You are using an unsupported browser. Please upgrade your browser to a newer version to get the best experience on DrugBank.
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 It has also been withdrawn from the Canadian market.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 KeyInChIKey=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\[C@@H](O)C[C@@H](O)CC(O)=O)=C(C(C)C)N=C1C(C)C
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
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.
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.
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
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
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
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Cerivastatin can be increased when it is combined with Abiraterone.
AcenocoumarolCerivastatin may increase the anticoagulant activities of Acenocoumarol.
AcetaminophenThe serum concentration of Cerivastatin can be increased when it is combined with Acetaminophen.
AcipimoxAcipimox may increase the myopathic rhabdomyolysis activities of Cerivastatin.
AfatinibThe serum concentration of Cerivastatin can be increased when it is combined with Afatinib.
AlbendazoleThe serum concentration of Cerivastatin can be increased when it is combined with Albendazole.
AldosteroneThe serum concentration of Cerivastatin can be decreased when it is combined with Aldosterone.
AlectinibThe serum concentration of Cerivastatin can be increased when it is combined with Alectinib.
AlfentanilThe serum concentration of Cerivastatin can be increased when it is combined with Alfentanil.
Aluminum hydroxideThe serum concentration of Cerivastatin can be decreased when it is combined with Aluminum hydroxide.
Aluminum phosphateThe serum concentration of Cerivastatin can be decreased when it is combined with Aluminum phosphate.
AmantadineThe serum concentration of Cerivastatin can be increased when it is combined with Amantadine.
Aminohippuric acidThe serum concentration of Cerivastatin can be increased when it is combined with Aminohippuric acid.
AmiodaroneThe serum concentration of Cerivastatin can be decreased when it is combined with Amiodarone.
AmitriptylineThe serum concentration of Cerivastatin can be increased when it is combined with Amitriptyline.
AmlodipineThe serum concentration of Cerivastatin can be increased when it is combined with Amlodipine.
AmodiaquineThe serum concentration of Amodiaquine can be increased when it is combined with Cerivastatin.
AmprenavirThe serum concentration of Cerivastatin can be decreased when it is combined with Amprenavir.
AmsacrineThe serum concentration of Cerivastatin can be increased when it is combined with Amsacrine.
AprepitantThe serum concentration of Cerivastatin can be increased when it is combined with Aprepitant.
AripiprazoleThe serum concentration of Aripiprazole can be decreased when it is combined with Cerivastatin.
AstemizoleThe serum concentration of Cerivastatin can be increased when it is combined with Astemizole.
AtazanavirThe serum concentration of Cerivastatin can be increased when it is combined with Atazanavir.
AtenololThe serum concentration of Cerivastatin can be increased when it is combined with Atenolol.
AtomoxetineThe metabolism of Cerivastatin can be decreased when combined with Atomoxetine.
AtorvastatinThe serum concentration of Cerivastatin can be increased when it is combined with Atorvastatin.
AzelastineThe serum concentration of Cerivastatin can be increased when it is combined with Azelastine.
AzithromycinThe serum concentration of Cerivastatin can be increased when it is combined with Azithromycin.
BenzocaineThe serum concentration of Cerivastatin can be increased when it is combined with Benzocaine.
BepridilThe serum concentration of Cerivastatin can be increased when it is combined with Bepridil.
BexaroteneThe serum concentration of Cerivastatin can be decreased when it is combined with Bexarotene.
BezafibrateBezafibrate may increase the myopathic rhabdomyolysis activities of Cerivastatin.
BiperidenThe serum concentration of Cerivastatin can be increased when it is combined with Biperiden.
Bismuth SubcitrateThe serum concentration of Cerivastatin can be decreased when it is combined with Bismuth Subcitrate.
BoceprevirThe metabolism of Cerivastatin can be decreased when combined with Boceprevir.
BortezomibThe metabolism of Cerivastatin can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Cerivastatin can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Cerivastatin can be increased when it is combined with Bosutinib.
