Drug/Small Molecule:
cerivastatin

PharmGKB contains no dosing guidelines for this drug/small molecule. To report known genotype-based dosing guidelines, or if you are interested in developing guidelines, click here.

PharmGKB has no annotated drug labels with pharmacogenomic information for this drug/small molecule. If you know of a drug label with PGx, send us a message.

PharmGKB contains no Clinical Variants that meet the highest level of criteria.

To see more Clinical Variants with lower levels of criteria, click the button at the bottom of the page.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

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This is a non-comprehensive list of genetic tests with pharmacogenetics relevance, typically submitted by the manufacturer and manually curated by PharmGKB. The information listed is provided for educational purposes only and does not constitute an endorsement of any listed test or manufacturer.

A more complete listing of genetic tests is found at the Genetic Testing Registry (GTR).

PGx Test Variants Assayed Gene?

The table below contains information about pharmacogenomic variants on PharmGKB. Please follow the link in the "Variant" column for more information about a particular variant. Each link in the "Variant" column leads to the corresponding PharmGKB Variant Page. The Variant Page contains summary data, including PharmGKB manually curated information about variant-drug pairs based on individual PubMed publications. The PMIDs for these PubMed publications can be found on the Variant Page.

The tags in the first column of the table indicate what type of information can be found on the corresponding Variant Page.

Links in the "Gene" column lead to PharmGKB Gene Pages.

Gene ? Variant?
(138)
Alternate Names / Tag SNPs ? Drugs ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
No VIP available No VIP available VA CYP2C8 *1A N/A N/A N/A
VIP No VIP available VA CYP2C8 *3 N/A N/A N/A
No VIP available No VIP available VA CYP2C8 *4 N/A N/A N/A
VIP No Clinical Annotations available No Variant Annotations available
rs10509681 1196A>G, 35506A>G, 47603213T>C, 890A>G, 96798749T>C, 986A>G, A1196G, CYP2C8*3, CYP2C8: K399R, Lys297Arg, Lys329Arg, Lys399Arg
T > C
Missense
Lys329Arg
VIP No Clinical Annotations available No Variant Annotations available
rs11572080 110G>A, 206G>A, 416G>A, 47631494C>T, 7225G>A, 96827030C>T, Arg139Lys, Arg37Lys, Arg69Lys, CYP2C8*3, CYP2C8: R139K, G416A, R139K, rs11572080 G>A
C > T
Missense
Arg69Lys
No VIP available No Clinical Annotations available VA
rs17238540 2298+117T>G, 2457+117T>G, 25249857T>G, 27506T>G, 74655498T>G, HMGCR:SNP 29
T > G
Intronic
VIP No Clinical Annotations available No Variant Annotations available
rs2306283 14089862A>G, 21329738A>G, 388A>G, 50611A>G, Asn130Asp, SLCO1B1*1B
A > G
Missense
Asn130Asp
No VIP available CA VA
rs2819742 14591-1559A>G, 237990122A>G, 31507901A>G, 789421A>G
A > G
Intronic
VIP No Clinical Annotations available No Variant Annotations available
rs4149015 -910G>A, 14043446G>A, 21283322G>A, 4195G>A, SLCO1B1:11187G>A, SLCO1B1:G-11187A
G > A
5' Flanking
rs4149056 14091673T>C, 21331549T>C, 521T>C, 52422T>C, SLCO1B1*5, Val174Ala
T > C
Missense
Val174Ala
VIP No Clinical Annotations available No Variant Annotations available
rs776746 12083G>A, 219-237G>A, 321-1G>A, 37303382C>T, 581-237G>A, 689-1G>A, 99270539C>T, CYP3A5*1, CYP3A5*3, CYP3A5*3C, CYP3A5:6986A>G, g.6986A>G, intron 3 splicing defect, rs776746 A>G
C > T
Acceptor
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 138
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • Cerivastatin sodium
  • Cerivastatin, sodium salt
Trade Names
  • Baycol
  • Lipobay
  • Rivastatin
Brand Mixture Names

PharmGKB Accession Id:
PA448897

Description

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.

Source: Drug Bank

Indication

Used 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.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Cerivastatin competitively inhibits hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase, the hepatic enzyme responsible for converting HMG-CoA to mevalonate. As mevalonate is a precursor of sterols such as cholesterol, this results in a decrease in cholesterol in hepatic cells, upregulation of LDL-receptors, and an increase in hepatic uptake of LDL-cholesterol from the circulation.

Source: Drug Bank

Pharmacology

Cerivastatin, 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).

