Identification

Name
Cerivastatin
Accession Number
DB00439  (APRD00102)
Type
Small Molecule
Groups
Withdrawn
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 It has also been withdrawn from the Canadian market.

Structure
Thumb
Synonyms
Not Available
Product Ingredients
IngredientUNIICASInChI Key
Cerivastatin sodium6Q18G1060S143201-11-0GPUADMRJQVPIAS-ASTDGNLGSA-M
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
BaycolTablet0.8 mgOralBayer2000-12-282001-10-26Canada
BaycolTablet0.4 mgOralBayer2000-01-062001-10-26Canada
Baycol (0.2mg)Tablet0.2 mgOralBayer1998-03-112001-10-26Canada
Baycol (0.3mg)Tablet0.3 mgOralBayer1998-03-112001-10-26Canada
International/Other Brands
Lipobay / Rivastatin
Categories
UNII
AM91H2KS67
CAS number
145599-86-6
Weight
Average: 459.5503
Monoisotopic: 459.242101408
Chemical Formula
C26H34FNO5
InChI Key
SEERZIQQUAZTOL-ANMDKAQQSA-N
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
IUPAC Name
(3R,5S,6E)-7-[4-(4-fluorophenyl)-5-(methoxymethyl)-2,6-bis(propan-2-yl)pyridin-3-yl]-3,5-dihydroxyhept-6-enoic acid
SMILES
COCC1=C(C2=CC=C(F)C=C2)C(\C=C\[[email protected]@H](O)C[[email protected]@H](O)CC(O)=O)=C(C(C)C)N=C1C(C)C

Pharmacology

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.

Structured Indications
Not Available
Pharmacodynamics

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).

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.

TargetActionsOrganism
A3-hydroxy-3-methylglutaryl-coenzyme A reductase
inhibitor
Human
Absorption

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

Volume of distribution
Not Available
Protein binding

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

Metabolism

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.

