Transporter pharmacogenetics and statin toxicity

Clin Pharmacol Ther. 2010 Jan;87(1):130-3. doi: 10.1038/clpt.2009.197. Epub 2009 Nov 4.


Polymorphisms in transporter genes can have profound effects on statin pharmacokinetics. In particular, a common genetic variant of organic anion-transporting polypeptide 1B1 reduces the hepatic uptake of many statins, increasing the risk of statin-induced myopathy. Similarly, genetically impaired adenosine triphosphate (ATP)-binding cassette G2 transporter efflux activity results in a marked increase in systemic exposure to various statins. Importantly, the effects of these genetic polymorphisms differ depending on the specific statin that is used. This provides a rational basis for the individualization of lipid-lowering therapy.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Humans
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / adverse effects*
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / metabolism*
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / toxicity
  • Membrane Transport Proteins / genetics*
  • Membrane Transport Proteins / metabolism*
  • Pharmacogenetics*
  • Polymorphism, Genetic / genetics


  • Hydroxymethylglutaryl-CoA Reductase Inhibitors
  • Membrane Transport Proteins