Source: Drug Bank

Food Interaction

Grapefruit and grapefruit juice should be avoided throughout treatment as grapefruit can significantly increase serum levels of this product.|Take without regard to meals.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic. 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.

Source: Drug Bank

Protein Binding

More than 99% of the circulating drug is bound to plasma proteins (80% to albumin).

Source: Drug Bank

Absorption

The mean absolute oral bioavailability 60% (range 39 - 101%).

Source: Drug Bank

Half-Life

2-3 hours

Source: Drug Bank

Toxicity

Rhabdomyolysis, liver concerns

Source: Drug Bank

Chemical Properties

Chemical Formula

C26H34FNO5

Source: Drug Bank

Isomeric SMILES

CC(C)c1c(c(c(c(n1)C(C)C)/C=C/[C@H](C[C@H](CC(=O)O)O)O)c2ccc(cc2)F)COC

Source: OpenEye

Canonical SMILES

COCC1=C(C2=CC=C(F)C=C2)C(\C=C\[C@@H](O)C[C@@H]

Source: Drug Bank

Average Molecular Weight

459.5503

Source: Drug Bank

Monoisotopic Molecular Weight

459.242101408

Source: Drug Bank

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

Drug Targets

Gene Description
HMGCR (source: Drug Bank)

Drug Interactions

Drug Description
cerivastatin Bosentan could decrease the statin effect (source: Drug Bank)
cerivastatin Bosentan could decrease the statin effect (source: Drug Bank)
bezafibrate Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
bezafibrate Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
bosentan Bosentan could decrease the statin effect (source: Drug Bank)
bosentan Bosentan could decrease the statin effect (source: Drug Bank)
clarithromycin The macrolide possibly increases the statin toxicity (source: Drug Bank)
clarithromycin The macrolide, clarithromycin, may increase the toxicity of the statin, cerivastatin. (source: Drug Bank)
colchicine Increased risk of rhabdomyolysis with this combination (source: Drug Bank)
colchicine Increased risk of rhabdomyolysis with this combination (source: Drug Bank)
cyclosporine Possible myopathy and rhabdomyolysis (source: Drug Bank)
cyclosporine Possible myopathy and rhabdomyolysis (source: Drug Bank)
diltiazem Diltiazem increases the effect and toxicity of the statin (source: Drug Bank)
diltiazem Diltiazem increases the effect and toxicity of the statin (source: Drug Bank)
erythromycin The macrolide possibly increases the statin toxicity (source: Drug Bank)
erythromycin The macrolide, erythromycin, may increase the toxicity of the statin, cerivastatin. (source: Drug Bank)
fenofibrate Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
fenofibrate Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
gemfibrozil Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
gemfibrozil Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
imatinib Imatinib increases the effect and toxicity of statin (source: Drug Bank)
imatinib Imatinib increases the effect and toxicity of statin (source: Drug Bank)
itraconazole Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
itraconazole Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
josamycin The macrolide, josamycin, may increase the toxicity of the statin, cerivastatin. (source: Drug Bank)
ketoconazole Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
ketoconazole Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
nefazodone Nefazodone increases the effect and toxicity of the statin drug (source: Drug Bank)
nefazodone Nefazodone increases the effect and toxicity of the statin drug (source: Drug Bank)
quinupristin This combination presents an increased risk of toxicity (source: Drug Bank)
rifabutin The rifamycin decreases the effect of statin drug (source: Drug Bank)
rifabutin The rifamycin decreases the effect of statin drug (source: Drug Bank)
rifampin The rifamycin decreases the effect of statin drug (source: Drug Bank)
rifampin The rifamycin decreases the effect of statin drug (source: Drug Bank)
cerivastatin The macrolide possibly increases the statin toxicity (source: Drug Bank)
cerivastatin The macrolide, clarithromycin, may increase the toxicity of the statin, cerivastatin. (source: Drug Bank)
cerivastatin Increased risk of rhabdomyolysis with this combination (source: Drug Bank)
cerivastatin Increased risk of rhabdomyolysis with this combination (source: Drug Bank)
cerivastatin Possible myopathy and rhabdomyolysis (source: Drug Bank)
cerivastatin Possible myopathy and rhabdomyolysis (source: Drug Bank)
cerivastatin Increases the effect and toxicity of the statin (source: Drug Bank)
cerivastatin Increases the effect and toxicity of the statin (source: Drug Bank)
cerivastatin The macrolide possibly increases the statin toxicity (source: Drug Bank)
cerivastatin The macrolide, erythromycin, may increase the toxicity of the statin, cerivastatin. (source: Drug Bank)
cerivastatin Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
cerivastatin Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
cerivastatin Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
cerivastatin Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
cerivastatin Imatinib increases the effect and toxicity of statin (source: Drug Bank)
cerivastatin Imatinib increases the effect and toxicity of statin (source: Drug Bank)
cerivastatin Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
cerivastatin Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
cerivastatin Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
cerivastatin Increased risk of myopathy/rhabdomyolysis (source: Drug Bank)
cerivastatin Nefazodone increases the effect and toxicity of the statin drug (source: Drug Bank)
cerivastatin Nefazodone increases the effect and toxicity of the statin drug (source: Drug Bank)
cerivastatin This combination presents an increased risk of toxicity (source: Drug Bank)
cerivastatin The rifamycin decreases the effect of the statin drug (source: Drug Bank)
cerivastatin The rifamycin decreases the effect of the statin drug (source: Drug Bank)
cerivastatin The rifamycin decreases the effect of the statin drug (source: Drug Bank)
cerivastatin The rifamycin decreases the effect of the statin drug (source: Drug Bank)