Route of elimination
Not Available
Half life

2-3 hours

Clearance
Not Available
Toxicity

Rhabdomyolysis, liver concerns

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Cerivastatin Action PathwayDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AbafunginThe risk or severity of adverse effects can be increased when Abafungin is combined with Cerivastatin.Investigational
AbirateroneThe serum concentration of Cerivastatin can be increased when it is combined with Abiraterone.Approved
AcenocoumarolCerivastatin may increase the anticoagulant activities of Acenocoumarol.Approved
AcetaminophenThe serum concentration of Cerivastatin can be increased when it is combined with Acetaminophen.Approved
AcetazolamideThe serum concentration of Cerivastatin can be increased when it is combined with Acetazolamide.Approved, Vet Approved
AcipimoxAcipimox may increase the myopathic rhabdomyolysis activities of Cerivastatin.Approved, Investigational
AlbaconazoleThe risk or severity of adverse effects can be increased when Albaconazole is combined with Cerivastatin.Investigational
AldesleukinThe serum concentration of Cerivastatin can be increased when it is combined with Aldesleukin.Approved
AlgeldrateThe serum concentration of Cerivastatin can be decreased when it is combined with Algeldrate.Approved, Experimental
AlmagateThe serum concentration of Cerivastatin can be decreased when it is combined with Almagate.Experimental
AlmasilateThe serum concentration of Cerivastatin can be decreased when it is combined with Almasilate.Approved, Experimental
AloglutamolThe serum concentration of Cerivastatin can be decreased when it is combined with Aloglutamol.Experimental
AlprazolamThe serum concentration of Cerivastatin can be increased when it is combined with Alprazolam.Approved, Illicit, Investigational
AluminiumThe serum concentration of Cerivastatin can be decreased when it is combined with Aluminium.Approved
Aluminium acetoacetateThe serum concentration of Cerivastatin can be decreased when it is combined with Aluminium acetoacetate.Experimental
Aluminium glycinateThe serum concentration of Cerivastatin can be decreased when it is combined with Aluminium glycinate.Experimental
Aluminum hydroxideThe serum concentration of Cerivastatin can be decreased when it is combined with Aluminum hydroxide.Approved
AmbroxolThe serum concentration of Cerivastatin can be increased when it is combined with Ambroxol.Approved, Investigational
AmiodaroneThe metabolism of Cerivastatin can be decreased when combined with Amiodarone.Approved, Investigational
AmlodipineThe serum concentration of Cerivastatin can be increased when it is combined with Amlodipine.Approved
AmodiaquineThe serum concentration of Amodiaquine can be increased when it is combined with Cerivastatin.Approved, Investigational
AmprenavirThe serum concentration of Cerivastatin can be increased when it is combined with Amprenavir.Approved
AmrinoneThe risk or severity of adverse effects can be increased when Amrinone is combined with Cerivastatin.Approved
AnastrozoleThe serum concentration of Cerivastatin can be increased when it is combined with Anastrozole.Approved, Investigational
AntipyrineThe serum concentration of Cerivastatin can be increased when it is combined with Antipyrine.Approved
AprepitantThe serum concentration of Cerivastatin can be increased when it is combined with Aprepitant.Approved, Investigational
AripiprazoleThe serum concentration of Aripiprazole can be decreased when it is combined with Cerivastatin.Approved, Investigational
Arsenic trioxideThe serum concentration of Cerivastatin can be increased when it is combined with Arsenic trioxide.Approved, Investigational
AstemizoleThe serum concentration of Cerivastatin can be increased when it is combined with Astemizole.Approved, Withdrawn
AtazanavirThe metabolism of Cerivastatin can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Cerivastatin can be decreased when combined with Atomoxetine.Approved
AtorvastatinThe risk or severity of adverse effects can be increased when Cerivastatin is combined with Atorvastatin.Approved
AzelastineThe serum concentration of Cerivastatin can be increased when it is combined with Azelastine.Approved
AzelnidipineThe risk or severity of adverse effects can be increased when Azelnidipine is combined with Cerivastatin.Approved, Investigational
AzimilideThe risk or severity of adverse effects can be increased when Azimilide is combined with Cerivastatin.Investigational
AzithromycinThe serum concentration of Cerivastatin can be increased when it is combined with Azithromycin.Approved
BarnidipineThe risk or severity of adverse effects can be increased when Barnidipine is combined with Cerivastatin.Approved
BencyclaneThe risk or severity of adverse effects can be increased when Bencyclane is combined with Cerivastatin.Experimental
BenidipineThe risk or severity of adverse effects can be increased when Benidipine is combined with Cerivastatin.Approved, Investigational
BepridilThe risk or severity of adverse effects can be increased when Bepridil is combined with Cerivastatin.Approved, Withdrawn
BetamethasoneThe serum concentration of Cerivastatin can be increased when it is combined with Betamethasone.Approved, Vet Approved
BezafibrateBezafibrate may increase the myopathic rhabdomyolysis activities of Cerivastatin.Approved
BicalutamideThe serum concentration of Cerivastatin can be increased when it is combined with Bicalutamide.Approved
BifonazoleThe serum concentration of Cerivastatin can be increased when it is combined with Bifonazole.Approved, Investigational
Bismuth SubcitrateThe serum concentration of Cerivastatin can be decreased when it is combined with Bismuth Subcitrate.Approved
Bismuth subnitrateThe serum concentration of Cerivastatin can be decreased when it is combined with Bismuth subnitrate.Experimental
BoceprevirThe metabolism of Cerivastatin can be decreased when combined with Boceprevir.Approved, Withdrawn
BortezomibThe metabolism of Cerivastatin can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe metabolism of Cerivastatin can be increased when combined with Bosentan.Approved, Investigational
Brentuximab vedotinThe serum concentration of Cerivastatin can be increased when it is combined with Brentuximab vedotin.Approved
BromocriptineThe serum concentration of Cerivastatin can be increased when it is combined with Bromocriptine.Approved, Investigational
BuprenorphineThe serum concentration of Cerivastatin can be increased when it is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
ButoconazoleThe risk or severity of adverse effects can be increased when Butoconazole is combined with Cerivastatin.Approved
CabergolineThe serum concentration of Cerivastatin can be increased when it is combined with Cabergoline.Approved
CaffeineThe serum concentration of Cerivastatin can be increased when it is combined with Caffeine.Approved
Calcium CarbonateThe serum concentration of Cerivastatin can be decreased when it is combined with Calcium Carbonate.Approved
Calcium silicateThe serum concentration of Cerivastatin can be decreased when it is combined with Calcium silicate.Experimental
CapsaicinThe serum concentration of Cerivastatin can be increased when it is combined with Capsaicin.Approved
CarbamazepineThe metabolism of Cerivastatin can be increased when combined with Carbamazepine.Approved, Investigational
CarbomycinThe risk or severity of adverse effects can be increased when Carbomycin is combined with Cerivastatin.Vet Approved
CarboxyamidotriazoleThe risk or severity of adverse effects can be increased when Carboxyamidotriazole is combined with Cerivastatin.Investigational
CaroverineThe risk or severity of adverse effects can be increased when Caroverine is combined with Cerivastatin.Experimental
CaspofunginThe serum concentration of Cerivastatin can be increased when it is combined with Caspofungin.Approved
