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Identification
NameCerivastatin
Accession NumberDB00439  (APRD00102)
TypeSmall Molecule
GroupsWithdrawn
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 It has also been withdrawn from the Canadian market.
Structure
Thumb
SynonymsNot Available
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
BaycolTablet0.4 mgOralBayer Inc2000-01-062001-10-26Canada
BaycolTablet0.8 mgOralBayer Inc2000-12-282001-10-26Canada
Baycol (0.2mg)Tablet0.2 mgOralBayer Inc1998-03-112001-10-26Canada
Baycol (0.3mg)Tablet0.3 mgOralBayer Inc1998-03-112001-10-26Canada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
LipobayNot Available
RivastatinNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Cerivastatin sodium
143201-11-0
Thumb
  • InChI Key: GPUADMRJQVPIAS-QCVDVZFFSA-M
  • Monoisotopic Mass: 481.224046051
  • Average Mass: 481.5321
DBSALT000330
Categories
UNIIAM91H2KS67
CAS number145599-86-6
WeightAverage: 459.5503
Monoisotopic: 459.242101408
Chemical FormulaC26H34FNO5
InChI KeySEERZIQQUAZTOL-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\[C@@H](O)C[C@@H](O)CC(O)=O)=C(C(C)C)N=C1C(C)C
Pharmacology
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.
Structured Indications Not Available
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).
Mechanism of actionCerivastatin 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.
TargetKindPharmacological actionActionsOrganismUniProt ID
3-hydroxy-3-methylglutaryl-coenzyme A reductaseProteinyes
inhibitor
HumanP04035 details
Related Articles
AbsorptionThe mean absolute oral bioavailability 60% (range 39 - 101%).
Volume of distributionNot Available
Protein bindingMore 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.

SubstrateEnzymesProduct
Cerivastatin
HydroxycerivastatinDetails
Cerivastatin
DesmethylcerivastatinDetails
Route of eliminationNot Available
Half life2-3 hours
ClearanceNot Available
ToxicityRhabdomyolysis, liver concerns
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Cerivastatin Action PathwayDrug actionSMP00111
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
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
AcipimoxAcipimox may increase the myopathic rhabdomyolysis activities of Cerivastatin.Approved
AfatinibThe serum concentration of Cerivastatin can be increased when it is combined with Afatinib.Approved
AlbendazoleThe serum concentration of Cerivastatin can be increased when it is combined with Albendazole.Approved, Vet Approved
AldosteroneThe serum concentration of Cerivastatin can be decreased when it is combined with Aldosterone.Experimental
AlectinibThe serum concentration of Cerivastatin can be increased when it is combined with Alectinib.Approved
AlfentanilThe serum concentration of Cerivastatin can be increased when it is combined with Alfentanil.Approved, Illicit
Aluminum hydroxideThe serum concentration of Cerivastatin can be decreased when it is combined with Aluminum hydroxide.Approved
Aluminum phosphateThe serum concentration of Cerivastatin can be decreased when it is combined with Aluminum phosphate.Approved
AmantadineThe serum concentration of Cerivastatin can be increased when it is combined with Amantadine.Approved
Aminohippuric acidThe serum concentration of Cerivastatin can be increased when it is combined with Aminohippuric acid.Approved
AmiodaroneThe metabolism of Cerivastatin can be decreased when combined with Amiodarone.Approved, Investigational
AmitriptylineThe serum concentration of Cerivastatin can be increased when it is combined with Amitriptyline.Approved
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
AmprenavirThe serum concentration of Cerivastatin can be decreased when it is combined with Amprenavir.Approved
AmsacrineThe serum concentration of Cerivastatin can be increased when it is combined with Amsacrine.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
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
AtenololThe serum concentration of Cerivastatin can be increased when it is combined with Atenolol.Approved
AtomoxetineThe metabolism of Cerivastatin can be decreased when combined with Atomoxetine.Approved
AtorvastatinThe serum concentration of Cerivastatin can be increased when it is combined with Atorvastatin.Approved
AzelastineThe serum concentration of Cerivastatin can be increased when it is combined with Azelastine.Approved
AzithromycinThe serum concentration of Cerivastatin can be increased when it is combined with Azithromycin.Approved
BenzocaineThe serum concentration of Cerivastatin can be increased when it is combined with Benzocaine.Approved
BepridilThe serum concentration of Cerivastatin can be increased when it is combined with Bepridil.Approved, Withdrawn
BexaroteneThe serum concentration of Cerivastatin can be decreased when it is combined with Bexarotene.Approved, Investigational
