Pitavastatin: A Review in Hypercholesterolemia.

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Hoy SM

Pitavastatin: A Review in Hypercholesterolemia.

Am J Cardiovasc Drugs. 2017 Apr;17(2):157-168. doi: 10.1007/s40256-017-0213-8.

PubMed ID

28130659 [ View in PubMed

]

Abstract

Oral pitavastatin (Livalo((R)); Livazo((R))) is a competitive HMG-CoA reductase inhibitor that is available in the EU for the reduction of elevated total cholesterol and low-density lipoprotein cholesterol (LDL-C) levels in adults with primary hypercholesterolemia and combined (mixed) dyslipidemia. In short-term, phase III or IV studies in this patient population, pitavastatin 1-4 mg once daily was generally no less effective than presumed equipotent dosages of atorvastatin and simvastatin (including in patients with type 2 diabetes or >/=2 cardiovascular risk factors) and was superior to pravastatin (including in patients aged >/=65 years) in lowering LDL-C levels. Pitavastatin provided sustained LDL-C-lowering efficacy over up to 60 weeks' therapy in extension studies, and was associated with short- and longer-term improvements in several other lipid parameters. Short- and longer-term outcomes in studies in Asian patients were consistent with these findings. Pitavastatin was generally well tolerated and did not appear to adversely affect glucose metabolism parameters (e.g. fasting blood glucose, fasting plasma glucose, fasting plasma insulin, glycated hemoglobin) in short- and longer-term prospective and post-marketing surveillance studies in adults. Moreover, in combination with lifestyle modification advice, it was associated with a significant reduction in the risk of progression from impaired glucose tolerance to diabetes relative to lifestyle modification advice alone in a longer-term study in Japanese subjects. Thus, pitavastatin is an effective treatment option in adults with primary hypercholesterolemia and combined (mixed) dyslipidemia, including those at risk of developing type 2 diabetes.

DrugBank Data that Cites this Article

Drugs

Pitavastatin

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Pitavastatin	3-hydroxy-3-methylglutaryl-coenzyme A reductase	Protein	Humans	Yes	Inhibitor	Details

Drug Enzymes

Drug	Enzyme	Kind	Organism	Pharmacological Action	Actions
Pitavastatin	Cytochrome P450 2C9	Protein	Humans	Unknown	Substrate	Details
Pitavastatin	UDP-glucuronosyltransferase 1-3	Protein	Humans	Unknown	Substrate	Details
Pitavastatin	UDP-glucuronosyltransferase 2B7	Protein	Humans	Unknown	Substrate	Details

Drug Transporters

Drug	Transporter	Kind	Organism	Pharmacological Action	Actions
Pitavastatin	Sodium/bile acid cotransporter	Protein	Humans	Unknown	Substrate	Details
Pitavastatin	Solute carrier organic anion transporter family member 1B1	Protein	Humans	Unknown	Substrate Inhibitor	Details
Pitavastatin	Solute carrier organic anion transporter family member 1B3	Protein	Humans	Unknown	Substrate	Details
Pitavastatin	Solute carrier organic anion transporter family member 2B1	Protein	Humans	Unknown	Substrate	Details