BromocriptineThe serum concentration of Cerivastatin can be increased when it is combined with Bromocriptine.
BuprenorphineThe serum concentration of Cerivastatin can be increased when it is combined with Buprenorphine.
BuspironeThe serum concentration of Cerivastatin can be increased when it is combined with Buspirone.
CabazitaxelThe serum concentration of Cerivastatin can be increased when it is combined with Cabazitaxel.
CaffeineThe serum concentration of Cerivastatin can be increased when it is combined with Caffeine.
Calcium carbonateThe serum concentration of Cerivastatin can be decreased when it is combined with Calcium carbonate.
CanagliflozinThe serum concentration of Cerivastatin can be increased when it is combined with Canagliflozin.
CandesartanThe serum concentration of Cerivastatin can be increased when it is combined with Candesartan.
CaptoprilThe serum concentration of Cerivastatin can be increased when it is combined with Captopril.
CarbamazepineThe serum concentration of Cerivastatin can be decreased when it is combined with Carbamazepine.
CarvedilolThe serum concentration of Cerivastatin can be increased when it is combined with Carvedilol.
CaspofunginThe serum concentration of Cerivastatin can be increased when it is combined with Caspofungin.
CelecoxibThe metabolism of Cerivastatin can be decreased when combined with Celecoxib.
CeritinibThe serum concentration of Cerivastatin can be increased when it is combined with Ceritinib.
ChloroquineThe serum concentration of Cerivastatin can be increased when it is combined with Chloroquine.
ChlorpromazineThe serum concentration of Cerivastatin can be increased when it is combined with Chlorpromazine.
ChlorpropamideThe serum concentration of Cerivastatin can be increased when it is combined with Chlorpropamide.
ChlorprothixeneThe serum concentration of Cerivastatin can be increased when it is combined with Chlorprothixene.
CholesterolThe serum concentration of Cerivastatin can be increased when it is combined with Cholesterol.
Cholic AcidThe serum concentration of Cerivastatin can be decreased when it is combined with Cholic Acid.
CilazaprilThe serum concentration of Cerivastatin can be increased when it is combined with Cilazapril.
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Cerivastatin.
CimetidineThe serum concentration of Cerivastatin can be decreased when it is combined with Cimetidine.
CiprofibrateThe risk or severity of adverse effects can be increased when Ciprofibrate is combined with Cerivastatin.
CiprofloxacinThe serum concentration of Cerivastatin can be increased when it is combined with Ciprofloxacin.
CitalopramThe serum concentration of Cerivastatin can be increased when it is combined with Citalopram.
ClarithromycinThe serum concentration of Cerivastatin can be increased when it is combined with Clarithromycin.
ClemastineThe metabolism of Cerivastatin can be decreased when combined with Clemastine.
ClofazimineThe serum concentration of Cerivastatin can be increased when it is combined with Clofazimine.
ClomipramineThe serum concentration of Cerivastatin can be increased when it is combined with Clomipramine.
ClopidogrelThe metabolism of Cerivastatin can be decreased when combined with Clopidogrel.
ClotrimazoleThe metabolism of Cerivastatin can be decreased when combined with Clotrimazole.
CobicistatThe serum concentration of Cerivastatin can be increased when it is combined with Cobicistat.
ColchicineThe serum concentration of Cerivastatin can be increased when it is combined with Colchicine.
ColforsinThe serum concentration of Cerivastatin can be increased when it is combined with Colforsin.
ConivaptanThe serum concentration of Cerivastatin can be increased when it is combined with Conivaptan.
CrizotinibThe metabolism of Cerivastatin can be decreased when combined with Crizotinib.
CyclophosphamideThe serum concentration of Cerivastatin can be increased when it is combined with Cyclophosphamide.
CyclosporineThe metabolism of Cerivastatin can be decreased when combined with Cyclosporine.
