Products
Cerivastatin was commercially available in the form of film-coated tablets (Lipobay, Baycol). Because of rare possible adverse effects, it was withdrawn from the market in August 2001 (see below).
Structure and properties
Cerivastatin (C26H34FNO5, Mr = 459.6 g/mol) is a pyridine derivative and is present in drugs as cerivastatin sodium. Unlike other statins, it is already in the active form and is not a prodrug.
Effects
Cerivastatin (ATC C10AA06) has lipid-lowering properties. It lowers LDL, triglycerides, total cholesterol, and increases HDL. The effects are due to inhibition of HMG-CoA reductase. This enzyme catalyzes an early step in cholesterol biosynthesis. Cerivastatin has additional pleiotropic effects.
Indications
For the treatment of lipid metabolism disorders (hypercholesterolemia and mixed dyslipidemia).
Adverse effects
Since the launch of cerivastatin in June 1987 through June 2001, 31 cases of fatal rhabdomyolysis during therapy with the drug had been reported to the U.S. Food and Drug Administration. This was a very rare, possibly dose-dependent adverse effect. The reason for withdrawal from the market was primarily due to evidence suggesting that rhabdomyolysis was more common with cerivastatin as opposed to the other statins. Fatal cases had also been reported with other statins, but significantly fewer over a longer period of time. 12 Of the patients who died on cerivastatin had also taken the fibrate gemfibrozil (Gevilon), although this combination was specifically contraindicated.