BezafibrateBezafibrate may increase the myopathic rhabdomyolysis activities of Cerivastatin.Approved
BiperidenThe serum concentration of Cerivastatin can be increased when it is combined with Biperiden.Approved
Bismuth SubcitrateThe serum concentration of Cerivastatin can be decreased when it is combined with Bismuth Subcitrate.Approved
BoceprevirThe metabolism of Cerivastatin can be decreased when combined with Boceprevir.Approved
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
BosutinibThe serum concentration of Cerivastatin can be increased when it is combined with Bosutinib.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
BuspironeThe serum concentration of Cerivastatin can be increased when it is combined with Buspirone.Approved, Investigational
CabazitaxelThe serum concentration of Cerivastatin can be increased when it is combined with Cabazitaxel.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
CanagliflozinThe serum concentration of Cerivastatin can be increased when it is combined with Canagliflozin.Approved
CandesartanThe serum concentration of Cerivastatin can be increased when it is combined with Candesartan.Approved
CaptoprilThe serum concentration of Cerivastatin can be increased when it is combined with Captopril.Approved
CarbamazepineThe metabolism of Cerivastatin can be increased when combined with Carbamazepine.Approved, Investigational
CarvedilolThe serum concentration of Cerivastatin can be increased when it is combined with Carvedilol.Approved, Investigational
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
ChloroquineThe serum concentration of Cerivastatin can be increased when it is combined with Chloroquine.Approved, Vet Approved
ChlorpromazineThe serum concentration of Cerivastatin can be increased when it is combined with Chlorpromazine.Approved, Vet Approved
ChlorpropamideThe serum concentration of Cerivastatin can be increased when it is combined with Chlorpropamide.Approved
ChlorprothixeneThe serum concentration of Cerivastatin can be increased when it is combined with Chlorprothixene.Approved, Withdrawn
CholesterolThe serum concentration of Cerivastatin can be increased when it is combined with Cholesterol.Experimental
Cholic AcidThe serum concentration of Cerivastatin can be decreased when it is combined with Cholic Acid.Approved
CilazaprilThe serum concentration of Cerivastatin can be increased when it is combined with Cilazapril.Approved
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Cerivastatin.Approved
CimetidineThe serum concentration of Cerivastatin can be decreased when it is combined with Cimetidine.Approved
CiprofibrateThe risk or severity of adverse effects can be increased when Ciprofibrate is combined with Cerivastatin.Approved
CiprofloxacinThe serum concentration of Cerivastatin can be increased when it is combined with Ciprofloxacin.Approved, Investigational
CitalopramThe serum concentration of Cerivastatin can be increased when it is combined with Citalopram.Approved
ClarithromycinThe metabolism of Cerivastatin can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Cerivastatin can be decreased when combined with Clemastine.Approved
ClofazimineThe serum concentration of Cerivastatin can be increased when it is combined with Clofazimine.Approved, Investigational
ClomipramineThe serum concentration of Cerivastatin can be increased when it is combined with Clomipramine.Approved, Vet Approved
ClopidogrelThe metabolism of Cerivastatin can be decreased when combined with Clopidogrel.Approved, Nutraceutical
ClotrimazoleThe metabolism of Cerivastatin can be decreased when combined with Clotrimazole.Approved, Vet Approved
CobicistatThe metabolism of Cerivastatin can be decreased when combined with Cobicistat.Approved
ColchicineColchicine may increase the myopathic rhabdomyolysis activities of Cerivastatin.Approved
ColforsinThe serum concentration of Cerivastatin can be increased when it is combined with Colforsin.Experimental
ConivaptanThe serum concentration of Cerivastatin can be increased when it is combined with Conivaptan.Approved, Investigational
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
DactinomycinThe serum concentration of Cerivastatin can be increased when it is combined with Dactinomycin.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
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 decreased 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
DesloratadineThe serum concentration of Cerivastatin can be increased when it is combined with Desloratadine.Approved, Investigational
DexamethasoneThe serum concentration of Cerivastatin can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DextromethorphanThe serum concentration of Cerivastatin can be increased when it is combined with Dextromethorphan.Approved
