Pitavastatin: an overview

Atheroscler Suppl. 2011 Nov;12(3):271-6. doi: 10.1016/S1567-5688(11)70886-8.


Compared to other statins, pitavastatin is a highly potent 3-hydroxy-3-methyl-glutaryl-CoA (HMG-CoA) reductase inhibitor and an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Its characteristic structure (heptenoate as the basic structure, a core quinoline ring and side chains that include fluorophenyl and cyclopropyl moieties) provides improved pharmacokinetics and significant LDL-C-lowering efficacy at low doses. Unlike other statins, the cyclopropyl group on the pitavastatin molecule appears to divert the drug away from metabolism by cytochrome P450 (CYP) 3 A4 and allows only a small degree of clinically insignificant metabolism by CYP2C9. As a result, pitavastatin is minimally metabolized; most of the bioavailable fraction of an oral dose is excreted unchanged in the bile and is reabsorbed by the small intestine ready for enterohepatic recirculation. This process probably accounts for pitavastatin's increased bioavailability relative to most other statins and contributes to its prolonged duration of action. In addition to its potent LDL-C-lowering efficacy, a number of pleiotropic benefits that might lead to a reduction in residual risk have been suggested in vitro. These include beneficial effects on endothelial function, stabilisation of the coronary plaque, anti-inflammatory effects and anti-oxidation. With regard to the clinical safety and efficacy of pitavastatin, the Phase IV Collaborative study of Hypercholesterolemia drug Intervention and their Benefits for Atherosclerosis prevention (CHIBA study) showed similar changes in lipid profile with pitavastatin and atorvastatin in Japanese patients with hypercholesterolemia. However, a subgroup analysis of the CHIBA study showed that pitavastatin produced more significant changes from baseline in LDL-C, TG, and HDL-C in patients with hypercholesterolemia and metabolic syndrome. The clinical usefulness of pitavastatin has been further demonstrated in a number of Japanese patient groups with hypercholesterolemia, including those with insulin resistance, low levels of high-density lipoprotein-cholesterol (HDL-C), high levels of C-reactive protein, and chronic kidney disease. Finally, the Japan Assessment of Pitavastatin and AtorvastatiN in Acute Coronary Syndrome (JAPAN-ACS) study showed that pitavastatin induces plaque regression in patients with ACS, which suggests potential benefits for pitavastatin in reducing CV risk.

Publication types

  • Review

MeSH terms

  • Antioxidants / pharmacology
  • Antioxidants / therapeutic use
  • Atorvastatin
  • Cardiovascular Diseases / blood
  • Cardiovascular Diseases / prevention & control*
  • Cholesterol, HDL / blood*
  • Cholesterol, HDL / physiology
  • Cholesterol, LDL / blood
  • Clinical Trials, Phase IV as Topic
  • Endothelium, Vascular / drug effects
  • Hepatocytes / drug effects
  • Hepatocytes / metabolism
  • Heptanoic Acids / therapeutic use
  • Humans
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / adverse effects
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / chemistry
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / pharmacokinetics
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / pharmacology
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / therapeutic use*
  • Hypercholesterolemia / drug therapy
  • Hypercholesterolemia / epidemiology
  • Inflammation / drug therapy
  • Japan / epidemiology
  • Metabolic Syndrome / drug therapy
  • Metabolic Syndrome / epidemiology
  • Molecular Structure
  • Multicenter Studies as Topic
  • Plaque, Atherosclerotic / drug therapy
  • Pyrroles / therapeutic use
  • Quinolines / adverse effects
  • Quinolines / chemistry
  • Quinolines / pharmacokinetics
  • Quinolines / pharmacology
  • Quinolines / therapeutic use*
  • Receptors, LDL / metabolism


  • Antioxidants
  • Cholesterol, HDL
  • Cholesterol, LDL
  • Heptanoic Acids
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors
  • Pyrroles
  • Quinolines
  • Receptors, LDL
  • Atorvastatin
  • pitavastatin