CelecoxibThe metabolism of Cerivastatin can be decreased when combined with Celecoxib.Approved, Investigational
CeritinibThe serum concentration of Cerivastatin can be increased when it is combined with Ceritinib.Approved
ChloramphenicolThe serum concentration of Cerivastatin can be increased when it is combined with Chloramphenicol.Approved, Vet Approved
ChlorzoxazoneThe serum concentration of Cerivastatin can be increased when it is combined with Chlorzoxazone.Approved
CilnidipineThe risk or severity of adverse effects can be increased when Cilnidipine is combined with Cerivastatin.Approved, Investigational
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Cerivastatin.Approved
CimetidineThe serum concentration of Cerivastatin can be increased when it is combined with Cimetidine.Approved
CinnarizineThe risk or severity of adverse effects can be increased when Cinnarizine is combined with Cerivastatin.Approved, Investigational
CiprofibrateThe risk or severity of adverse effects can be increased when Ciprofibrate is combined with Cerivastatin.Approved, Investigational
CiprofloxacinThe serum concentration of Cerivastatin can be increased when it is combined with Ciprofloxacin.Approved, Investigational
CisaprideThe serum concentration of Cerivastatin can be increased when it is combined with Cisapride.Approved, Investigational, Withdrawn
ClarithromycinThe metabolism of Cerivastatin can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Cerivastatin can be decreased when combined with Clemastine.Approved
ClevidipineThe risk or severity of adverse effects can be increased when Clevidipine is combined with Cerivastatin.Approved
ClindamycinThe serum concentration of Cerivastatin can be increased when it is combined with Clindamycin.Approved, Vet Approved
ClofazimineThe serum concentration of Cerivastatin can be increased when it is combined with Clofazimine.Approved, Investigational
ClomifeneThe serum concentration of Cerivastatin can be increased when it is combined with Clomifene.Approved, Investigational
ClorindioneCerivastatin may increase the anticoagulant activities of Clorindione.Experimental
ClotiazepamThe serum concentration of Cerivastatin can be increased when it is combined with Clotiazepam.Approved, Illicit
ClotrimazoleThe metabolism of Cerivastatin can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe serum concentration of Cerivastatin can be increased when it is combined with Clozapine.Approved
CobicistatThe metabolism of Cerivastatin can be decreased when combined with Cobicistat.Approved
CocaineThe serum concentration of Cerivastatin can be increased when it is combined with Cocaine.Approved, Illicit
ColchicineColchicine may increase the myopathic rhabdomyolysis activities of Cerivastatin.Approved
ConivaptanThe serum concentration of Cerivastatin can be increased when it is combined with Conivaptan.Approved, Investigational
Cortisone acetateThe serum concentration of Cerivastatin can be increased when it is combined with Cortisone acetate.Approved
CrisaboroleThe metabolism of Cerivastatin can be decreased when combined with Crisaborole.Approved
CrizotinibThe metabolism of Cerivastatin can be decreased when combined with Crizotinib.Approved
CyclophosphamideThe serum concentration of Cerivastatin can be increased when it is combined with Cyclophosphamide.Approved, Investigational
CyclosporineThe metabolism of Cerivastatin can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
Cyproterone acetateThe serum concentration of Cerivastatin can be increased when it is combined with Cyproterone acetate.Approved, Investigational
DabrafenibThe serum concentration of Cerivastatin can be decreased when it is combined with Dabrafenib.Approved
DaclatasvirThe serum concentration of Cerivastatin can be increased when it is combined with Daclatasvir.Approved
DalfopristinThe serum concentration of Cerivastatin can be increased when it is combined with Dalfopristin.Approved
DanazolThe serum concentration of Cerivastatin can be increased when it is combined with Danazol.Approved
DaptomycinThe risk or severity of adverse effects can be increased when Cerivastatin is combined with Daptomycin.Approved, Investigational
DarodipineThe risk or severity of adverse effects can be increased when Darodipine is combined with Cerivastatin.Experimental
DarunavirThe metabolism of Cerivastatin can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Cerivastatin can be increased when it is combined with Dasatinib.Approved, Investigational
DaunorubicinThe serum concentration of Cerivastatin can be increased when it is combined with Daunorubicin.Approved
DeferasiroxThe serum concentration of Cerivastatin can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Cerivastatin can be decreased when combined with Delavirdine.Approved
DesipramineThe serum concentration of Cerivastatin can be increased when it is combined with Desipramine.Approved
DexamethasoneThe serum concentration of Cerivastatin can be increased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DextropropoxypheneThe serum concentration of Cerivastatin can be increased when it is combined with Dextropropoxyphene.Approved, Illicit, Investigational, Withdrawn
DiazepamThe serum concentration of Cerivastatin can be increased when it is combined with Diazepam.Approved, Illicit, Vet Approved
DicoumarolCerivastatin may increase the anticoagulant activities of Dicoumarol.Approved
DiethylstilbestrolThe serum concentration of Cerivastatin can be increased when it is combined with Diethylstilbestrol.Approved, Investigational
DihydroergocornineThe risk or severity of adverse effects can be increased when Dihydroergocornine is combined with Cerivastatin.Approved
DihydroergocristineThe risk or severity of adverse effects can be increased when Dihydroergocristine is combined with Cerivastatin.Experimental
DihydroergocryptineThe risk or severity of adverse effects can be increased when Dihydroergocryptine is combined with Cerivastatin.Experimental
DihydroergotamineThe metabolism of Cerivastatin can be decreased when combined with Dihydroergotamine.Approved
DiltiazemThe metabolism of Cerivastatin can be decreased when combined with Diltiazem.Approved
Dimethyl sulfoxideThe serum concentration of Cerivastatin can be increased when it is combined with Dimethyl sulfoxide.Approved, Vet Approved
DiphenadioneCerivastatin may increase the anticoagulant activities of Diphenadione.Experimental
DocetaxelThe serum concentration of Cerivastatin can be increased when it is combined with Docetaxel.Approved, Investigational
DotarizineThe risk or severity of adverse effects can be increased when Dotarizine is combined with Cerivastatin.Investigational
DoxorubicinThe serum concentration of Cerivastatin can be increased when it is combined with Doxorubicin.Approved, Investigational
DoxycyclineThe metabolism of Cerivastatin can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Cerivastatin can be decreased when combined with Dronedarone.Approved
EconazoleThe serum concentration of Cerivastatin can be increased when it is combined with Econazole.Approved
EfavirenzThe metabolism of Cerivastatin can be decreased when combined with Efavirenz.Approved, Investigational
EfinaconazoleThe risk or severity of adverse effects can be increased when Efinaconazole is combined with Cerivastatin.Approved
EfonidipineThe risk or severity of adverse effects can be increased when Efonidipine is combined with Cerivastatin.Approved, Investigational
ElbasvirThe serum concentration of Cerivastatin can be increased when it is combined with Elbasvir.Approved
EltrombopagThe serum concentration of Cerivastatin can be increased when it is combined with Eltrombopag.Approved
EnasidenibThe serum concentration of Cerivastatin can be increased when it is combined with Enasidenib.Approved
EnzalutamideThe serum concentration of Cerivastatin can be decreased when it is combined with Enzalutamide.Approved