Cyproterone acetateThe serum concentration of Cerivastatin can be increased when it is combined with Cyproterone acetate.
DabrafenibThe serum concentration of Cerivastatin can be decreased when it is combined with Dabrafenib.
DaclatasvirThe serum concentration of Cerivastatin can be increased when it is combined with Daclatasvir.
DactinomycinThe serum concentration of Cerivastatin can be increased when it is combined with Dactinomycin.
DanazolThe serum concentration of Cerivastatin can be increased when it is combined with Danazol.
DaptomycinThe risk or severity of adverse effects can be increased when Cerivastatin is combined with Daptomycin.
DarunavirThe metabolism of Cerivastatin can be decreased when combined with Darunavir.
DasatinibThe serum concentration of Cerivastatin can be increased when it is combined with Dasatinib.
DaunorubicinThe serum concentration of Cerivastatin can be decreased when it is combined with Daunorubicin.
DeferasiroxThe serum concentration of Cerivastatin can be decreased when it is combined with Deferasirox.
DelavirdineThe metabolism of Cerivastatin can be decreased when combined with Delavirdine.
DesipramineThe serum concentration of Cerivastatin can be increased when it is combined with Desipramine.
DesloratadineThe serum concentration of Cerivastatin can be increased when it is combined with Desloratadine.
DexamethasoneThe serum concentration of Cerivastatin can be decreased when it is combined with Dexamethasone.
DextromethorphanThe serum concentration of Cerivastatin can be increased when it is combined with Dextromethorphan.
DiclofenacThe serum concentration of Cerivastatin can be increased when it is combined with Diclofenac.
DicoumarolCerivastatin may increase the anticoagulant activities of Dicoumarol.
DigoxinThe serum concentration of Cerivastatin can be decreased when it is combined with Digoxin.
DihydroergotamineThe metabolism of Cerivastatin can be decreased when combined with Dihydroergotamine.
DiltiazemThe metabolism of Cerivastatin can be decreased when combined with Diltiazem.
DipyridamoleThe serum concentration of Cerivastatin can be increased when it is combined with Dipyridamole.
DoxazosinThe serum concentration of Cerivastatin can be increased when it is combined with Doxazosin.
DoxepinThe serum concentration of Cerivastatin can be increased when it is combined with Doxepin.
DoxorubicinThe serum concentration of Cerivastatin can be decreased when it is combined with Doxorubicin.
DoxycyclineThe metabolism of Cerivastatin can be decreased when combined with Doxycycline.
DronabinolThe serum concentration of Cerivastatin can be increased when it is combined with Dronabinol.
DronedaroneThe metabolism of Cerivastatin can be decreased when combined with Dronedarone.
EfavirenzThe serum concentration of Cerivastatin can be decreased when it is combined with Efavirenz.
ElbasvirThe serum concentration of Cerivastatin can be increased when it is combined with Elbasvir.
EltrombopagThe serum concentration of Cerivastatin can be increased when it is combined with Eltrombopag.
EnalaprilThe serum concentration of Cerivastatin can be increased when it is combined with Enalapril.
EnzalutamideThe serum concentration of Cerivastatin can be increased when it is combined with Enzalutamide.
ErgonovineThe serum concentration of Cerivastatin can be increased when it is combined with Ergonovine.
ErgotamineThe serum concentration of Cerivastatin can be increased when it is combined with Ergotamine.
ErythromycinThe metabolism of Cerivastatin can be decreased when combined with Erythromycin.
Eslicarbazepine acetateThe serum concentration of Cerivastatin can be decreased when it is combined with Eslicarbazepine acetate.
EstramustineThe serum concentration of Cerivastatin can be increased when it is combined with Estramustine.
EstriolThe serum concentration of Cerivastatin can be decreased when it is combined with Estriol.
EstroneThe serum concentration of Cerivastatin can be decreased when it is combined with Estrone.
