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Identification
NameClofibrate
Accession NumberDB00636  (APRD00879)
TypeSmall Molecule
GroupsApproved
DescriptionA fibric acid derivative used in the treatment of hyperlipoproteinemia type III and severe hypertriglyceridemia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p986)
Structure
Thumb
Synonyms
2-(4-Chlorophenoxy)-2-methylpropanoic acid ethyl ester
2-(p-Chlorophenoxy)-2-methylpropionic acid ethyl ester
alpha-(p-Chlorophenoxy)isobutyric acid, ethyl ester
alpha-p-Chlorophenoxyisobutyryl ethyl ester
Atromid-S
Clofibrate
Clofibrato
Clofibratum
ELPI
EPIB
Ethyl 2-(P-chlorophenoxy)isobutyrate
Ethyl chlorophenoxyisobutyrate
Ethyl clofibrate
Lipofacton
Liprin
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Atromid S Cap 500mgcapsule500 mgoralAyerst Laboratories1968-12-311997-08-15Canada
Atromid-S 1gmcapsule1 goralWyeth Ayerst Canada Inc.1994-12-311998-10-20Canada
Atromid-S Cap 500mgcapsule500 mgoralWyeth Ayerst Canada Inc.1996-10-252000-08-02Canada
Novo-fibrate Cap 500mgcapsule500 mgoralNovopharm Limited1976-12-312005-08-10Canada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
AlufibrateThe Central
Atromid-SNot Available
BinogracKotobuki Seiyaku
ClobrateJohnson
ClofibrateBanner
HisunseroNewai Chem
KolivaGolden Horse
MyanlinSinton
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIHPN91K7FU3
CAS number637-07-0
WeightAverage: 242.699
Monoisotopic: 242.070972053
Chemical FormulaC12H15ClO3
InChI KeyInChIKey=KNHUKKLJHYUCFP-UHFFFAOYSA-N
InChI
InChI=1S/C12H15ClO3/c1-4-15-11(14)12(2,3)16-10-7-5-9(13)6-8-10/h5-8H,4H2,1-3H3
IUPAC Name
ethyl 2-(4-chlorophenoxy)-2-methylpropanoate
SMILES
CCOC(=O)C(C)(C)OC1=CC=C(Cl)C=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenoxyacetic acid derivatives. These are compounds containing an anisole where the methane group is linked to an acetic acid or a derivative.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassPhenoxyacetic acid derivatives
Direct ParentPhenoxyacetic acid derivatives
Alternative Parents
Substituents
  • Phenoxyacetate
  • Phenol ether
  • Halobenzene
  • Chlorobenzene
  • Alkyl aryl ether
  • Aryl halide
  • Aryl chloride
  • Carboxylic acid ester
  • Monocarboxylic acid or derivatives
  • Ether
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organochloride
  • Organohalogen compound
  • Carbonyl group
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External Descriptors
Pharmacology
IndicationFor Primary Dysbetalipoproteinemia (Type III hyperlipidemia) that does not respond adequately to diet. This helps control high cholesterol and high triglyceride levels.
PharmacodynamicsClofibrate is an antilipidemic agent similar to gemfibrozil. It acts to lower elevated serum lipids by reducing the very low-density lipoprotein fraction (Sf 20-400) rich in triglycerides. Serum cholesterol may be decreased, particularly in those patients whose cholesterol elevation is due to the presence of IDL as a result of Type III hyperlipoproteinemia. Several investigators have observed in their studies that clofibrate may produce a decrease in cholesterol linoleate but an increase in palmitoleate and oleate, the latter being considered atherogenic in experimental animals. The significance of this finding is unknown at this time. Reduction of triglycerides in some patients treated with clofibrate or certain of its chemically and clinically similar analogs may be associated with an increase in LDL cholesterol. Increase in LDL cholesterol has been observed in patients whose cholesterol is initially normal. Animal studies suggest that clofibrate interrupts cholesterol biosynthesis prior to mevalonate formation.
Mechanism of actionClofibrate increases the activity of extrahepatic lipoprotein lipase (LL), thereby increasing lipoprotein triglyceride lipolysis. Chylomicrons are degraded, VLDLs are converted to LDLs, and LDLs are converted to HDL. This is accompanied by a slight increase in secretion of lipids into the bile and ultimately the intestine. Clofibrate also inhibits the synthesis and increases the clearance of apolipoprotein B, a carrier molecule for VLDL. Also, as a fibrate, Clofibrate is an agonist of the PPAR-α receptor[4] in muscle, liver, and other tissues. This agonism ultimately leads to modification in gene expression resulting in increased beta-oxidation, decreased triglyceride secretion, increased HDL, increased lipoprotein lipase activity.
Related Articles
AbsorptionCompletely but slowly absorbed from the intestine. Between 95% and 99% of an oral dose of clofibrate is excreted in the urine as free and conjugated clofibric acid; thus, the absorption of clofibrate is virtually complete.