EperisoneThe risk or severity of adverse effects can be increased when Eperisone is combined with Cerivastatin.Approved, Investigational
EpinephrineThe serum concentration of Cerivastatin can be increased when it is combined with Epinephrine.Approved, Vet Approved
Ergoloid mesylateThe serum concentration of Cerivastatin can be increased when it is combined with Ergoloid mesylate.Approved
ErgonovineThe serum concentration of Cerivastatin can be increased when it is combined with Ergonovine.Approved
ErgotamineThe serum concentration of Cerivastatin can be increased when it is combined with Ergotamine.Approved
ErythromycinThe metabolism of Cerivastatin can be decreased when combined with Erythromycin.Approved, Vet Approved
EthanolThe serum concentration of Cerivastatin can be increased when it is combined with Ethanol.Approved
Ethyl biscoumacetateCerivastatin may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
EtoposideThe serum concentration of Cerivastatin can be increased when it is combined with Etoposide.Approved
EtoricoxibThe serum concentration of Cerivastatin can be increased when it is combined with Etoricoxib.Approved, Investigational
EtravirineThe serum concentration of Cerivastatin can be decreased when it is combined with Etravirine.Approved
EzetimibeThe serum concentration of Cerivastatin can be increased when it is combined with Ezetimibe.Approved
FelodipineThe metabolism of Cerivastatin can be decreased when combined with Felodipine.Approved, Investigational
FendilineThe risk or severity of adverse effects can be increased when Fendiline is combined with Cerivastatin.Withdrawn
FenofibrateThe risk or severity of adverse effects can be increased when Fenofibrate is combined with Cerivastatin.Approved
FentanylThe serum concentration of Cerivastatin can be increased when it is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FenticonazoleThe risk or severity of adverse effects can be increased when Fenticonazole is combined with Cerivastatin.Experimental
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Cerivastatin.Approved
FidaxomicinThe risk or severity of adverse effects can be increased when Fidaxomicin is combined with Cerivastatin.Approved
FluconazoleThe metabolism of Cerivastatin can be decreased when combined with Fluconazole.Approved
FluindioneCerivastatin may increase the anticoagulant activities of Fluindione.Investigational
FlunarizineThe risk or severity of adverse effects can be increased when Flunarizine is combined with Cerivastatin.Approved
FluoxetineThe serum concentration of Cerivastatin can be increased when it is combined with Fluoxetine.Approved, Vet Approved
Fluticasone propionateThe serum concentration of Cerivastatin can be increased when it is combined with Fluticasone propionate.Approved
FluvastatinThe serum concentration of Cerivastatin can be increased when it is combined with Fluvastatin.Approved
FluvoxamineThe metabolism of Cerivastatin can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Cerivastatin can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Cerivastatin can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe serum concentration of Cerivastatin can be decreased when it is combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Cerivastatin can be increased when it is combined with Fusidic Acid.Approved
GabapentinThe risk or severity of adverse effects can be increased when Gabapentin is combined with Cerivastatin.Approved, Investigational
GallopamilThe risk or severity of adverse effects can be increased when Gallopamil is combined with Cerivastatin.Investigational
GemfibrozilThe serum concentration of Cerivastatin can be increased when it is combined with Gemfibrozil.Approved
GlyburideThe serum concentration of Cerivastatin can be increased when it is combined with Glyburide.Approved
Glycerol PhenylbutyrateThe serum concentration of Cerivastatin can be increased when it is combined with Glycerol Phenylbutyrate.Approved
HaloperidolThe serum concentration of Cerivastatin can be increased when it is combined with Haloperidol.Approved
HistamineThe serum concentration of Cerivastatin can be increased when it is combined with Histamine.Approved, Investigational
HydralazineThe serum concentration of Cerivastatin can be increased when it is combined with Hydralazine.Approved
HydrocortisoneThe serum concentration of Cerivastatin can be increased when it is combined with Hydrocortisone.Approved, Vet Approved
HydrotalciteThe serum concentration of Cerivastatin can be decreased when it is combined with Hydrotalcite.Experimental, Investigational
IdelalisibThe serum concentration of Cerivastatin can be increased when it is combined with Idelalisib.Approved
IfosfamideThe serum concentration of Cerivastatin can be increased when it is combined with Ifosfamide.Approved
IloperidoneThe serum concentration of Cerivastatin can be increased when it is combined with Iloperidone.Approved
ImatinibThe metabolism of Cerivastatin can be decreased when combined with Imatinib.Approved
IndinavirThe metabolism of Cerivastatin can be decreased when combined with Indinavir.Approved
indisulamThe serum concentration of Cerivastatin can be increased when it is combined with indisulam.Investigational
IrbesartanThe metabolism of Cerivastatin can be decreased when combined with Irbesartan.Approved, Investigational
IrinotecanThe serum concentration of Cerivastatin can be increased when it is combined with Irinotecan.Approved, Investigational
IsavuconazoleThe risk or severity of adverse effects can be increased when Isavuconazole is combined with Cerivastatin.Approved, Investigational
IsavuconazoniumThe metabolism of Cerivastatin can be decreased when combined with Isavuconazonium.Approved, Investigational
IsoconazoleThe risk or severity of adverse effects can be increased when Isoconazole is combined with Cerivastatin.Approved
IsoniazidThe serum concentration of Cerivastatin can be increased when it is combined with Isoniazid.Approved
IsradipineThe metabolism of Cerivastatin can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Cerivastatin can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Cerivastatin can be increased when it is combined with Ivacaftor.Approved
JosamycinThe serum concentration of Cerivastatin can be increased when it is combined with Josamycin.Approved, Investigational
KetazolamThe serum concentration of Cerivastatin can be increased when it is combined with Ketazolam.Approved
KetoconazoleThe metabolism of Cerivastatin can be decreased when combined with Ketoconazole.Approved, Investigational
KitasamycinThe risk or severity of adverse effects can be increased when Kitasamycin is combined with Cerivastatin.Experimental
LacidipineThe risk or severity of adverse effects can be increased when Lacidipine is combined with Cerivastatin.Approved, Investigational
LamotrigineThe risk or severity of adverse effects can be increased when Lamotrigine is combined with Cerivastatin.Approved, Investigational
LansoprazoleThe serum concentration of Cerivastatin can be increased when it is combined with Lansoprazole.Approved, Investigational
Lanthanum carbonateThe serum concentration of Lanthanum carbonate can be decreased when it is combined with Cerivastatin.Approved
LapatinibThe metabolism of Cerivastatin can be decreased when combined with Lapatinib.Approved, Investigational
LercanidipineThe serum concentration of Cerivastatin can be increased when it is combined with Lercanidipine.Approved, Investigational
LevofloxacinThe serum concentration of Cerivastatin can be increased when it is combined with Levofloxacin.Approved, Investigational
LevosalbutamolThe serum concentration of Cerivastatin can be increased when it is combined with Levosalbutamol.Approved
LidocaineThe serum concentration of Cerivastatin can be increased when it is combined with Lidocaine.Approved, Vet Approved
LidoflazineThe risk or severity of adverse effects can be increased when Lidoflazine is combined with Cerivastatin.Experimental
