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Cerivastatin: a cellular and molecular drug for the future? 总被引:7,自引:0,他引:7
Siegel-Axel DI 《Cellular and molecular life sciences : CMLS》2003,60(1):144-164
The 'statin story' began in 1987 when the first-generation, fungal HMG-CoA reductase inhibitor lovastatin received FDA approval
in the USA. Ten years later, the sixth compound of this class came onto the world market - the fully synthetic statin cerivastatin.
A number of clinical studies had confirmed its high pharmacological efficacy, its excellent pharmacokinetic properties with
fast and nearly complete absorption after oral uptake, a linear kinetic over a broad concentration range, and its favorable
safety profile. The greatest advantages, of cerivastatin, however, are its lipophilicity, its high bioavailability of about
60% after oral application and its potency at 100-fold lower doses compared to other lipophilic statins. Nevertheless, the
most exciting findings are certainly its non-lipid-related, pleiotropic effects at the cellular and molecular level. Statin
therapy was also found to reduce mortality in cases where cholesterol levels or atherosclerotic plaque formation remained
unaltered. However, cerivastatin improves endothelial dysfunction, possesses anti-inflammatory, antioxidant, anticoagulant,
antithrombotic, antiproliferative, plaque-stabilizing, immunmodulatory, and angiogenic effects, and may even prevent tumor
growth, Alzheimer's disease, and osteoporosis. Most of these effects seem to be based on the inhibition of isoprenoid synthesis.
Although cerivastatin is no longer on the market because of some problematic side effects, it could be one of the most potent
cellular and molecular drugs for the future.
Received 29 May 2002; received after revision 23 August 2002; accepted 26 August 2002
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