2013•Handbook of Metabolic Pathways of XenobioticsRequires access
Simvastatin
Angela Wehr
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Abstract
Simvastatin (brand name: Zocor) is a 3‐hydroxy‐3‐methyl‐glutaryl‐CoA (HMGCoA) reductase inhibitor. It is used to lower blood cholesterol and triglyceride levels. The reversible conversion of simvastatin lactone to the active hydroxy acid form is NADPH independent. While simvastatin acid is not a substrate for microsomal metabolism, the lactone form is converted to the major metabolites, 3″‐hydroxy simvastatin, 3′,5′‐dihydrodiol simvastatin, 6′‐exomethylene simvastatin, and 6′‐hydroxysimvastatin, and in an NADPH dependent fashion. Active metabolites 6′‐hydroxysimvastatin and 3″‐hydroxy simvastatin inhibit HMG‐CoA reductase activity in vitro.