LinagliptinThe serum concentration of Cerivastatin can be increased when it is combined with Linagliptin.Approved
LisurideThe risk or severity of adverse effects can be increased when Lisuride is combined with Cerivastatin.Approved, Investigational
LomitapideThe serum concentration of Cerivastatin can be increased when it is combined with Lomitapide.Approved
LomustineThe serum concentration of Cerivastatin can be increased when it is combined with Lomustine.Approved
LopinavirThe metabolism of Cerivastatin can be decreased when combined with Lopinavir.Approved
LoratadineThe serum concentration of Cerivastatin can be increased when it is combined with Loratadine.Approved
LosartanThe metabolism of Cerivastatin can be decreased when combined with Losartan.Approved
LovastatinThe metabolism of Cerivastatin can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Cerivastatin can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Cerivastatin can be increased when it is combined with Lumacaftor.Approved
LurasidoneThe serum concentration of Cerivastatin can be increased when it is combined with Lurasidone.Approved
Lysergic Acid DiethylamideThe risk or severity of adverse effects can be increased when Lysergic Acid Diethylamide is combined with Cerivastatin.Illicit, Investigational, Withdrawn
MagaldrateThe serum concentration of Cerivastatin can be decreased when it is combined with Magaldrate.Approved, Withdrawn
Magnesium HydroxideThe serum concentration of Cerivastatin can be decreased when it is combined with Magnesium Hydroxide.Approved
Magnesium oxideThe serum concentration of Cerivastatin can be decreased when it is combined with Magnesium oxide.Approved
Magnesium peroxideThe serum concentration of Cerivastatin can be decreased when it is combined with Magnesium peroxide.Experimental
Magnesium silicateThe serum concentration of Cerivastatin can be decreased when it is combined with Magnesium silicate.Approved, Experimental
Magnesium SulfateThe risk or severity of adverse effects can be increased when Magnesium Sulfate is combined with Cerivastatin.Approved, Vet Approved
Magnesium TrisilicateThe serum concentration of Cerivastatin can be decreased when it is combined with Magnesium Trisilicate.Approved
ManidipineThe serum concentration of Cerivastatin can be increased when it is combined with Manidipine.Approved, Investigational
MefloquineThe serum concentration of Cerivastatin can be increased when it is combined with Mefloquine.Approved
MequitazineThe serum concentration of Cerivastatin can be increased when it is combined with Mequitazine.Approved
MetergolineThe risk or severity of adverse effects can be increased when Metergoline is combined with Cerivastatin.Experimental
MethadoneThe serum concentration of Cerivastatin can be increased when it is combined with Methadone.Approved
MethazolamideThe serum concentration of Cerivastatin can be increased when it is combined with Methazolamide.Approved
MethimazoleThe serum concentration of Cerivastatin can be increased when it is combined with Methimazole.Approved
MethylergometrineThe serum concentration of Cerivastatin can be increased when it is combined with Methylergometrine.Approved
MethylprednisoloneThe serum concentration of Cerivastatin can be increased when it is combined with Methylprednisolone.Approved, Vet Approved
MethysergideThe risk or severity of adverse effects can be increased when Methysergide is combined with Cerivastatin.Approved
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Cerivastatin.Approved, Investigational
MetronidazoleThe serum concentration of Cerivastatin can be increased when it is combined with Metronidazole.Approved
MetyraponeThe serum concentration of Cerivastatin can be increased when it is combined with Metyrapone.Approved
MevastatinThe serum concentration of Mevastatin can be increased when it is combined with Cerivastatin.Experimental
MibefradilThe serum concentration of Cerivastatin can be increased when it is combined with Mibefradil.Investigational, Withdrawn
MiconazoleThe serum concentration of Cerivastatin can be increased when it is combined with Miconazole.Approved, Investigational, Vet Approved
MidazolamThe serum concentration of Cerivastatin can be increased when it is combined with Midazolam.Approved, Illicit
MifepristoneThe serum concentration of Cerivastatin can be increased when it is combined with Mifepristone.Approved, Investigational
MirtazapineThe serum concentration of Cerivastatin can be increased when it is combined with Mirtazapine.Approved
MitotaneThe serum concentration of Cerivastatin can be decreased when it is combined with Mitotane.Approved
MitoxantroneThe serum concentration of Cerivastatin can be increased when it is combined with Mitoxantrone.Approved, Investigational
ModafinilThe serum concentration of Cerivastatin can be increased when it is combined with Modafinil.Approved, Investigational
NaftopidilThe risk or severity of adverse effects can be increased when Naftopidil is combined with Cerivastatin.Investigational
NefazodoneThe metabolism of Cerivastatin can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Cerivastatin can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Cerivastatin can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Cerivastatin can be increased when combined with Nevirapine.Approved
NiacinThe risk or severity of adverse effects can be increased when Niacin is combined with Cerivastatin.Approved, Investigational, Nutraceutical
NicardipineThe serum concentration of Cerivastatin can be increased when it is combined with Nicardipine.Approved
NicergolineThe risk or severity of adverse effects can be increased when Nicergoline is combined with Cerivastatin.Approved, Investigational
NicotinamideThe risk or severity of adverse effects can be increased when Nicotinamide is combined with Cerivastatin.Approved
NifedipineThe serum concentration of Cerivastatin can be increased when it is combined with Nifedipine.Approved
NiguldipineThe risk or severity of adverse effects can be increased when Niguldipine is combined with Cerivastatin.Experimental
NilotinibThe metabolism of Cerivastatin can be decreased when combined with Nilotinib.Approved, Investigational
NiludipineThe risk or severity of adverse effects can be increased when Niludipine is combined with Cerivastatin.Experimental
NilvadipineThe serum concentration of Cerivastatin can be increased when it is combined with Nilvadipine.Approved, Investigational
NimesulideThe risk or severity of adverse effects can be increased when Nimesulide is combined with Cerivastatin.Approved, Investigational, Withdrawn
NimodipineThe risk or severity of adverse effects can be increased when Nimodipine is combined with Cerivastatin.Approved
NisoldipineThe serum concentration of Cerivastatin can be increased when it is combined with Nisoldipine.Approved
NitrendipineThe serum concentration of Cerivastatin can be increased when it is combined with Nitrendipine.Approved, Investigational
Nitric OxideThe serum concentration of Cerivastatin can be increased when it is combined with Nitric Oxide.Approved
NorfloxacinThe serum concentration of Cerivastatin can be increased when it is combined with Norfloxacin.Approved
NoscapineThe serum concentration of Cerivastatin can be increased when it is combined with Noscapine.Investigational
OlanzapineThe serum concentration of Cerivastatin can be increased when it is combined with Olanzapine.Approved, Investigational
OlaparibThe metabolism of Cerivastatin can be decreased when combined with Olaparib.Approved
OleandomycinThe risk or severity of adverse effects can be increased when Oleandomycin is combined with Cerivastatin.Vet Approved
OmeprazoleThe serum concentration of Cerivastatin can be increased when it is combined with Omeprazole.Approved, Investigational, Vet Approved
OmoconazoleThe risk or severity of adverse effects can be increased when Omoconazole is combined with Cerivastatin.Experimental