Ethyl biscoumacetateCerivastatin may increase the anticoagulant activities of Ethyl biscoumacetate.
EtoposideThe serum concentration of Cerivastatin can be increased when it is combined with Etoposide.
EtravirineThe serum concentration of Cerivastatin can be decreased when it is combined with Etravirine.
FelodipineThe serum concentration of Cerivastatin can be increased when it is combined with Felodipine.
FenofibrateThe risk or severity of adverse effects can be increased when Fenofibrate is combined with Cerivastatin.
FentanylThe serum concentration of Cerivastatin can be increased when it is combined with Fentanyl.
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Cerivastatin.
FexofenadineThe serum concentration of Cerivastatin can be increased when it is combined with Fexofenadine.
FidaxomicinThe serum concentration of Cerivastatin can be increased when it is combined with Fidaxomicin.
FluconazoleThe metabolism of Cerivastatin can be decreased when combined with Fluconazole.
FluoxetineThe serum concentration of Cerivastatin can be increased when it is combined with Fluoxetine.
FlupentixolThe serum concentration of Cerivastatin can be increased when it is combined with Flupentixol.
FluphenazineThe serum concentration of Cerivastatin can be increased when it is combined with Fluphenazine.
FlurazepamThe serum concentration of Cerivastatin can be increased when it is combined with Flurazepam.
FluvoxamineThe metabolism of Cerivastatin can be decreased when combined with Fluvoxamine.
FosamprenavirThe metabolism of Cerivastatin can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Cerivastatin can be increased when it is combined with Fosaprepitant.
FosphenytoinThe serum concentration of Cerivastatin can be decreased when it is combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Cerivastatin can be increased when it is combined with Fusidic Acid.
GefitinibThe serum concentration of Cerivastatin can be increased when it is combined with Gefitinib.
GemfibrozilThe metabolism of Cerivastatin can be decreased when combined with Gemfibrozil.
GenisteinThe serum concentration of Cerivastatin can be increased when it is combined with Genistein.
GlyburideThe serum concentration of Cerivastatin can be increased when it is combined with Glyburide.
GlycerolThe serum concentration of Cerivastatin can be increased when it is combined with Glycerol.
Gramicidin DThe serum concentration of Cerivastatin can be increased when it is combined with Gramicidin D.
GrepafloxacinThe serum concentration of Cerivastatin can be increased when it is combined with Grepafloxacin.
HaloperidolThe serum concentration of Cerivastatin can be increased when it is combined with Haloperidol.
HydrocortisoneThe serum concentration of Cerivastatin can be increased when it is combined with Hydrocortisone.
IdelalisibThe serum concentration of Cerivastatin can be increased when it is combined with Idelalisib.
ImatinibThe metabolism of Cerivastatin can be decreased when combined with Imatinib.
ImipramineThe serum concentration of Cerivastatin can be increased when it is combined with Imipramine.
IndinavirThe serum concentration of Cerivastatin can be decreased when it is combined with Indinavir.
IndomethacinThe serum concentration of Cerivastatin can be increased when it is combined with Indomethacin.
IrbesartanThe metabolism of Cerivastatin can be decreased when combined with Irbesartan.
IsavuconazoniumThe metabolism of Cerivastatin can be decreased when combined with Isavuconazonium.
IsradipineThe metabolism of Cerivastatin can be decreased when combined with Isradipine.
ItraconazoleThe serum concentration of Cerivastatin can be increased when it is combined with Itraconazole.
IvacaftorThe serum concentration of Cerivastatin can be increased when it is combined with Ivacaftor.
IvermectinThe serum concentration of Cerivastatin can be increased when it is combined with Ivermectin.
KetamineThe serum concentration of Cerivastatin can be increased when it is combined with Ketamine.
KetoconazoleThe serum concentration of Cerivastatin can be increased when it is combined with Ketoconazole.
LansoprazoleThe serum concentration of Cerivastatin can be increased when it is combined with Lansoprazole.
