Drug intelligence / Profile preview

cerivastatin

Development stage
Discontinued
Lead developer
Bayer
Modality
Small Molecules
Administration
Oral
01

Overview

Cerivastatin is a fully synthetic small molecule member of the statin class, previously marketed for lowering cholesterol and prevention of cardiovascular disease. It is an extremely potent and enantiomerically pure competitive inhibitor of HMG-CoA reductase, the rate-limiting enzyme in cholesterol biosynthesis via the mevalonate pathway[1][3][5][9]. By blocking this enzyme, cerivastatin reduces hepatic cholesterol synthesis and upregulates hepatic LDL receptors, increasing LDL clearance from plasma and reducing total and LDL cholesterol levels. Cerivastatin was notable for its high potency, high oral bioavailability, and lipophilicity, resulting in effective LDL lowering at lower doses compared to other statins[5]. Developed and marketed primarily by Bayer, cerivastatin was withdrawn globally in 2001 due to increased risk of fatal rhabdomyolysis, especially when combined with other lipid-lowering drugs, but remains a paradigm for potent HMG-CoA reductase inhibition[8][9].

Brand names
BaycolLipobayZenas
Other names
cerivastatinumCerivastatinaCerivastatineCervastatincerivastatin acidCerivastatin sodium salt hydratecerivastatin systemic(3R,5S,6E)-7-(4-(4-fluorophenyl)-5-(methoxymethyl)-2,6-di(propan-2-yl)pyridin-3-yl)-3,5-dihydroxyhept-6-enoic acid
02

Targets

HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)

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