DiclofenacThe serum concentration of Cerivastatin can be increased when it is combined with Diclofenac.Approved, Vet Approved
DicoumarolCerivastatin may increase the anticoagulant activities of Dicoumarol.Approved
DigoxinThe serum concentration of Cerivastatin can be decreased when it is combined with Digoxin.Approved
DihydroergotamineThe metabolism of Cerivastatin can be decreased when combined with Dihydroergotamine.Approved
DiltiazemThe metabolism of Cerivastatin can be decreased when combined with Diltiazem.Approved
DipyridamoleThe serum concentration of Cerivastatin can be increased when it is combined with Dipyridamole.Approved
DoxazosinThe serum concentration of Cerivastatin can be increased when it is combined with Doxazosin.Approved
DoxepinThe serum concentration of Cerivastatin can be increased when it is combined with Doxepin.Approved
DoxorubicinThe serum concentration of Cerivastatin can be decreased when it is combined with Doxorubicin.Approved, Investigational
DoxycyclineThe metabolism of Cerivastatin can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronabinolThe serum concentration of Cerivastatin can be increased when it is combined with Dronabinol.Approved, Illicit
DronedaroneThe metabolism of Cerivastatin can be decreased when combined with Dronedarone.Approved
EfavirenzThe serum concentration of Cerivastatin can be decreased when it is combined with Efavirenz.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
EnalaprilThe serum concentration of Cerivastatin can be increased when it is combined with Enalapril.Approved, Vet Approved
EnzalutamideThe serum concentration of Cerivastatin can be decreased when it is combined with Enzalutamide.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
Eslicarbazepine acetateThe serum concentration of Cerivastatin can be decreased when it is combined with Eslicarbazepine acetate.Approved
EstramustineThe serum concentration of Cerivastatin can be increased when it is combined with Estramustine.Approved
EstriolThe serum concentration of Cerivastatin can be decreased when it is combined with Estriol.Approved, Vet Approved
EstroneThe serum concentration of Cerivastatin can be decreased when it is combined with Estrone.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
EtravirineThe serum concentration of Cerivastatin can be decreased when it is combined with Etravirine.Approved
FelodipineThe serum concentration of Cerivastatin can be increased when it is combined with Felodipine.Approved, Investigational
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
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Cerivastatin.Approved
FexofenadineThe serum concentration of Cerivastatin can be increased when it is combined with Fexofenadine.Approved
FidaxomicinThe serum concentration of Cerivastatin can be increased when it is combined with Fidaxomicin.Approved
FluconazoleThe metabolism of Cerivastatin can be decreased when combined with Fluconazole.Approved
FluindioneCerivastatin may increase the anticoagulant activities of Fluindione.Investigational
FluoxetineThe serum concentration of Cerivastatin can be increased when it is combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe serum concentration of Cerivastatin can be increased when it is combined with Flupentixol.Approved, Withdrawn
FluphenazineThe serum concentration of Cerivastatin can be increased when it is combined with Fluphenazine.Approved
FlurazepamThe serum concentration of Cerivastatin can be increased when it is combined with Flurazepam.Approved, Illicit
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
GefitinibThe serum concentration of Cerivastatin can be increased when it is combined with Gefitinib.Approved, Investigational
GemfibrozilThe metabolism of Cerivastatin can be decreased when combined with Gemfibrozil.Approved
GenisteinThe serum concentration of Cerivastatin can be increased when it is combined with Genistein.Investigational
GlyburideThe serum concentration of Cerivastatin can be increased when it is combined with Glyburide.Approved
GlycerolThe serum concentration of Cerivastatin can be increased when it is combined with Glycerol.Experimental
Gramicidin DThe serum concentration of Cerivastatin can be increased when it is combined with Gramicidin D.Approved
GrepafloxacinThe serum concentration of Cerivastatin can be increased when it is combined with Grepafloxacin.Withdrawn
HaloperidolThe serum concentration of Cerivastatin can be increased when it is combined with Haloperidol.Approved
HydrocortisoneThe serum concentration of Cerivastatin can be increased when it is combined with Hydrocortisone.Approved, Vet Approved
IdelalisibThe serum concentration of Cerivastatin can be increased when it is combined with Idelalisib.Approved
