The Medical Letter on Drugs and Therapeutics
Pitavastatin (Livalo) - The Seventh Statin
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Revised 7/28/10: In the table, the usual decrease in LDL-cholesterol with pitavastatin has been changed to 35-40% (2 mg) and 40-45% (4 mg). Also, in the Dosage and Administration paragraph, the GFR has been changed to 30-<60 ml/min/1.73 m2.

The FDA has approved the marketing of pitavastatin (Livalo – Kowa), an HMG-CoA reductase inhibitor (“statin”), for treatment of primary hyperlipidemia or mixed dyslipidemia. It has been available in Japan since 2003. All of the statins now available in the US are listed in the table on page 58.

PHARMACOLOGY — After oral administration, plasma concentrations of pitavastatin reach a peak (Cmax) in about one hour (Tmax). Taking the drug with a high-fat meal decreases Cmax by about 50%, but does not significantly lower the area under the concentration/time curve (AUC). Pitavastatin is metabolized in the liver mainly by glucuronidation and minimally by CYP2C9. It is also a substrate of organic anion transporting peptide 1B1 (OATP1B1), a hepatic drug transporter. OATP1B1-mediated uptake is thought to be the major rate-limiting step in the hepatobiliary clearance of pitavastatin. The plasma elimination half-life ... more      

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