Lanthanum carbonateThe serum concentration of Lanthanum carbonate can be decreased when it is combined with Cerivastatin.
LapatinibThe serum concentration of Cerivastatin can be increased when it is combined with Lapatinib.
LevofloxacinThe serum concentration of Cerivastatin can be increased when it is combined with Levofloxacin.
LevothyroxineThe serum concentration of Cerivastatin can be decreased when it is combined with Levothyroxine.
LidocaineThe serum concentration of Cerivastatin can be increased when it is combined with Lidocaine.
LiothyronineThe serum concentration of Cerivastatin can be decreased when it is combined with Liothyronine.
LiotrixThe serum concentration of Cerivastatin can be decreased when it is combined with Liotrix.
LisinoprilThe serum concentration of Cerivastatin can be increased when it is combined with Lisinopril.
LomitapideThe serum concentration of Cerivastatin can be increased when it is combined with Lomitapide.
LoperamideThe serum concentration of Cerivastatin can be increased when it is combined with Loperamide.
LopinavirThe serum concentration of Cerivastatin can be increased when it is combined with Lopinavir.
LoratadineThe serum concentration of Cerivastatin can be increased when it is combined with Loratadine.
LosartanThe serum concentration of Cerivastatin can be increased when it is combined with Losartan.
LovastatinThe metabolism of Cerivastatin can be decreased when combined with Lovastatin.
LuliconazoleThe serum concentration of Cerivastatin can be increased when it is combined with Luliconazole.
LumacaftorThe serum concentration of Cerivastatin can be decreased when it is combined with Lumacaftor.
MagaldrateThe serum concentration of Cerivastatin can be decreased when it is combined with Magaldrate.
Magnesium carbonateThe serum concentration of Cerivastatin can be decreased when it is combined with Magnesium carbonate.
Magnesium hydroxideThe serum concentration of Cerivastatin can be decreased when it is combined with Magnesium hydroxide.
Magnesium oxideThe serum concentration of Cerivastatin can be decreased when it is combined with Magnesium oxide.
Magnesium TrisilicateThe serum concentration of Cerivastatin can be decreased when it is combined with Magnesium Trisilicate.
MaprotilineThe serum concentration of Cerivastatin can be increased when it is combined with Maprotiline.
MebendazoleThe serum concentration of Cerivastatin can be increased when it is combined with Mebendazole.
MefloquineThe serum concentration of Cerivastatin can be increased when it is combined with Mefloquine.
Megestrol acetateThe serum concentration of Cerivastatin can be increased when it is combined with Megestrol acetate.
MeprobamateThe serum concentration of Cerivastatin can be increased when it is combined with Meprobamate.
MethadoneThe serum concentration of Cerivastatin can be increased when it is combined with Methadone.
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Cerivastatin.
MibefradilThe serum concentration of Cerivastatin can be increased when it is combined with Mibefradil.
MiconazoleThe serum concentration of Cerivastatin can be increased when it is combined with Miconazole.
MidazolamThe serum concentration of Cerivastatin can be decreased when it is combined with Midazolam.
MifepristoneThe metabolism of Cerivastatin can be decreased when combined with Mifepristone.
MitomycinThe serum concentration of Cerivastatin can be increased when it is combined with Mitomycin.
MitotaneThe serum concentration of Cerivastatin can be decreased when it is combined with Mitotane.
MitoxantroneThe serum concentration of Cerivastatin can be decreased when it is combined with Mitoxantrone.
ModafinilThe serum concentration of Cerivastatin can be decreased when it is combined with Modafinil.
MorphineThe serum concentration of Cerivastatin can be increased when it is combined with Morphine.
NafcillinThe serum concentration of Cerivastatin can be decreased when it is combined with Nafcillin.
NaltrexoneThe serum concentration of Cerivastatin can be increased when it is combined with Naltrexone.