OsimertinibThe serum concentration of Cerivastatin can be increased when it is combined with Osimertinib.Approved
OtiloniumThe risk or severity of adverse effects can be increased when Otilonium is combined with Cerivastatin.Experimental, Investigational
OxiconazoleThe risk or severity of adverse effects can be increased when Oxiconazole is combined with Cerivastatin.Approved
OxybutyninThe serum concentration of Cerivastatin can be increased when it is combined with Oxybutynin.Approved, Investigational
OxymetholoneThe serum concentration of Cerivastatin can be increased when it is combined with Oxymetholone.Approved, Illicit
PaclitaxelThe serum concentration of Cerivastatin can be increased when it is combined with Paclitaxel.Approved, Vet Approved
PalbociclibThe serum concentration of Cerivastatin can be increased when it is combined with Palbociclib.Approved
ParamethasoneThe serum concentration of Cerivastatin can be increased when it is combined with Paramethasone.Approved
PazopanibCerivastatin may increase the hepatotoxic activities of Pazopanib.Approved
PentobarbitalThe metabolism of Cerivastatin can be increased when combined with Pentobarbital.Approved, Vet Approved
PergolideThe serum concentration of Cerivastatin can be increased when it is combined with Pergolide.Approved, Investigational, Vet Approved, Withdrawn
PerhexilineThe risk or severity of adverse effects can be increased when Perhexiline is combined with Cerivastatin.Approved, Investigational
PhenelzineThe serum concentration of Cerivastatin can be increased when it is combined with Phenelzine.Approved
PhenindioneCerivastatin may increase the anticoagulant activities of Phenindione.Approved, Investigational
PhenobarbitalThe metabolism of Cerivastatin can be increased when combined with Phenobarbital.Approved
PhenprocoumonCerivastatin may increase the anticoagulant activities of Phenprocoumon.Approved, Investigational
PhenytoinThe serum concentration of Cerivastatin can be decreased when it is combined with Phenytoin.Approved, Vet Approved
PilocarpineThe serum concentration of Cerivastatin can be increased when it is combined with Pilocarpine.Approved
PimozideThe serum concentration of Cerivastatin can be increased when it is combined with Pimozide.Approved
PinaveriumThe risk or severity of adverse effects can be increased when Pinaverium is combined with Cerivastatin.Approved
PioglitazoneThe metabolism of Cerivastatin can be decreased when combined with Pioglitazone.Approved, Investigational
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Cerivastatin.Approved
PosaconazoleThe metabolism of Cerivastatin can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Cerivastatin.Approved
PrednisoloneThe serum concentration of Cerivastatin can be increased when it is combined with Prednisolone.Approved, Vet Approved
PrednisoneThe serum concentration of Cerivastatin can be increased when it is combined with Prednisone.Approved, Vet Approved
PregabalinThe risk or severity of adverse effects can be increased when Pregabalin is combined with Cerivastatin.Approved, Illicit, Investigational
PrenylamineThe risk or severity of adverse effects can be increased when Prenylamine is combined with Cerivastatin.Withdrawn
PrimaquineThe serum concentration of Cerivastatin can be increased when it is combined with Primaquine.Approved
PrimidoneThe metabolism of Cerivastatin can be increased when combined with Primidone.Approved, Vet Approved
ProgesteroneThe serum concentration of Cerivastatin can be increased when it is combined with Progesterone.Approved, Vet Approved
PropofolThe serum concentration of Cerivastatin can be increased when it is combined with Propofol.Approved, Investigational, Vet Approved
QuinidineThe serum concentration of Cerivastatin can be increased when it is combined with Quinidine.Approved
QuinineThe serum concentration of Cerivastatin can be increased when it is combined with Quinine.Approved
QuinupristinThe serum concentration of Cerivastatin can be increased when it is combined with Quinupristin.Approved
RabeprazoleThe metabolism of Cerivastatin can be decreased when combined with Rabeprazole.Approved, Investigational
RaloxifeneThe serum concentration of Cerivastatin can be increased when it is combined with Raloxifene.Approved, Investigational
RaltegravirRaltegravir may increase the myopathic rhabdomyolysis activities of Cerivastatin.Approved
RanitidineThe serum concentration of Cerivastatin can be increased when it is combined with Ranitidine.Approved
RanolazineThe serum concentration of Cerivastatin can be increased when it is combined with Ranolazine.Approved, Investigational
RavuconazoleThe risk or severity of adverse effects can be increased when Ravuconazole is combined with Cerivastatin.Investigational
RegorafenibThe serum concentration of Cerivastatin can be increased when it is combined with Regorafenib.Approved
RepaglinideThe serum concentration of Cerivastatin can be increased when it is combined with Repaglinide.Approved, Investigational
ResveratrolThe serum concentration of Cerivastatin can be increased when it is combined with Resveratrol.Approved, Experimental, Investigational
RifabutinThe metabolism of Cerivastatin can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Cerivastatin can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Cerivastatin can be increased when combined with Rifapentine.Approved
RifaximinThe serum concentration of Cerivastatin can be decreased when it is combined with Rifaximin.Approved, Investigational
RilpivirineThe serum concentration of Cerivastatin can be increased when it is combined with Rilpivirine.Approved
RisedronateThe risk or severity of adverse effects can be increased when Risedronate is combined with Cerivastatin.Approved, Investigational
RisperidoneThe serum concentration of Cerivastatin can be increased when it is combined with Risperidone.Approved, Investigational
RivastigmineThe serum concentration of Cerivastatin can be increased when it is combined with Rivastigmine.Approved, Investigational
RolapitantThe serum concentration of Cerivastatin can be increased when it is combined with Rolapitant.Approved
RolitetracyclineThe serum concentration of Cerivastatin can be increased when it is combined with Rolitetracycline.Approved
RosiglitazoneThe metabolism of Cerivastatin can be decreased when combined with Rosiglitazone.Approved, Investigational
RosuvastatinThe serum concentration of Rosuvastatin can be increased when it is combined with Cerivastatin.Approved
RoxithromycinThe serum concentration of Cerivastatin can be increased when it is combined with Roxithromycin.Approved, Investigational, Withdrawn
RutinThe serum concentration of Cerivastatin can be increased when it is combined with Rutin.Experimental, Investigational
SalbutamolThe serum concentration of Cerivastatin can be increased when it is combined with Salbutamol.Approved, Vet Approved
SaquinavirThe metabolism of Cerivastatin can be decreased when combined with Saquinavir.Approved, Investigational
SarilumabThe serum concentration of Cerivastatin can be increased when it is combined with Sarilumab.Approved
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Cerivastatin.Approved
SecobarbitalThe metabolism of Cerivastatin can be increased when combined with Secobarbital.Approved, Vet Approved
SertaconazoleThe risk or severity of adverse effects can be increased when Sertaconazole is combined with Cerivastatin.Approved
SertralineThe serum concentration of Cerivastatin can be increased when it is combined with Sertraline.Approved
SildenafilThe metabolism of Cerivastatin can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Cerivastatin can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Cerivastatin can be increased when it is combined with Simeprevir.Approved
SimvastatinThe serum concentration of Cerivastatin can be increased when it is combined with Simvastatin.Approved
