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Pitavastatin: evidence for its place in treatment of hypercholesterolemia.

Alagona P - Core Evid (2010)

Bottom Line: Statins, inhibitors of 3-hydroxy-3-methylglutaryl-coenzyme A reductase, are the most potent pharmacologic agents for lowering total cholesterol (TC) and low-density lipoprotein cholesterol (LDL-C).Considering the numbers of patients who need LDL-C-lowering therapy and questions of individual tolerance and therapeutic response, having a variety of agents to choose from is beneficial for patient care.This paper presents background information on statin treatment and reviews data regarding a new agent, pitavastatin, which has recently been approved for clinical use.

View Article: PubMed Central - PubMed

Affiliation: Penn State Heart and Vascular Institute, Penn State College of Medicine, Hershey, Pennsylvania, USA.

ABSTRACT
Statins, inhibitors of 3-hydroxy-3-methylglutaryl-coenzyme A reductase, are the most potent pharmacologic agents for lowering total cholesterol (TC) and low-density lipoprotein cholesterol (LDL-C). They have become an accepted standard of care in the treatment of patients with known atherosclerotic cardiovascular disease (secondary prevention) and also those at increased risk of cardiovascular events. There are currently six statin drugs commercially available in the US. Although they are chemically similar and have the same primary mechanisms of action in lowering TC and LDL-C, there are differences in their efficacy or potency, metabolism, drug-drug interactions, and individual tolerability. Considering the numbers of patients who need LDL-C-lowering therapy and questions of individual tolerance and therapeutic response, having a variety of agents to choose from is beneficial for patient care. This paper presents background information on statin treatment and reviews data regarding a new agent, pitavastatin, which has recently been approved for clinical use.

No MeSH data available.


Related in: MedlinePlus

Chemical structure of pitavastatin. Note commonality to other statins in Figure 1.
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f4-ce-5-091: Chemical structure of pitavastatin. Note commonality to other statins in Figure 1.

Mentions: Pitavastatin is a potent HMG-CoA reductase inhibitor which induces a substantial increase in LDL receptor activity and lowers LDL-C. It has a characteristic structure (Figure 4) with a quinoline ring at the core, a cyclopropyl moiety, and a flourophenyl group, similar to other statins, especially fluvastatin and rosuvastatin.35 This structure improves pharmacokinetics, with better absorption and activity (Table 1).36 After oral administration of C-14-labeled pitavastatin, the concentration is 54 times greater in the liver than in serum. Pitavastatin is more potent at inhibiting cholesterol synthesis in vitro and is more effective at induction of LDL receptor expression and activity than any other statin.37 In isolated rat liver microsomes, pitavastatin inhibited HMG-CoA reductase activity in a concentration-dependent manner, with an IC50 of 6.8 nmol/L, 2.4-fold higher than simvastatin and 6.8-fold higher than pravastatin. Similar results were obtained in a cultured human hepatoma cell line, with pitavastatin having a two-fold higher affinity for HMG-CoA reductase inhibition than simvastatin and a 5.7-fold higher affinity than atorvastatin. These data imply that pitavastatin is a stronger inhibitor of HMG-CoA reductase activity than any other statin, including rosuvastatin.38 Using the same cultured human hepatoma cell model, pitavastatin was found to have a superior ApoA-1 secretion-promoting effect compared with simvastatin and atorvastatin.39


Pitavastatin: evidence for its place in treatment of hypercholesterolemia.

Alagona P - Core Evid (2010)

Chemical structure of pitavastatin. Note commonality to other statins in Figure 1.
© Copyright Policy
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC3065553&req=5

f4-ce-5-091: Chemical structure of pitavastatin. Note commonality to other statins in Figure 1.
Mentions: Pitavastatin is a potent HMG-CoA reductase inhibitor which induces a substantial increase in LDL receptor activity and lowers LDL-C. It has a characteristic structure (Figure 4) with a quinoline ring at the core, a cyclopropyl moiety, and a flourophenyl group, similar to other statins, especially fluvastatin and rosuvastatin.35 This structure improves pharmacokinetics, with better absorption and activity (Table 1).36 After oral administration of C-14-labeled pitavastatin, the concentration is 54 times greater in the liver than in serum. Pitavastatin is more potent at inhibiting cholesterol synthesis in vitro and is more effective at induction of LDL receptor expression and activity than any other statin.37 In isolated rat liver microsomes, pitavastatin inhibited HMG-CoA reductase activity in a concentration-dependent manner, with an IC50 of 6.8 nmol/L, 2.4-fold higher than simvastatin and 6.8-fold higher than pravastatin. Similar results were obtained in a cultured human hepatoma cell line, with pitavastatin having a two-fold higher affinity for HMG-CoA reductase inhibition than simvastatin and a 5.7-fold higher affinity than atorvastatin. These data imply that pitavastatin is a stronger inhibitor of HMG-CoA reductase activity than any other statin, including rosuvastatin.38 Using the same cultured human hepatoma cell model, pitavastatin was found to have a superior ApoA-1 secretion-promoting effect compared with simvastatin and atorvastatin.39

Bottom Line: Statins, inhibitors of 3-hydroxy-3-methylglutaryl-coenzyme A reductase, are the most potent pharmacologic agents for lowering total cholesterol (TC) and low-density lipoprotein cholesterol (LDL-C).Considering the numbers of patients who need LDL-C-lowering therapy and questions of individual tolerance and therapeutic response, having a variety of agents to choose from is beneficial for patient care.This paper presents background information on statin treatment and reviews data regarding a new agent, pitavastatin, which has recently been approved for clinical use.

View Article: PubMed Central - PubMed

Affiliation: Penn State Heart and Vascular Institute, Penn State College of Medicine, Hershey, Pennsylvania, USA.

ABSTRACT
Statins, inhibitors of 3-hydroxy-3-methylglutaryl-coenzyme A reductase, are the most potent pharmacologic agents for lowering total cholesterol (TC) and low-density lipoprotein cholesterol (LDL-C). They have become an accepted standard of care in the treatment of patients with known atherosclerotic cardiovascular disease (secondary prevention) and also those at increased risk of cardiovascular events. There are currently six statin drugs commercially available in the US. Although they are chemically similar and have the same primary mechanisms of action in lowering TC and LDL-C, there are differences in their efficacy or potency, metabolism, drug-drug interactions, and individual tolerability. Considering the numbers of patients who need LDL-C-lowering therapy and questions of individual tolerance and therapeutic response, having a variety of agents to choose from is beneficial for patient care. This paper presents background information on statin treatment and reviews data regarding a new agent, pitavastatin, which has recently been approved for clinical use.

No MeSH data available.


Related in: MedlinePlus