ImatinibThe metabolism of Cerivastatin can be decreased when combined with Imatinib.Approved
ImipramineThe serum concentration of Cerivastatin can be increased when it is combined with Imipramine.Approved
IndinavirThe metabolism of Cerivastatin can be decreased when combined with Indinavir.Approved
IndomethacinThe serum concentration of Cerivastatin can be increased when it is combined with Indomethacin.Approved, Investigational
IrbesartanThe metabolism of Cerivastatin can be decreased when combined with Irbesartan.Approved, Investigational
IsavuconazoniumThe metabolism of Cerivastatin can be decreased when combined with Isavuconazonium.Approved, Investigational
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
IvermectinThe serum concentration of Cerivastatin can be increased when it is combined with Ivermectin.Approved, Vet Approved
KetamineThe serum concentration of Cerivastatin can be increased when it is combined with Ketamine.Approved, Vet Approved
KetoconazoleThe metabolism of Cerivastatin can be decreased when combined with Ketoconazole.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 serum concentration of Cerivastatin can be increased when it is combined with Lapatinib.Approved, Investigational
LevofloxacinThe serum concentration of Cerivastatin can be increased when it is combined with Levofloxacin.Approved, Investigational
LevothyroxineThe serum concentration of Cerivastatin can be decreased when it is combined with Levothyroxine.Approved
LidocaineThe serum concentration of Cerivastatin can be increased when it is combined with Lidocaine.Approved, Vet Approved
LiothyronineThe serum concentration of Cerivastatin can be decreased when it is combined with Liothyronine.Approved, Vet Approved
LiotrixThe serum concentration of Cerivastatin can be decreased when it is combined with Liotrix.Approved
LisinoprilThe serum concentration of Cerivastatin can be increased when it is combined with Lisinopril.Approved, Investigational
LomitapideThe serum concentration of Cerivastatin can be increased when it is combined with Lomitapide.Approved
LoperamideThe serum concentration of Cerivastatin can be increased when it is combined with Loperamide.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 serum concentration of Cerivastatin can be increased when it is 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
MagaldrateThe serum concentration of Cerivastatin can be decreased when it is combined with Magaldrate.Withdrawn
Magnesium carbonateThe serum concentration of Cerivastatin can be decreased when it is combined with Magnesium carbonate.Approved
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 TrisilicateThe serum concentration of Cerivastatin can be decreased when it is combined with Magnesium Trisilicate.Approved
MaprotilineThe serum concentration of Cerivastatin can be increased when it is combined with Maprotiline.Approved
MebendazoleThe serum concentration of Cerivastatin can be increased when it is combined with Mebendazole.Approved, Vet Approved
MefloquineThe serum concentration of Cerivastatin can be increased when it is combined with Mefloquine.Approved
Megestrol acetateThe serum concentration of Cerivastatin can be increased when it is combined with Megestrol acetate.Approved, Vet Approved
MeprobamateThe serum concentration of Cerivastatin can be increased when it is combined with Meprobamate.Approved, Illicit
MethadoneThe serum concentration of Cerivastatin can be increased when it is combined with Methadone.Approved
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Cerivastatin.Approved, Investigational
MibefradilThe serum concentration of Cerivastatin can be increased when it is combined with Mibefradil.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 decreased when it is combined with Midazolam.Approved, Illicit
MifepristoneThe serum concentration of Cerivastatin can be increased when it is combined with Mifepristone.Approved, Investigational
MitomycinThe serum concentration of Cerivastatin can be increased when it is combined with Mitomycin.Approved
MitotaneThe serum concentration of Cerivastatin can be decreased when it is combined with Mitotane.Approved
MitoxantroneThe serum concentration of Cerivastatin can be decreased when it is combined with Mitoxantrone.Approved, Investigational
ModafinilThe serum concentration of Cerivastatin can be decreased when it is combined with Modafinil.Approved, Investigational
MorphineThe serum concentration of Cerivastatin can be increased when it is combined with Morphine.Approved, Investigational
NafcillinThe serum concentration of Cerivastatin can be decreased when it is combined with Nafcillin.Approved
NaltrexoneThe serum concentration of Cerivastatin can be increased when it is combined with Naltrexone.Approved, Investigational, Vet Approved
