Cerivastatin
A synthetic HMG-CoA reductase inhibitor (statin) used to lower LDL cholesterol and reduce cardiovascular risk. It was voluntarily withdrawn from the worldwide market in 2001 due to an unacceptably high incidence of potentially fatal rhabdomyolysis, particularly when combined with gemfibrozil. It represents an important pharmacovigilance case study in post-marketing drug safety.
Molecular Weight
459.5000 g/mol
LogP
3.60
TPSA
99.90 Ų
Lipinski RO5
Pass
Therapeutic Areas
Mechanism of Action
Competitively inhibits HMG-CoA reductase, the rate-limiting enzyme in the mevalonate pathway of cholesterol biosynthesis. This reduces intracellular cholesterol, upregulates LDL receptor expression, and lowers circulating LDL cholesterol.
Pharmacokinetics (PK)
Pharmacodynamics (PD)
Competitively inhibits HMG-CoA reductase, the rate-limiting enzyme in the mevalonate pathway of cholesterol biosynthesis. This reduces intracellular cholesterol, upregulates LDL receptor expression, and lowers circulating LDL cholesterol.
2D Structure
Cite this structure
Embed this structure
SMILES
COCc1c(C(C)C)nc(C(C)C)c(/C=C/[C@@H](O)C[C@@H](O)CC(=O)O)c1-c1ccc(F)cc1
InChI
InChI=1S/C26H34FNO5/c1-15(2)25-21(11-10-19(29)12-20(30)13-23(31)32)24(17-6-8-18(27)9-7-17)22(14-33-5)26(28-25)16(3)4/h6-11,15-16,19-20,29-30H,12-14H2,1-5H3,(H,31,32)/b11-10+/t19-,20-/m1/s1
Molecular Formula
C26H34FNO5
HBD / HBA
3 / 7
Rotatable Bonds
11
Heavy Atoms
33
No targets recorded
Target interaction data is not yet available for this drug.
No interactions recorded
Drug interaction data is not yet available for this compound.
No side effects recorded
Side effect data is not yet available for this drug.
Frequently Asked Questions
A synthetic HMG-CoA reductase inhibitor (statin) used to lower LDL cholesterol and reduce cardiovascular risk. It was voluntarily withdrawn from the worldwide market in 2001 due to an unacceptably high incidence of potentially fatal rhabdomyolysis, particularly when combined with gemfibrozil. It represents an important pharmacovigilance case study in post-marketing drug safety.
Competitively inhibits HMG-CoA reductase, the rate-limiting enzyme in the mevalonate pathway of cholesterol biosynthesis. This reduces intracellular cholesterol, upregulates LDL receptor expression, and lowers circulating LDL cholesterol.
Yes, Cerivastatin is an approved drug. It has reached clinical phase 4. It is classified as a Small molecule.
References & Data Sources
- ChEMBL — European Bioinformatics Institute (EBI). CHEMBL1477. Open-access bioactivity database.
- PubChem — National Center for Biotechnology Information (NCBI). CID 446156. Chemical information database.
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-04.
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