clinical pharmacologist or pharmacist.