Volume of distributionNot Available
Protein bindingHighly protein-bound (95% to 97%).
Metabolism

Hepatic and gastrointestinal: rapid de-esterification occurs in the gastrointestinal tract and/or on first-pass metabolism to produce the active form, clofibric acid (chlorophenoxy isobutyric acid [CPIB]).

Route of eliminationNot Available
Half lifeHalf-life in normal volunteers averages 18 to 22 hours (range 14 to 35 hours) but can vary by up to 7 hours in the same subject at different times.
ClearanceNot Available
ToxicityOral, mouse: LD50 = 1220 mg/kg; Oral, rabbit: LD50 = 1370 mg/kg; Oral, rat: LD50 = 940 mg/kg. No reported case of overdosage in humans.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9329
Caco-2 permeable+0.717
P-glycoprotein substrateNon-substrate0.589
P-glycoprotein inhibitor INon-inhibitor0.7133
P-glycoprotein inhibitor IINon-inhibitor0.8544
Renal organic cation transporterNon-inhibitor0.8868
CYP450 2C9 substrateNon-substrate0.8517
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.6692
CYP450 1A2 substrateInhibitor0.9107
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorNon-inhibitor0.8861
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.5832
Ames testNon AMES toxic0.9132
CarcinogenicityNon-carcinogens0.5492
BiodegradationNot ready biodegradable0.9711
Rat acute toxicity2.3806 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9891
hERG inhibition (predictor II)Non-inhibitor0.8735
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Wyeth ayerst laboratories
  • Banner pharmacaps inc
  • Sandoz inc
  • Teva pharmaceuticals usa inc
  • Usl pharma inc
  • Watson laboratories inc
Packagers
Dosage forms
FormRouteStrength
Capsuleoral1 g
Capsuleoral500 mg
PricesNot Available
PatentsNot Available
Properties
StateLiquid
Experimental Properties
PropertyValueSource
melting point118-119Jones, W.G.M.,Thorp, J.M. and Waring, W.S.; U.S. Patent 3,262,850; July 26, 1966; assigned to Imperial Chemical Industries Limited, England.
boiling point149 °C at 2.00E+01 mm HgPhysProp
water solubilityInsolubleNot Available
logP3.3Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.029 mg/mLALOGPS
logP3.99ALOGPS
logP3.4ChemAxon
logS-3.9ALOGPS
pKa (Strongest Basic)-4.9ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area35.53 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity62.14 m3·mol-1ChemAxon
Polarizability24.7 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (7.78 KB)
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
MSMass Spectrum (Electron Ionization)splash10-004i-3900000000-fc2f01df51d424557e9fView in MoNA
References
Synthesis Reference

Jones, W.G.M.,Thorp, J.M. and Waring, W.S.; U.S. Patent 3,262,850; July 26, 1966; assigned to Imperial Chemical Industries Limited, England.

General ReferencesNot Available
External Links
ATC CodesC10AB01
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (62.6 KB)
Interactions
Drug Interactions
Drug
AcenocoumarolClofibrate may increase the anticoagulant activities of Acenocoumarol.
AcetohexamideClofibrate may increase the hypoglycemic activities of Acetohexamide.
AcipimoxAcipimox may increase the myopathic rhabdomyolysis activities of Clofibrate.
AmiodaroneThe metabolism of Clofibrate can be decreased when combined with Amiodarone.
AprepitantThe serum concentration of Clofibrate can be increased when it is combined with Aprepitant.
AripiprazoleThe serum concentration of Aripiprazole can be decreased when it is combined with Clofibrate.
ArtesunateThe serum concentration of the active metabolites of Artesunate can be reduced when Artesunate is used in combination with Clofibrate resulting in a loss in efficacy.
AtazanavirThe metabolism of Clofibrate can be decreased when combined with Atazanavir.
AtomoxetineThe metabolism of Clofibrate can be decreased when combined with Atomoxetine.
BexaroteneThe serum concentration of Clofibrate can be decreased when it is combined with Bexarotene.
BoceprevirThe metabolism of Clofibrate can be decreased when combined with Boceprevir.
BortezomibThe metabolism of Clofibrate can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Clofibrate can be decreased when it is combined with Bosentan.
CarbamazepineThe metabolism of Clofibrate can be increased when combined with Carbamazepine.
CeritinibThe serum concentration of Clofibrate can be increased when it is combined with Ceritinib.
Chenodeoxycholic acidThe therapeutic efficacy of Chenodeoxycholic acid can be decreased when used in combination with Clofibrate.
ChlorpropamideClofibrate may increase the hypoglycemic activities of Chlorpropamide.
CholestyramineCholestyramine can cause a decrease in the absorption of Clofibrate resulting in a reduced serum concentration and potentially a decrease in efficacy.