NaringeninThe serum concentration of Cerivastatin can be increased when it is combined with Naringenin.
NefazodoneThe serum concentration of Cerivastatin can be decreased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Cerivastatin can be decreased when it is combined with Nelfinavir.
NeostigmineThe serum concentration of Cerivastatin can be increased when it is combined with Neostigmine.
NetupitantThe serum concentration of Cerivastatin can be increased when it is combined with Netupitant.
NevirapineThe metabolism of Cerivastatin can be decreased when combined with Nevirapine.
NiacinThe risk or severity of adverse effects can be increased when Niacin is combined with Cerivastatin.
NicardipineThe serum concentration of Cerivastatin can be increased when it is combined with Nicardipine.
NicotinamideThe risk or severity of adverse effects can be increased when Nicotinamide is combined with Cerivastatin.
NifedipineThe serum concentration of Cerivastatin can be decreased when it is combined with Nifedipine.
NilotinibThe metabolism of Cerivastatin can be decreased when combined with Nilotinib.
NintedanibThe serum concentration of Nintedanib can be decreased when it is combined with Cerivastatin.
NisoldipineThe serum concentration of Cerivastatin can be increased when it is combined with Nisoldipine.
NitrazepamThe serum concentration of Cerivastatin can be increased when it is combined with Nitrazepam.
NitrendipineThe serum concentration of Cerivastatin can be increased when it is combined with Nitrendipine.
NorethisteroneThe serum concentration of Cerivastatin can be decreased when it is combined with Norethisterone.
OlaparibThe metabolism of Cerivastatin can be decreased when combined with Olaparib.
OmeprazoleThe serum concentration of Cerivastatin can be increased when it is combined with Omeprazole.
OsimertinibThe serum concentration of Cerivastatin can be increased when it is combined with Osimertinib.
P-NitrophenolThe serum concentration of Cerivastatin can be increased when it is combined with P-Nitrophenol.
PaclitaxelThe serum concentration of Cerivastatin can be increased when it is combined with Paclitaxel.
PalbociclibThe serum concentration of Cerivastatin can be increased when it is combined with Palbociclib.
Palmitic AcidThe serum concentration of Cerivastatin can be increased when it is combined with Palmitic Acid.
PantoprazoleThe serum concentration of Cerivastatin can be increased when it is combined with Pantoprazole.
ParoxetineThe serum concentration of Cerivastatin can be increased when it is combined with Paroxetine.
PazopanibCerivastatin may increase the hepatotoxic activities of Pazopanib.
PentobarbitalThe metabolism of Cerivastatin can be increased when combined with Pentobarbital.
PerindoprilThe serum concentration of Cerivastatin can be increased when it is combined with Perindopril.
PhenindioneCerivastatin may increase the anticoagulant activities of Phenindione.
PhenobarbitalThe serum concentration of Cerivastatin can be decreased when it is combined with Phenobarbital.
PhenprocoumonCerivastatin may increase the anticoagulant activities of Phenprocoumon.
PhenytoinThe serum concentration of Cerivastatin can be decreased when it is combined with Phenytoin.
PimozideThe serum concentration of Cerivastatin can be increased when it is combined with Pimozide.
PioglitazoneThe metabolism of Cerivastatin can be decreased when combined with Pioglitazone.
Platelet Activating FactorThe serum concentration of Cerivastatin can be decreased when it is combined with Platelet Activating Factor.
PonatinibThe serum concentration of Cerivastatin can be increased when it is combined with Ponatinib.
PosaconazoleThe serum concentration of Cerivastatin can be increased when it is combined with Posaconazole.
PravastatinThe serum concentration of Cerivastatin can be increased when it is combined with Pravastatin.
PrazosinThe serum concentration of Cerivastatin can be increased when it is combined with Prazosin.
PrednisoneThe serum concentration of Cerivastatin can be increased when it is combined with Prednisone.