SirolimusThe serum concentration of Cerivastatin can be increased when it is combined with Sirolimus.Approved, Investigational
SitaxentanThe serum concentration of Cerivastatin can be increased when it is combined with Sitaxentan.Approved, Investigational, Withdrawn
Sodium bicarbonateThe serum concentration of Cerivastatin can be decreased when it is combined with Sodium bicarbonate.Approved
SolithromycinThe risk or severity of adverse effects can be increased when Solithromycin is combined with Cerivastatin.Investigational
SorafenibThe serum concentration of Cerivastatin can be increased when it is combined with Sorafenib.Approved, Investigational
SpiramycinThe risk or severity of adverse effects can be increased when Spiramycin is combined with Cerivastatin.Approved
St. John's WortThe metabolism of Cerivastatin can be increased when combined with St. John's Wort.Investigational, Nutraceutical
StiripentolThe serum concentration of Cerivastatin can be increased when it is combined with Stiripentol.Approved
SulconazoleThe risk or severity of adverse effects can be increased when Sulconazole is combined with Cerivastatin.Approved
SulfamethoxazoleThe metabolism of Cerivastatin can be decreased when combined with Sulfamethoxazole.Approved
SulfanilamideThe serum concentration of Cerivastatin can be increased when it is combined with Sulfanilamide.Approved
SulfinpyrazoneThe serum concentration of Cerivastatin can be increased when it is combined with Sulfinpyrazone.Approved
SulfisoxazoleThe metabolism of Cerivastatin can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
TacrolimusThe serum concentration of Cerivastatin can be increased when it is combined with Tacrolimus.Approved, Investigational
TadalafilThe serum concentration of Cerivastatin can be increased when it is combined with Tadalafil.Approved, Investigational
TamoxifenThe metabolism of Cerivastatin can be decreased when combined with Tamoxifen.Approved
TelaprevirThe metabolism of Cerivastatin can be decreased when combined with Telaprevir.Approved, Withdrawn
TelithromycinThe metabolism of Cerivastatin can be decreased when combined with Telithromycin.Approved
TemsirolimusThe serum concentration of Cerivastatin can be increased when it is combined with Temsirolimus.Approved
TeniposideThe serum concentration of Cerivastatin can be increased when it is combined with Teniposide.Approved
TerconazoleThe risk or severity of adverse effects can be increased when Terconazole is combined with Cerivastatin.Approved
TerfenadineThe serum concentration of Cerivastatin can be increased when it is combined with Terfenadine.Withdrawn
TergurideThe risk or severity of adverse effects can be increased when Terguride is combined with Cerivastatin.Experimental
TeriflunomideThe serum concentration of Cerivastatin can be increased when it is combined with Teriflunomide.Approved
TerodilineThe risk or severity of adverse effects can be increased when Terodiline is combined with Cerivastatin.Experimental
TesmilifeneThe serum concentration of Cerivastatin can be increased when it is combined with Tesmilifene.Investigational
TestosteroneThe serum concentration of Cerivastatin can be increased when it is combined with Testosterone.Approved, Investigational
TetracyclineThe serum concentration of Cerivastatin can be increased when it is combined with Tetracycline.Approved, Vet Approved
TetrahydropalmatineThe risk or severity of adverse effects can be increased when Tetrahydropalmatine is combined with Cerivastatin.Investigational
ThiopentalThe serum concentration of Cerivastatin can be increased when it is combined with Thiopental.Approved, Vet Approved
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Cerivastatin.Approved, Withdrawn
TicagrelorThe serum concentration of Cerivastatin can be increased when it is combined with Ticagrelor.Approved
TiclopidineThe metabolism of Cerivastatin can be decreased when combined with Ticlopidine.Approved
TioclomarolCerivastatin may increase the anticoagulant activities of Tioclomarol.Experimental
TioconazoleThe serum concentration of Cerivastatin can be increased when it is combined with Tioconazole.Approved
TipranavirThe serum concentration of Cerivastatin can be increased when it is combined with Tipranavir.Approved, Investigational
TocilizumabThe serum concentration of Cerivastatin can be decreased when it is combined with Tocilizumab.Approved
TofisopamThe serum concentration of Cerivastatin can be increased when it is combined with Tofisopam.Approved
Tolfenamic AcidThe risk or severity of adverse effects can be increased when Tolfenamic Acid is combined with Cerivastatin.Approved
TopiroxostatThe metabolism of Cerivastatin can be decreased when combined with Topiroxostat.Approved, Investigational
TopotecanThe serum concentration of Cerivastatin can be increased when it is combined with Topotecan.Approved, Investigational
TrabectedinCerivastatin may increase the myopathic rhabdomyolysis activities of Trabectedin.Approved, Investigational
TramadolThe serum concentration of Cerivastatin can be increased when it is combined with Tramadol.Approved, Investigational
TranilastThe risk or severity of adverse effects can be increased when Tranilast is combined with Cerivastatin.Approved, Investigational
TranylcypromineThe serum concentration of Cerivastatin can be increased when it is combined with Tranylcypromine.Approved
TrimethoprimThe metabolism of Cerivastatin can be decreased when combined with Trimethoprim.Approved, Vet Approved
TroglitazoneThe serum concentration of Cerivastatin can be increased when it is combined with Troglitazone.Investigational, Withdrawn
TroleandomycinThe serum concentration of Cerivastatin can be increased when it is combined with Troleandomycin.Approved
TromethamineThe serum concentration of Cerivastatin can be decreased when it is combined with Tromethamine.Approved
TylosinThe risk or severity of adverse effects can be increased when Tylosin is combined with Cerivastatin.Vet Approved
UbidecarenoneThe serum concentration of Ubidecarenone can be increased when it is combined with Cerivastatin.Approved, Experimental
Valproic AcidThe serum concentration of Cerivastatin can be increased when it is combined with Valproic Acid.Approved, Investigational
VenlafaxineThe metabolism of Cerivastatin can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Cerivastatin can be decreased when combined with Verapamil.Approved
VinblastineThe serum concentration of Cerivastatin can be increased when it is combined with Vinblastine.Approved
VincristineThe serum concentration of Cerivastatin can be increased when it is combined with Vincristine.Approved, Investigational
VinorelbineThe serum concentration of Cerivastatin can be increased when it is combined with Vinorelbine.Approved, Investigational
VinpocetineThe risk or severity of adverse effects can be increased when Vinpocetine is combined with Cerivastatin.Investigational
VoriconazoleThe metabolism of Cerivastatin can be decreased when combined with Voriconazole.Approved, Investigational
WarfarinCerivastatin may increase the anticoagulant activities of Warfarin.Approved
XylometazolineThe risk or severity of adverse effects can be increased when Xylometazoline is combined with Cerivastatin.Approved
ZafirlukastThe serum concentration of Cerivastatin can be increased when it is combined with Zafirlukast.Approved, Investigational
ZiconotideThe risk or severity of adverse effects can be increased when Ziconotide is combined with Cerivastatin.Approved
ZiprasidoneThe metabolism of Cerivastatin can be decreased when combined with Ziprasidone.Approved
ZucapsaicinThe serum concentration of Cerivastatin can be increased when it is combined with Zucapsaicin.Approved
Food Interactions
  • Grapefruit and grapefruit juice should be avoided throughout treatment as grapefruit can significantly increase serum levels of this product.
  • Take without regard to meals.

