Figure 11 Structures of key compounds leading to the discovery of rosuvastatin.

have not been reported, synthetic details have been described.70 In animal studies, pitavastatin also dose-dependently reduces total plasma cholesterol and LDLc, with concomitant reductions in serum TG.

Oral administration of pitavastatin (0.5mgkg_ 1 day_ 1) to hyperlipidemic rabbits for 26 weeks reduced total plasma cholesterol by 7-20% and also reduced the atherosclerotic lesion area. Pitavastatin is rapidly absorbed and has the highest overall bioavailability of any statin (~80%). Pitavastatin is also highly protein-bound (>95%). Like rosuvastatin and pravastatin, pitavastatin is not significantly metabolized by CYP3A4 enzymes, so the potential for drug-drug interactions is reduced. Pitavastatin is metabolized by CYP2C9 and CYP2C8. Pitavastatin has a reasonable duration of action and plasma half-life (t1/2 = 4-5 h). Pitavastatin 9 was launched in Japan in 2003 and is being tested clinically in the US.

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