Pitavastatin: A new HMG-CoA reductase inhibitor for the treatment of hypercholesterolemia

Because of their good tolerability and their positive effect on lipid parameters and clinical outcomes, 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors (statins) have become the drugs of first choice for the management of dyslipidemia. Pitavastatin is the newest member in the statin family and received Food and Drug Administration approval for oral use in August 2009. Compared to other statins such as atorvastatin, simvastatin and pravastatin at specific doses, pitavastatin dosed at 1 to 4 mg daily showed similar efficacy in lowering low-density lipoprotein cholesterol (LDL-C) and altering other lipid parameters according to a number of studies. In addition, pitavastatin demonstrated cholesterol-lowering efficacy in special populations such as the elderly, patients with diabetes, and patients with higher cardiovascular risk. Because pitavastatin is minimally metabolized by the cytochrome P-450 isoenzymes, it is associated with a lower frequency of drug-drug interactions, and this may be a desirable characteristic of pitavastatin. Beneficial effects, such as reductions of coronary plaque volume and fibrofatty composition, have also been observed with pitavastatin. Thus far, the safety profile of pitavastatin is favorable and appears to be similar to those of other statins. Given its encouraging pharmacokinetic and pharmacodynamic characteristics, pitavastatin is likely to be a good alternative to other more established statins. The pharmacologic and pharmacokinetic properties of pitavastatin are reviewed in this article.