PrimidoneThe metabolism of Cerivastatin can be increased when combined with Primidone.
ProbenecidThe serum concentration of Cerivastatin can be increased when it is combined with Probenecid.
ProgesteroneThe serum concentration of Cerivastatin can be decreased when it is combined with Progesterone.
PromethazineThe serum concentration of Cerivastatin can be increased when it is combined with Promethazine.
PropafenoneThe serum concentration of Cerivastatin can be increased when it is combined with Propafenone.
PropranololThe serum concentration of Cerivastatin can be increased when it is combined with Propranolol.
ProtriptylineThe serum concentration of Cerivastatin can be increased when it is combined with Protriptyline.
QuercetinThe serum concentration of Cerivastatin can be increased when it is combined with Quercetin.
QuinacrineThe serum concentration of Cerivastatin can be increased when it is combined with Quinacrine.
QuinidineThe serum concentration of Cerivastatin can be increased when it is combined with Quinidine.
QuinineThe serum concentration of Cerivastatin can be increased when it is combined with Quinine.
RabeprazoleThe metabolism of Cerivastatin can be decreased when combined with Rabeprazole.
RaltegravirRaltegravir may increase the myopathic rhabdomyolysis activities of Cerivastatin.
RanitidineThe serum concentration of Cerivastatin can be increased when it is combined with Ranitidine.
RanolazineThe serum concentration of Cerivastatin can be increased when it is combined with Ranolazine.
ReboxetineThe serum concentration of Cerivastatin can be increased when it is combined with Reboxetine.
RegorafenibThe serum concentration of Cerivastatin can be increased when it is combined with Regorafenib.
ReserpineThe serum concentration of Cerivastatin can be decreased when it is combined with Reserpine.
RifabutinThe metabolism of Cerivastatin can be increased when combined with Rifabutin.
RifampicinThe serum concentration of Cerivastatin can be decreased when it is combined with Rifampicin.
RifapentineThe metabolism of Cerivastatin can be increased when combined with Rifapentine.
RilpivirineThe serum concentration of Cerivastatin can be increased when it is combined with Rilpivirine.
RitonavirThe serum concentration of Cerivastatin can be decreased when it is combined with Ritonavir.
RolapitantThe serum concentration of Cerivastatin can be increased when it is combined with Rolapitant.
RosiglitazoneThe metabolism of Cerivastatin can be decreased when combined with Rosiglitazone.
SaquinavirThe serum concentration of Cerivastatin can be decreased when it is combined with Saquinavir.
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Cerivastatin.
ScopolamineThe serum concentration of Cerivastatin can be increased when it is combined with Scopolamine.
SecobarbitalThe metabolism of Cerivastatin can be increased when combined with Secobarbital.
SelegilineThe serum concentration of Cerivastatin can be increased when it is combined with Selegiline.
SertralineThe serum concentration of Cerivastatin can be increased when it is combined with Sertraline.
SildenafilThe metabolism of Cerivastatin can be decreased when combined with Sildenafil.
SiltuximabThe serum concentration of Cerivastatin can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Cerivastatin can be increased when it is combined with Simeprevir.
SimvastatinThe serum concentration of Cerivastatin can be increased when it is combined with Simvastatin.
SirolimusThe serum concentration of Cerivastatin can be decreased when it is combined with Sirolimus.
SorafenibThe serum concentration of Cerivastatin can be increased when it is combined with Sorafenib.
SpironolactoneThe serum concentration of Cerivastatin can be increased when it is combined with Spironolactone.
St. John's WortThe serum concentration of Cerivastatin can be decreased when it is combined with St. John's Wort.
StaurosporineThe serum concentration of Cerivastatin can be increased when it is combined with Staurosporine.
StiripentolThe serum concentration of Cerivastatin can be increased when it is combined with Stiripentol.
StreptozocinThe serum concentration of Cerivastatin can be decreased when it is combined with Streptozocin.
