Pitavastatin: A different pharmacological profile

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Pitavastatin, a synthetic HMG-CoA reductase inhibitor, is characterized by a cyclopropyl moiety that results in several pharmacological differences compared with other statins. These include inhibition of cholesterol synthesis and increased lipoprotein lipase expression at lower doses than other statins, and significant high-density and apolipoprotein A1-elevating activity that persists with time. Pitavastatin has a higher bioavailability (60%) than any other statin and the majority of the bioavailable fraction after oral dosing is excreted unchanged in the bile. The enterohepatic circulation of unchanged pitavastatin contributes to the prolonged duration of action, allowing once-daily, any-time dosing. Pitavastatin undergoes only minor metabolism by CYP2C9 but is not metabolized by CYP3A4. Neither pitavastatin nor its lactone form have inhibitory effects on cytochrome P450, and CYP3A4 inhibitors have no effect on pitavastatin plasma concentrations. Moreover, P-glycoprotein-mediated transport does not play a major role in the disposition of pitavastatin and pitavastatin does not inhibit P-glycoprotein activity. Pitavastatin is transported into the liver by several hepatic transporters, but organic anion-transporting polypeptide 1B1 inhibitors have relatively little effect on plasma pitavastatin concentrations compared with other statins. With the exception of multitransporter inhibitors, such as ciclosporin, interactions are generally of no clinical significance. As a result, pitavastatin has minimal drug-drug and drug-food interactions, making it a good treatment option in the large population of individuals with dyslipidemia who require multidrug therapy.

Original languageEnglish
Pages (from-to)3-9
Number of pages7
JournalFuture Lipidology
Issue number3 SUPPL.
Publication statusPublished - Jun 2012


  • drug-drug interaction
  • metabolism
  • pharmacokinetics
  • pharmacology
  • pitavastatin

ASJC Scopus subject areas

  • Cardiology and Cardiovascular Medicine
  • Endocrinology, Diabetes and Metabolism


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