Cerivastatin

Cerivastatin (INN,[1] brand names: Baycol, Lipobay) is a synthetic member of the class of statins used to lower cholesterol and prevent cardiovascular disease.

It was marketed by the pharmaceutical company Bayer A.G. in the late 1990s, competing with Pfizer's highly successful atorvastatin (Lipitor).

Bayer A.G. added a contraindication for the concomitant use of cerivastatin and gemfibrozil to the package 18 months after the drug interaction was found.

Cerivastatin also induced myopathy in a dose-dependent manner when administered as monotherapy, but that was revealed only after Bayer was sued and unpublished company documents were opened.

Cerivastatin mainly acts by competitively inhibiting HMG-CoA-reductase, which is the rate-limiting enzyme step in cholesterol biosynthesis.

[citation needed] The inhibitory activity of cerivastatin was compared to that of other statins, specifically lovastatin, simvastatin and pravastatin.

[citation needed] The pharmacological results from cerivastatin show that it is the most active HMG-CoA-reductase inhibitor among reported statins.

[citation needed] The strengths of the available cerivastatin medicine ranged from 0.2 - 0.8 mg, resulting in an actual dose of 1.9 - 13.1 μg/kg body weight for which rhabdomyolysis has been reported.

[3][16][17] This risk also appears to increase among patients who received gemfibrozil[3][18] or lovastatin[16] concomitantly, and there is a known interaction between these drugs and cerivastatin.

[3] In 12 of the 31 reported deaths of cerivastatin-related rhabdomyolysis in the US the cerivastatin-gemfibrozil interaction was implicated, while in 7 of the 31 fatal cases in the US, cerivastatin was combined with lovastatin.

[3][16] The reporting rate of fatal rhabdomyolysis in association with cerivastatin monotherapy is 1.9 per million prescriptions, which is 10-50 times as high as for other statins.

Minor side effects include diarrhea, fatigue, gas, heartburn, nasal congestion and headache.