Curated Information ?

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
May Prevent
Contraindicated With

Publications related to cerivastatin: 17

No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
PharmGKB summary: very important pharmacogene information for cytochrome P450, family 2, subfamily C, polypeptide 8. Pharmacogenetics and genomics. 2013. Aquilante Christina L, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
PharmGKB summary: very important pharmacogene information for CYP3A5. Pharmacogenetics and genomics. 2012. Lamba Jatinder, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pharmacogenetics of drugs withdrawn from the market. Pharmacogenomics. 2012. Zhang Wei, et al. PubMed
Cerivastatin, genetic variants, and the risk of rhabdomyolysis. Pharmacogenetics and genomics. 2011. Marciante Kristin D, et al. PubMed
Cerivastatin in vitro metabolism by CYP2C8 variants found in patients experiencing rhabdomyolysis. Pharmacogenetics and genomics. 2010. Kaspera RĂ¼diger, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
PharmGKB very important pharmacogene: SLCO1B1. Pharmacogenetics and genomics. 2010. Oshiro Connie, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available VA No VIP available No VIP available
A paucimorphic variant in the HMG-CoA reductase gene is associated with lipid-lowering response to statin treatment in diabetes: a GoDARTS study. Pharmacogenetics and genomics. 2008. Donnelly Louise A, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Xenobiotic transporters of the human organic anion transporting polypeptides (OATP) family. Xenobiotica; the fate of foreign compounds in biological systems. 2008. Hagenbuch B, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
CYP2D6*4 polymorphism is associated with statin-induced muscle effects. Pharmacogenetics and genomics. 2007. Frudakis Tony N, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Genetic risk factors associated with lipid-lowering drug-induced myopathies. Muscle & nerve. 2006. Vladutiu Georgirene D, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Drug interactions with lipid-lowering drugs: mechanisms and clinical relevance. Clinical pharmacology and therapeutics. 2006. Neuvonen Pertti J, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Organic anion transporting polypeptide 2B1 is a high-affinity transporter for atorvastatin and is expressed in the human heart. Clinical pharmacology and therapeutics. 2006. Grube Markus, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Functional characterization of SLCO1B1 (OATP-C) variants, SLCO1B1*5, SLCO1B1*15 and SLCO1B1*15+C1007G, by using transient expression systems of HeLa and HEK293 cells. Pharmacogenetics and genomics. 2005. Kameyama Yoshio, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
A frameshift variant of CYP2C8 was identified in a patient who suffered from rhabdomyolysis after administration of cerivastatin. Journal of human genetics. 2004. Ishikawa Chikako, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Cerivastatin and reports of fatal rhabdomyolysis. The New England journal of medicine. 2002. Staffa Judy A, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Med-psych drug-drug interactions update. Psychosomatics. 2002. Armstrong Scott C, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Equally potent inhibitors of cholesterol synthesis in human hepatocytes have distinguishable effects on different cytochrome P450 enzymes. Biopharmaceutics & drug disposition. 2000. Cohen L H, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB00439
PDB:
116
ChEBI:
3558
KEGG Compound:
C07966
PubChem Compound:
446156
PubChem Substance:
206660
46505877
Drugs Product Database (DPD):
2237325
BindingDB:
18376
ChemSpider:
393588

Clinical Trials

These are trials that mention cerivastatin and are related to either pharmacogenetics or pharmacogenomics.

Common Searches

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Sources for PharmGKB drug information: DrugBank, Open Eye Scientific Software.