NaringeninThe serum concentration of Cerivastatin can be increased when it is combined with Naringenin.Experimental
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
NeostigmineThe serum concentration of Cerivastatin can be increased when it is combined with Neostigmine.Approved, Vet 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
NicotinamideThe risk or severity of adverse effects can be increased when Nicotinamide is combined with Cerivastatin.Approved
NifedipineThe serum concentration of Cerivastatin can be decreased when it is combined with Nifedipine.Approved
NilotinibThe metabolism of Cerivastatin can be decreased when combined with Nilotinib.Approved, Investigational
NisoldipineThe serum concentration of Cerivastatin can be increased when it is combined with Nisoldipine.Approved
NitrazepamThe serum concentration of Cerivastatin can be increased when it is combined with Nitrazepam.Approved
NitrendipineThe serum concentration of Cerivastatin can be increased when it is combined with Nitrendipine.Approved
NorethisteroneThe serum concentration of Cerivastatin can be decreased when it is combined with Norethisterone.Approved
OlaparibThe metabolism of Cerivastatin can be decreased when combined with Olaparib.Approved
OmeprazoleThe serum concentration of Cerivastatin can be increased when it is combined with Omeprazole.Approved, Investigational, Vet Approved
OsimertinibThe serum concentration of Cerivastatin can be increased when it is combined with Osimertinib.Approved
P-NitrophenolThe serum concentration of Cerivastatin can be increased when it is combined with P-Nitrophenol.Experimental
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
Palmitic AcidThe serum concentration of Cerivastatin can be increased when it is combined with Palmitic Acid.Experimental
PantoprazoleThe serum concentration of Cerivastatin can be increased when it is combined with Pantoprazole.Approved
ParoxetineThe serum concentration of Cerivastatin can be increased when it is combined with Paroxetine.Approved, Investigational
PazopanibCerivastatin may increase the hepatotoxic activities of Pazopanib.Approved
PentobarbitalThe metabolism of Cerivastatin can be increased when combined with Pentobarbital.Approved, Vet Approved
PerindoprilThe serum concentration of Cerivastatin can be increased when it is combined with Perindopril.Approved
PhenindioneCerivastatin may increase the anticoagulant activities of Phenindione.Approved
PhenobarbitalThe metabolism of Cerivastatin can be increased when combined with Phenobarbital.Approved
PhenprocoumonCerivastatin may increase the anticoagulant activities of Phenprocoumon.Approved
PhenytoinThe serum concentration of Cerivastatin can be decreased when it is combined with Phenytoin.Approved, Vet Approved
PimozideThe serum concentration of Cerivastatin can be increased when it is combined with Pimozide.Approved
PioglitazoneThe metabolism of Cerivastatin can be decreased when combined with Pioglitazone.Approved, Investigational
Platelet Activating FactorThe serum concentration of Cerivastatin can be decreased when it is combined with Platelet Activating Factor.Experimental
PonatinibThe serum concentration of Cerivastatin can be increased when it is combined with Ponatinib.Approved
PosaconazoleThe metabolism of Cerivastatin can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PravastatinThe serum concentration of Cerivastatin can be increased when it is combined with Pravastatin.Approved
PrazosinThe serum concentration of Cerivastatin can be increased when it is combined with Prazosin.Approved
PrednisoneThe serum concentration of Cerivastatin can be increased when it is combined with Prednisone.Approved, Vet Approved
PrimidoneThe metabolism of Cerivastatin can be increased when combined with Primidone.Approved, Vet Approved
ProbenecidThe serum concentration of Cerivastatin can be increased when it is combined with Probenecid.Approved
ProgesteroneThe serum concentration of Cerivastatin can be decreased when it is combined with Progesterone.Approved, Vet Approved
PromethazineThe serum concentration of Cerivastatin can be increased when it is combined with Promethazine.Approved
PropafenoneThe serum concentration of Cerivastatin can be increased when it is combined with Propafenone.Approved
PropranololThe serum concentration of Cerivastatin can be increased when it is combined with Propranolol.Approved, Investigational
ProtriptylineThe serum concentration of Cerivastatin can be increased when it is combined with Protriptyline.Approved
QuercetinThe serum concentration of Cerivastatin can be increased when it is combined with Quercetin.Experimental
QuinacrineThe serum concentration of Cerivastatin can be increased when it is combined with Quinacrine.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
RabeprazoleThe metabolism of Cerivastatin can be decreased when combined with Rabeprazole.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
