Cerivastatin

Approved, Withdrawn Small Molecule

Cerivastatin

On August 8, 2001 the U.S. Food and Drug Administration (FDA) announced that Bayer Pharmaceutical Division voluntarily withdrew Baycol from the U.S. market, due to reports of fatal Rhabdomyolysis, a severe adverse reaction from this cholesterol-lowering (lipid-lowering) product. It has also been withdrawn from the Canadian market. On August 8, 2001 the U.S. Food and Drug Administration (FDA) announced that Bayer Pharmaceutical Division voluntarily withdrew Baycol from the U.S. market, due to reports of fatal Rhabdomyolysis, a severe adverse reaction from this cholesterol-lowering (lipid-lowering) product. It has also been withdrawn from the Canadian market.

This compound belongs to the class of organic compounds known as phenylpyridines. These are polycyclic aromatic compounds containing a benzene ring linked to a pyridine ring through a CC or CN bond.

Structure

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Summary of Product Characteristics

Field Name Value
NameCerivastatin
TypeSmall Molecule
GroupsApproved, Withdrawn
DescriptionOn August 8, 2001 the U.S. Food and Drug Administration (FDA) announced that Bayer Pharmaceutical Division voluntarily withdrew Baycol from the U.S. market, due to reports of fatal Rhabdomyolysis, a severe adverse reaction from this cholesterol-lowering (lipid-lowering) product. It has also been withdrawn from the Canadian market.
IndicationUsed as an adjunct to diet for the reduction of elevated total and LDL cholesterol levels in patients with primary hypercholesterolemia and mixed dyslipidemia (Fredrickson Types IIa and IIb) when the response to dietary restriction of saturated fat and cholesterol and other non-pharmacological measures alone has been inadequate.
PharmacodynamicsCerivastatin, a competitive HMG-CoA reductase inhibitor effective in lowering LDL cholesterol and triglycerides, is used to treat primary hypercholesterolemia and mixed dyslipidemia (Fredrickson types IIa and IIb).
AbsorptionThe mean absolute oral bioavailability 60% (range 39 - 101%).
Protein bindingMore than 99% of the circulating drug is bound to plasma proteins (80% to albumin).
MetabolismHepatic. Biotransformation pathways for cerivastatin in humans include the following: demethylation of the benzylic methyl ether to form Ml and hydroxylation of the methyl group in the 6'-isopropyl moiety to form M23.
Half life2-3 hours
ToxicityRhabdomyolysis, liver concerns
Affected organismsHumans and other mammals
Food interactionsGrapefruit and grapefruit juice should be avoided throughout treatment as grapefruit can significantly increase serum levels of this product. Take without regard to meals.
Taxonomy descriptionThis compound belongs to the class of organic compounds known as phenylpyridines. These are polycyclic aromatic compounds containing a benzene ring linked to a pyridine ring through a CC or CN bond.
KingdomOrganic compounds
Super classOrganoheterocyclic compounds
ClassPyridines and derivatives
Sub classPhenylpyridines
Direct parentPhenylpyridines
Molecular frameworkAromatic heteromonocyclic compounds
External descriptorsstatin (synthetic), pyridines, dihydroxy monocarboxylic acid (CHEBI:3558)