アトルバスタチンカルシウム

用途強力な HMG-CoA リダクターゼ阻害剤です（IC50=8 nM）。

用途強力な HMG-CoA リダクターゼ阻害剤です（IC50=8 nmol/l）。

説明Atorvastatin calcium (Lipitor®) was launched in Canada, the Netherlands, the UK and the US as an orally-active hypocholesterolemic agent. It was the first pharmaceutical product ever to attain over one billion dollars in sales in its first year. It can be synthesized by a number of routes but the most efficient involves the Paal-Knorr reaction of an acetonide protected dihydroxy amino ester and a diaryl phenylacetamide diketone. Lipitor is a liver selective, reversible competitive inhibitor of HMG-CoA reductase, the rate limiting step in cholesterol biosynthesis. Lipitor monotherapy resulted in a reduction of LDL cholesterol by up to 60%. Lipitor is about 2-4 times more potent, on a dosage basis, than Simvastatin. The superior properties of Lipitor can be attributed to its greater uptake and longer duration of action in the liver. In addition to its effects on cholesterol, Lipitor is also effective in lowering triglycerides. While the mechanism is not clear, two theories proposed are: a) the decrease in cholesterol causes a concomitant increase in hepatic LDL-receptor activity (mostly B and E type) which results in a decrease in triglycerides through an increase in binding of triglycerides to VLDL and LDL, and b) the decreased level of cholesterol impairs VLDL transport of triglycerides.

使用A selective, competitive HMG-CoA reductase inhibitor. The only drug in its class specfically indicated for lowering both elevated LDL-cholesterol and triglycerides in patients with hypercholesterolemia