ReboxetineThe serum concentration of Cerivastatin can be increased when it is combined with Reboxetine.Approved, Investigational
RegorafenibThe serum concentration of Cerivastatin can be increased when it is combined with Regorafenib.Approved
ReserpineThe serum concentration of Cerivastatin can be decreased when it is combined with Reserpine.Approved
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
RilpivirineThe serum concentration of Cerivastatin can be increased when it is combined with Rilpivirine.Approved
RitonavirThe metabolism of Cerivastatin can be decreased when combined with Ritonavir.Approved, Investigational
RolapitantThe serum concentration of Cerivastatin can be increased when it is combined with Rolapitant.Approved
RosiglitazoneThe metabolism of Cerivastatin can be decreased when combined with Rosiglitazone.Approved, Investigational
SaquinavirThe metabolism of Cerivastatin can be decreased when combined with Saquinavir.Approved, Investigational
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Cerivastatin.Approved
ScopolamineThe serum concentration of Cerivastatin can be increased when it is combined with Scopolamine.Approved
SecobarbitalThe metabolism of Cerivastatin can be increased when combined with Secobarbital.Approved, Vet Approved
SelegilineThe serum concentration of Cerivastatin can be increased when it is combined with Selegiline.Approved, Investigational, Vet 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 decreased when it is combined with Sirolimus.Approved, Investigational
SorafenibThe serum concentration of Cerivastatin can be increased when it is combined with Sorafenib.Approved, Investigational
SpironolactoneThe serum concentration of Cerivastatin can be increased when it is combined with Spironolactone.Approved
St. John's WortThe metabolism of Cerivastatin can be increased when combined with St. John's Wort.Nutraceutical
StaurosporineThe serum concentration of Cerivastatin can be increased when it is combined with Staurosporine.Experimental
StiripentolThe serum concentration of Cerivastatin can be increased when it is combined with Stiripentol.Approved
StreptozocinThe serum concentration of Cerivastatin can be decreased when it is combined with Streptozocin.Approved
SulfamethoxazoleThe metabolism of Cerivastatin can be decreased when combined with Sulfamethoxazole.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
SumatriptanThe serum concentration of Cerivastatin can be increased when it is combined with Sumatriptan.Approved, Investigational
SunitinibThe serum concentration of Cerivastatin can be increased when it is combined with Sunitinib.Approved, Investigational
TacrineThe serum concentration of Cerivastatin can be increased when it is combined with Tacrine.Withdrawn
TacrolimusThe serum concentration of Cerivastatin can be decreased when it is combined with Tacrolimus.Approved, Investigational
TamoxifenThe serum concentration of Cerivastatin can be decreased when it is combined with Tamoxifen.Approved
Taurocholic AcidThe serum concentration of Cerivastatin can be increased when it is combined with Taurocholic Acid.Experimental
TelaprevirThe metabolism of Cerivastatin can be decreased when combined with Telaprevir.Approved
TelithromycinThe metabolism of Cerivastatin can be decreased when combined with Telithromycin.Approved
TelmisartanThe serum concentration of Cerivastatin can be increased when it is combined with Telmisartan.Approved, Investigational
TemsirolimusThe serum concentration of Cerivastatin can be increased when it is combined with Temsirolimus.Approved
TerazosinThe serum concentration of Cerivastatin can be increased when it is combined with Terazosin.Approved
TerfenadineThe serum concentration of Cerivastatin can be increased when it is combined with Terfenadine.Withdrawn
TeriflunomideThe serum concentration of Cerivastatin can be increased when it is combined with Teriflunomide.Approved
TesmilifeneThe serum concentration of Cerivastatin can be decreased when it is combined with Tesmilifene.Investigational
TestosteroneThe serum concentration of Cerivastatin can be increased when it is combined with Testosterone.Approved, Investigational
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Cerivastatin.Approved
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
TocilizumabThe serum concentration of Cerivastatin can be decreased when it is combined with Tocilizumab.Approved
TolvaptanThe serum concentration of Cerivastatin can be increased when it is combined with Tolvaptan.Approved
TrabectedinCerivastatin may increase the myopathic rhabdomyolysis activities of Trabectedin.Approved, Investigational
TrazodoneThe serum concentration of Cerivastatin can be decreased when it is combined with Trazodone.Approved, Investigational
