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Key Point: Rosuvastatin is not metabolized by the CYP450 3A4 system, has no clinically significant

 metabolites, and is relatively hydrophilic, unlike atorvastatin and simvastatin. 

The pharmacokinetic profiles of rosuvastatin, 3 other marketed statins, and ezetimibe are shown on this

 slide1-5

 

Atorvastatin and simvastatin are metabolized by the CYP450 3A4 pathway, have clinically significant

 metabolites, and are relatively lipophilic2-3

 

In contrast, rosuvastatin and pravastatin are not metabolized by CYP450 3A4,  do not have clinically

 significant metabolites, and are relatively hydrophilic1,4

 

Because it is known that the risk of myopathy increases with the dose of the statin, factors that increase

 the concentration of statin in muscle tissue may enhance its potential for myotoxic effects6-7

 

Rosuvastatin, pravastatin, atorvastatin, and simvastatin are hepatoselective and cleared by the liver or by

 the liver and the kidney1-4