SulfamethoxazoleThe metabolism of Cerivastatin can be decreased when combined with Sulfamethoxazole.
SulfinpyrazoneThe serum concentration of Cerivastatin can be increased when it is combined with Sulfinpyrazone.
SulfisoxazoleThe metabolism of Cerivastatin can be decreased when combined with Sulfisoxazole.
SumatriptanThe serum concentration of Cerivastatin can be increased when it is combined with Sumatriptan.
SunitinibThe serum concentration of Cerivastatin can be increased when it is combined with Sunitinib.
TacrineThe serum concentration of Cerivastatin can be increased when it is combined with Tacrine.
TacrolimusThe serum concentration of Cerivastatin can be decreased when it is combined with Tacrolimus.
TamoxifenThe serum concentration of Cerivastatin can be decreased when it is combined with Tamoxifen.
Taurocholic AcidThe serum concentration of Cerivastatin can be increased when it is combined with Taurocholic Acid.
TelaprevirThe metabolism of Cerivastatin can be decreased when combined with Telaprevir.
TelithromycinThe metabolism of Cerivastatin can be decreased when combined with Telithromycin.
TelmisartanThe serum concentration of Cerivastatin can be increased when it is combined with Telmisartan.
TemsirolimusThe serum concentration of Cerivastatin can be increased when it is combined with Temsirolimus.
TerazosinThe serum concentration of Cerivastatin can be increased when it is combined with Terazosin.
TerfenadineThe serum concentration of Cerivastatin can be increased when it is combined with Terfenadine.
TeriflunomideThe serum concentration of Cerivastatin can be increased when it is combined with Teriflunomide.
TesmilifeneThe serum concentration of Cerivastatin can be decreased when it is combined with Tesmilifene.
TestosteroneThe serum concentration of Cerivastatin can be increased when it is combined with Testosterone.
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Cerivastatin.
TicagrelorThe serum concentration of Cerivastatin can be increased when it is combined with Ticagrelor.
TiclopidineThe metabolism of Cerivastatin can be decreased when combined with Ticlopidine.
TocilizumabThe serum concentration of Cerivastatin can be decreased when it is combined with Tocilizumab.
TolvaptanThe serum concentration of Cerivastatin can be increased when it is combined with Tolvaptan.
TrabectedinCerivastatin may increase the myopathic rhabdomyolysis activities of Trabectedin.
TrazodoneThe serum concentration of Cerivastatin can be decreased when it is combined with Trazodone.
TrifluoperazineThe serum concentration of Cerivastatin can be increased when it is combined with Trifluoperazine.
TriflupromazineThe serum concentration of Cerivastatin can be increased when it is combined with Triflupromazine.
TrimethoprimThe serum concentration of Cerivastatin can be decreased when it is combined with Trimethoprim.
TrimipramineThe serum concentration of Cerivastatin can be increased when it is combined with Trimipramine.
TroleandomycinThe serum concentration of Cerivastatin can be increased when it is combined with Troleandomycin.
VenlafaxineThe metabolism of Cerivastatin can be decreased when combined with Venlafaxine.
VerapamilThe metabolism of Cerivastatin can be decreased when combined with Verapamil.
VinblastineThe serum concentration of Cerivastatin can be decreased when it is combined with Vinblastine.
VincristineThe serum concentration of Cerivastatin can be decreased when it is combined with Vincristine.
VinorelbineThe serum concentration of Cerivastatin can be increased when it is combined with Vinorelbine.
VoriconazoleThe metabolism of Cerivastatin can be decreased when combined with Voriconazole.
WarfarinCerivastatin may increase the anticoagulant activities of Warfarin.
ZimelidineThe serum concentration of Cerivastatin can be increased when it is combined with Zimelidine.
ZiprasidoneThe metabolism of Cerivastatin can be decreased when combined with Ziprasidone.
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.

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 ]
Comments
comments powered by Disqus
Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23