Fluvastatin enzyme activity

The statins, lovastatin (L), simvastatin (S), pravastatin (P), fluvastatin (F), cerivastatin, and atorvastatin, inhibit HMG CoA reductase. The active group of L, S, P, and F (or their metabolites) resembles that of the physiological substrate of the enzyme (A). L and S are lactones that are rapidly absorbed by the enteral route, subjected to extensive first-pass extraction in the liver, and there hydrolyzed into active metabolites. P and F represent the active form and, as acids, are actively transported by a specific anion carrier that moves bile acids from blood into liver and also mediates the selective hepatic uptake of the mycotoxin, amanitin (A), Atorvastatin has the longest duration of action. 

The HMG-CoA reductase inhibitors described above bind to two active sites on the enzyme the hydroxymethylglutaryl binding domain and an adjacent hydrophobicpocketto which the decalin moiety binds (167). The recognition that the ring-opened hydroxy acids resemble mevalonic acid and that the decalin moiety could be replaced by 4-fluorophenyl-substituted heterocycles led to the launch of several new products including fluvastatin... 

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