Description
Lipobay was launched in Denmark, Germany and the UK for treatment of
primary hypercholesteremia types Ⅱa and Ⅱb. It is available through a nine step
synthesis beginning with the Hantsch reaction of ethyl 3-amino-4-methylpent-2-enoate
and 4-(ethoxycarbonyl)-5-(4-fluorophenyl)-2-methylpent-4-en-3-one. Lipobay acts as
an HMG-CoA reductase inhibitor showing a high liver selectivity (50 fold). In vitro
Lipobay had a higher affinity (110x) for the enzyme than does Lovastatin, Simvastatin
and pravastatin which resulted in a lower ED
50, in vivo compared to Lovastatin. Three
metabolites generated by the CYP3A4 enzyme system were equal to the parent in
activity. Lipobay was as effective as Gemfibrozil in type lib hypercholesteremia and
had no age or gender effects. It decreased plasma levels of VLDL and LDL
cholesterol by a mechanism similar to other HMG-CoA reductase inhibitors. The (-)-
antipode is completely inactive indicating a high stereospecificity by the enzyme. It is
therapeutically useful at ultra-low doses which may minimize any drug-drug
interactions.
Chemical Properties
Solid
Originator
Bayer (Germany)
Uses
Cerivastatin is a competitive inhibitor of HMG-CoA reductase.
Uses
Cerivastatin sodium salt hydrate has been used as a supplement in cell culture.
Definition
ChEBI: The sodium salt of cerivastatin. Formerly used to lower cholesterol and prevent cardiovascular disease, it was withdrawn from the market worldwide in 2001 following reports of a severe form of muscle toxicity.
brand name
Baycol
(Bayer).
General Description
Cerivastatin sodium salt hydrate belongs to the statin class of lipid lowering agents. It helps in decreasing MAP kinase activation, blocking AP-1 (activator protein-1) and NF-kB (nuclear factor-kB ) binding activity, inhibiting inflammatory responses and ameliorated renal damage. It also lowers cholesterol. It is metabolized by cytochrome P450 (CYP)3A4 and (CYP)2C8. Cerivastatin sodium salt hydrate is linked to rhabdomyolysis.
Hazard
A poison by ingestion.
Biochem/physiol Actions
Cerivastatin sodium is an HMG-CoA reductase inhibitor. HMG-CoA is a key enzyme in the production of cholesterol.