TrifluoperazineThe serum concentration of Cerivastatin can be increased when it is combined with Trifluoperazine.Approved
TriflupromazineThe serum concentration of Cerivastatin can be increased when it is combined with Triflupromazine.Approved, Vet Approved
TrimethoprimThe serum concentration of Cerivastatin can be decreased when it is combined with Trimethoprim.Approved, Vet Approved
TrimipramineThe serum concentration of Cerivastatin can be increased when it is combined with Trimipramine.Approved
TroleandomycinThe serum concentration of Cerivastatin can be increased when it is combined with Troleandomycin.Approved
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 decreased when it is combined with Vinblastine.Approved
VincristineThe serum concentration of Cerivastatin can be decreased when it is combined with Vincristine.Approved, Investigational
VinorelbineThe serum concentration of Cerivastatin can be increased when it is combined with Vinorelbine.Approved, Investigational
VoriconazoleThe metabolism of Cerivastatin can be decreased when combined with Voriconazole.Approved, Investigational
WarfarinCerivastatin may increase the anticoagulant activities of Warfarin.Approved
ZimelidineThe serum concentration of Cerivastatin can be increased when it is combined with Zimelidine.Withdrawn
ZiprasidoneThe metabolism of Cerivastatin can be decreased when combined with Ziprasidone.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
Synthesis ReferenceNot Available
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
ATC CodesC10AA06
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (144 KB)
MSDSNot Available
ADMET
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 )
Pharmacoeconomics
Manufacturers
  • Bayer pharmaceuticals corp
Packagers
Dosage forms
FormRouteStrength
TabletOral0.4 mg
TabletOral0.8 mg
TabletOral0.2 mg
TabletOral0.3 mg
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA1340798 No1999-10-262016-10-26Canada
CA2057444 No1998-05-262011-12-11Canada
US5177080 No1994-11-262011-11-26Us
Properties
StateSolid
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 RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
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
Alternative Parents
Substituents
  • 4-phenylpyridine
  • Medium-chain hydroxy acid
  • Medium-chain fatty acid
  • Heterocyclic fatty acid
  • Halogenated fatty acid
  • Halobenzene
  • Fluorobenzene
  • Beta-hydroxy acid
  • Fatty acyl
  • Fatty acid
  • Benzenoid
  • Unsaturated fatty acid
  • Hydroxy acid
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl fluoride
  • Heteroaromatic compound
  • Secondary alcohol
  • Azacycle
  • Monocarboxylic acid or derivatives
  • Ether
  • Dialkyl ether
  • Carboxylic acid
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organofluoride
  • Organohalogen compound
  • Carbonyl group
  • Alcohol
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External Descriptors

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 ubiquinone and geranylgeranyl proteins.
Gene Name:
HMGCR
Uniprot ID:
P04035
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
substrateinhibitorinducer
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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
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 unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
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 unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A7
Uniprot ID:
P24462
Molecular Weight:
57525.03 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
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 antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
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 imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
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
inhibitorinducer
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. Acts as a 1,4-cineole 2-exo-monooxygenase.
Gene Name:
CYP2B6
Uniprot ID:
P20813
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
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
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 from mitochondria to cytosol and from cytosol to extracellular space, and cellular export of hemin, and heme. Xenobiotic transporter that may play an important role in the exclusion of xenobiotics from t...
Gene Name:
ABCG2
Uniprot ID:
Q9UNQ0
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, prostaglandin E2, thromboxane B2, leukotriene C3, leukotriene E4, thyroxine and triiodothyronine. Involved in the clearance of bile acids and organic anions from the liver.
Gene Name:
SLCO1B1
Uniprot ID:
Q9Y6L6
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 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23