References

General References
  1. Furberg CD, Pitt B: Withdrawal of cerivastatin from the world market. Curr Control Trials Cardiovasc Med. 2001;2(5):205-207. [PubMed:11806796]
External Links
KEGG Compound
C07966
PubChem Compound
446156
PubChem Substance
46505877
ChemSpider
393588
BindingDB
18376
ChEBI
3558
ChEMBL
CHEMBL1477
Therapeutic Targets Database
DNC000403
PharmGKB
PA448897
HET
116
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Cerivastatin
ATC Codes
C10AA06 — Cerivastatin
FDA label
Download (144 KB)

Clinical Trials

Clinical Trials
Not Available

Pharmacoeconomics

Manufacturers
  • Bayer pharmaceuticals corp
Packagers
Dosage forms
FormRouteStrength
TabletOral0.4 mg
TabletOral0.8 mg
TabletOral0.2 mg
TabletOral0.3 mg
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5177080No1994-11-262011-11-26Us
CA1340798No1999-10-262016-10-26Canada
CA2057444No1998-05-262011-12-11Canada

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubilityHighly solubilityNot Available
logP3.4Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00419 mg/mLALOGPS
logP4.15ALOGPS
logP2.67ChemAxon
logS-5ALOGPS
pKa (Strongest Acidic)4.05ChemAxon
pKa (Strongest Basic)5.58ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area99.88 Å2ChemAxon
Rotatable Bond Count11ChemAxon
Refractivity126.82 m3·mol-1ChemAxon
Polarizability50.23 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9628
Blood Brain Barrier+0.9381
Caco-2 permeable+0.5141
P-glycoprotein substrateSubstrate0.6231
P-glycoprotein inhibitor INon-inhibitor0.5221
P-glycoprotein inhibitor IINon-inhibitor0.719
Renal organic cation transporterNon-inhibitor0.8848
CYP450 2C9 substrateNon-substrate0.7898
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.672
CYP450 1A2 substrateNon-inhibitor0.67
CYP450 2C9 inhibitorNon-inhibitor0.64
CYP450 2D6 inhibitorNon-inhibitor0.8717
CYP450 2C19 inhibitorNon-inhibitor0.596
CYP450 3A4 inhibitorNon-inhibitor0.6191
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.5668
Ames testNon AMES toxic0.817
CarcinogenicityNon-carcinogens0.8706
BiodegradationNot ready biodegradable0.9881
Rat acute toxicity2.6748 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9901
hERG inhibition (predictor II)Non-inhibitor0.8623
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
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.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Pyridines and derivatives
Sub Class
Phenylpyridines
Direct Parent
Phenylpyridines
Alternative Parents
Medium-chain hydroxy acids and derivatives / Medium-chain fatty acids / Beta hydroxy acids and derivatives / Hydroxy fatty acids / Heterocyclic fatty acids / Halogenated fatty acids / Fluorobenzenes / Unsaturated fatty acids / Aryl fluorides / Heteroaromatic compounds
show 11 more
Substituents
4-phenylpyridine / Medium-chain hydroxy acid / Medium-chain fatty acid / Hydroxy fatty acid / Heterocyclic fatty acid / Beta-hydroxy acid / Fluorobenzene / Halogenated fatty acid / Halobenzene / Aryl fluoride
show 27 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
statin (synthetic), pyridines, dihydroxy monocarboxylic acid (CHEBI:3558)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Nadph binding
Specific Function
Transmembrane glycoprotein that is the rate-limiting enzyme in cholesterol biosynthesis as well as in the biosynthesis of nonsterol isoprenoids that are essential for normal cell function including...
Gene Name
HMGCR
Uniprot ID
P04035
Uniprot Name
3-hydroxy-3-methylglutaryl-coenzyme A reductase
Molecular Weight
97475.155 Da
References
  1. Shiomi M, Ito T: Effect of cerivastatin sodium, a new inhibitor of HMG-CoA reductase, on plasma lipid levels, progression of atherosclerosis, and the lesional composition in the plaques of WHHL rabbits. Br J Pharmacol. 1999 Feb;126(4):961-8. [PubMed:10193776]
  2. Blumenthal RS: Statins: effective antiatherosclerotic therapy. Am Heart J. 2000 Apr;139(4):577-83. [PubMed:10740137]
  3. Ganne F, Vasse M, Beaudeux JL, Peynet J, Francois A, Mishal Z, Chartier A, Tobelem G, Vannier JP, Soria J, Soria C: Cerivastatin, an inhibitor of HMG-CoA reductase, inhibits urokinase/urokinase-receptor expression and MMP-9 secretion by peripheral blood monocytes--a possible protective mechanism against atherothrombosis. Thromb Haemost. 2000 Oct;84(4):680-8. [PubMed:11057870]
  4. Wong WW, Tan MM, Xia Z, Dimitroulakos J, Minden MD, Penn LZ: Cerivastatin triggers tumor-specific apoptosis with higher efficacy than lovastatin. Clin Cancer Res. 2001 Jul;7(7):2067-75. [PubMed:11448925]
  5. Denoyelle C, Vasse M, Korner M, Mishal Z, Ganne F, Vannier JP, Soria J, Soria C: Cerivastatin, an inhibitor of HMG-CoA reductase, inhibits the signaling pathways involved in the invasiveness and metastatic properties of highly invasive breast cancer cell lines: an in vitro study. Carcinogenesis. 2001 Aug;22(8):1139-48. [PubMed:11470741]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
Inducer
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Neuvonen PJ, Niemi M, Backman JT: Drug interactions with lipid-lowering drugs: mechanisms and clinical relevance. Clin Pharmacol Ther. 2006 Dec;80(6):565-81. [PubMed:17178259]
  2. Cohen LH, van Leeuwen RE, van Thiel GC, van Pelt JF, Yap SH: Equally potent inhibitors of cholesterol synthesis in human hepatocytes have distinguishable effects on different cytochrome P450 enzymes. Biopharm Drug Dispos. 2000 Dec;21(9):353-64. [PubMed:11523064]
  3. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014]
  4. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  5. Boberg M, Angerbauer R, Fey P, Kanhai WK, Karl W, Kern A, Ploschke J, Radtke M: Metabolism of cerivastatin by human liver microsomes in vitro. Characterization of primary metabolic pathways and of cytochrome P450 isozymes involved. Drug Metab Dispos. 1997 Mar;25(3):321-31. [PubMed:9172950]
  6. Wang JS, Neuvonen M, Wen X, Backman JT, Neuvonen PJ: Gemfibrozil inhibits CYP2C8-mediated cerivastatin metabolism in human liver microsomes. Drug Metab Dispos. 2002 Dec;30(12):1352-6. [PubMed:12433802]
  7. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A7
Uniprot ID
P24462
Uniprot Name
Cytochrome P450 3A7
Molecular Weight
57525.03 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 Da
References
  1. Neuvonen PJ, Niemi M, Backman JT: Drug interactions with lipid-lowering drugs: mechanisms and clinical relevance. Clin Pharmacol Ther. 2006 Dec;80(6):565-81. [PubMed:17178259]
  2. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014]
  3. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  4. Wang JS, Neuvonen M, Wen X, Backman JT, Neuvonen PJ: Gemfibrozil inhibits CYP2C8-mediated cerivastatin metabolism in human liver microsomes. Drug Metab Dispos. 2002 Dec;30(12):1352-6. [PubMed:12433802]
  5. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Cohen LH, van Leeuwen RE, van Thiel GC, van Pelt JF, Yap SH: Equally potent inhibitors of cholesterol synthesis in human hepatocytes have distinguishable effects on different cytochrome P450 enzymes. Biopharm Drug Dispos. 2000 Dec;21(9):353-64. [PubMed:11523064]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 Da
References
  1. Cohen LH, van Leeuwen RE, van Thiel GC, van Pelt JF, Yap SH: Equally potent inhibitors of cholesterol synthesis in human hepatocytes have distinguishable effects on different cytochrome P450 enzymes. Biopharm Drug Dispos. 2000 Dec;21(9):353-64. [PubMed:11523064]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. Cohen LH, van Leeuwen RE, van Thiel GC, van Pelt JF, Yap SH: Equally potent inhibitors of cholesterol synthesis in human hepatocytes have distinguishable effects on different cytochrome P450 enzymes. Biopharm Drug Dispos. 2000 Dec;21(9):353-64. [PubMed:11523064]
  2. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
Molecular Weight
56277.81 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Matsushima S, Maeda K, Kondo C, Hirano M, Sasaki M, Suzuki H, Sugiyama Y: Identification of the hepatic efflux transporters of organic anions using double-transfected Madin-Darby canine kidney II cells expressing human organic anion-transporting polypeptide 1B1 (OATP1B1)/multidrug resistance-associated protein 2, OATP1B1/multidrug resistance 1, and OATP1B1/breast cancer resistance protein. J Pharmacol Exp Ther. 2005 Sep;314(3):1059-67. Epub 2005 May 18. [PubMed:15901800]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Organic anion transmembrane transporter activity
Specific Function
Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
Gene Name
ABCC2
Uniprot ID
Q92887
Uniprot Name
Canalicular multispecific organic anion transporter 1
Molecular Weight
174205.64 Da
References
  1. Matsushima S, Maeda K, Kondo C, Hirano M, Sasaki M, Suzuki H, Sugiyama Y: Identification of the hepatic efflux transporters of organic anions using double-transfected Madin-Darby canine kidney II cells expressing human organic anion-transporting polypeptide 1B1 (OATP1B1)/multidrug resistance-associated protein 2, OATP1B1/multidrug resistance 1, and OATP1B1/breast cancer resistance protein. J Pharmacol Exp Ther. 2005 Sep;314(3):1059-67. Epub 2005 May 18. [PubMed:15901800]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
Gene Name
ABCG2
Uniprot ID
Q9UNQ0
Uniprot Name
ATP-binding cassette sub-family G member 2
Molecular Weight
72313.47 Da
References
  1. Matsushima S, Maeda K, Kondo C, Hirano M, Sasaki M, Suzuki H, Sugiyama Y: Identification of the hepatic efflux transporters of organic anions using double-transfected Madin-Darby canine kidney II cells expressing human organic anion-transporting polypeptide 1B1 (OATP1B1)/multidrug resistance-associated protein 2, OATP1B1/multidrug resistance 1, and OATP1B1/breast cancer resistance protein. J Pharmacol Exp Ther. 2005 Sep;314(3):1059-67. Epub 2005 May 18. [PubMed:15901800]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
Gene Name
SLCO1B1
Uniprot ID
Q9Y6L6
Uniprot Name
Solute carrier organic anion transporter family member 1B1
Molecular Weight
76447.99 Da
References
  1. Matsushima S, Maeda K, Kondo C, Hirano M, Sasaki M, Suzuki H, Sugiyama Y: Identification of the hepatic efflux transporters of organic anions using double-transfected Madin-Darby canine kidney II cells expressing human organic anion-transporting polypeptide 1B1 (OATP1B1)/multidrug resistance-associated protein 2, OATP1B1/multidrug resistance 1, and OATP1B1/breast cancer resistance protein. J Pharmacol Exp Ther. 2005 Sep;314(3):1059-67. Epub 2005 May 18. [PubMed:15901800]
  2. Kameyama Y, Yamashita K, Kobayashi K, Hosokawa M, Chiba K: 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. Pharmacogenet Genomics. 2005 Jul;15(7):513-22. [PubMed:15970799]

Drug created on June 13, 2005 07:24 / Updated on November 07, 2017 01:37