Approved August 3, 2009

PITAVASTATIN CALCIUM
(FDA Category 1S)

LIVALO(R) (Kowa Pharmaceuticals America, Inc.) is a synthetic HMG-CoA reductase inhibitor (statin).

DOSING INFORMATION: The recommended initial dose is 2 milligrams (mg) orally daily with or without food administered at any time of the day. The dosing range is 1 mg to 4 mg with a maximum dose of 4 mg daily. Assess lipid parameters 4 weeks after initiation or titration

PHARMACOKINETICS: Pitavastatin reaches peak plasma concentrations approximately 1 hour after oral administration. It is more than 99% protein bound, primarily to albumin and alpha 1-acid glycoprotein. The mean volume of distribution is approximately 148 L. The mean elimination half-life is about 12 hours. Pitavastatin is minimally metabolized by CYP2C9 and to a lesser extent by CPY2C8. The major metabolite in human plasma is the lactone, which is formed via glucuronide conjugation by UGT1A3 and UGT2B7. Mean urine and fecal excretion are approximately 15% and 79%, respectively.

CAUTIONS: Pitavastatin is contraindicated in patients with active liver disease, including unexplained, persistently elevated transaminase levels, known hypersensitivity, pregnancy/breastfeeding, and concomitant use with cyclosporine. The most common adverse events occurring at an incidence 2% or greater are back pain, constipation, diarrhea, myalgia, and pain in the extremity.

FDA APPROVED INDICATION: Pitavastatin is indicated as adjunctive treatment to diet for primary hyperlipidemia and mixed dyslipidemia.