CiprofibrateThe risk or severity of adverse effects can be increased when Ciprofibrate is combined with Clofibrate.
ClarithromycinThe metabolism of Clofibrate can be decreased when combined with Clarithromycin.
ClemastineThe metabolism of Clofibrate can be decreased when combined with Clemastine.
ClotrimazoleThe metabolism of Clofibrate can be decreased when combined with Clotrimazole.
CobicistatThe metabolism of Clofibrate can be decreased when combined with Cobicistat.
ColchicineClofibrate may increase the myopathic rhabdomyolysis activities of Colchicine.
ColesevelamColesevelam can cause a decrease in the absorption of Clofibrate resulting in a reduced serum concentration and potentially a decrease in efficacy.
ColestipolColestipol can cause a decrease in the absorption of Clofibrate resulting in a reduced serum concentration and potentially a decrease in efficacy.
ConivaptanThe serum concentration of Clofibrate can be increased when it is combined with Conivaptan.
CrizotinibThe metabolism of Clofibrate can be decreased when combined with Crizotinib.
CyclosporineThe metabolism of Clofibrate can be decreased when combined with Cyclosporine.
DabrafenibThe serum concentration of Clofibrate can be decreased when it is combined with Dabrafenib.
DarunavirThe metabolism of Clofibrate can be decreased when combined with Darunavir.
DasatinibThe serum concentration of Clofibrate can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Clofibrate can be decreased when it is combined with Deferasirox.
DelavirdineThe metabolism of Clofibrate can be decreased when combined with Delavirdine.
DexamethasoneThe serum concentration of Clofibrate can be decreased when it is combined with Dexamethasone.
DicoumarolClofibrate may increase the anticoagulant activities of Dicoumarol.
DihydroergotamineThe metabolism of Clofibrate can be decreased when combined with Dihydroergotamine.
DiltiazemThe metabolism of Clofibrate can be decreased when combined with Diltiazem.
DoxycyclineThe metabolism of Clofibrate can be decreased when combined with Doxycycline.
DronedaroneThe metabolism of Clofibrate can be decreased when combined with Dronedarone.
EfavirenzThe serum concentration of Clofibrate can be decreased when it is combined with Efavirenz.
EnzalutamideThe serum concentration of Clofibrate can be decreased when it is combined with Enzalutamide.
ErythromycinThe metabolism of Clofibrate can be decreased when combined with Erythromycin.
Eslicarbazepine acetateThe serum concentration of Clofibrate can be decreased when it is combined with Eslicarbazepine acetate.
Ethyl biscoumacetateClofibrate may increase the anticoagulant activities of Ethyl biscoumacetate.
EtravirineThe serum concentration of Clofibrate can be decreased when it is combined with Etravirine.
FluconazoleThe metabolism of Clofibrate can be decreased when combined with Fluconazole.
FluvoxamineThe metabolism of Clofibrate can be decreased when combined with Fluvoxamine.
FosamprenavirThe metabolism of Clofibrate can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Clofibrate can be increased when it is combined with Fosaprepitant.
FosphenytoinThe metabolism of Clofibrate can be increased when combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Clofibrate can be increased when it is combined with Fusidic Acid.
GlibornurideClofibrate may increase the hypoglycemic activities of Glibornuride.
GliclazideClofibrate may increase the hypoglycemic activities of Gliclazide.
GlimepirideClofibrate may increase the hypoglycemic activities of Glimepiride.
GlipizideClofibrate may increase the hypoglycemic activities of Glipizide.
GliquidoneClofibrate may increase the hypoglycemic activities of Gliquidone.
GlisoxepideClofibrate may increase the hypoglycemic activities of Glisoxepide.
GlyburideClofibrate may increase the hypoglycemic activities of Glyburide.
IdelalisibThe serum concentration of Clofibrate can be increased when it is combined with Idelalisib.
ImatinibThe metabolism of Clofibrate can be decreased when combined with Imatinib.
IndinavirThe metabolism of Clofibrate can be decreased when combined with Indinavir.
IsavuconazoniumThe metabolism of Clofibrate can be decreased when combined with Isavuconazonium.
IsradipineThe metabolism of Clofibrate can be decreased when combined with Isradipine.
ItraconazoleThe metabolism of Clofibrate can be decreased when combined with Itraconazole.
IvacaftorThe serum concentration of Clofibrate can be increased when it is combined with Ivacaftor.
KetoconazoleThe metabolism of Clofibrate can be decreased when combined with Ketoconazole.
LopinavirThe metabolism of Clofibrate can be decreased when combined with Lopinavir.
LovastatinThe metabolism of Clofibrate can be decreased when combined with Lovastatin.
LuliconazoleThe serum concentration of Clofibrate can be increased when it is combined with Luliconazole.
MifepristoneThe metabolism of Clofibrate can be decreased when combined with Mifepristone.
MitotaneThe serum concentration of Clofibrate can be decreased when it is combined with Mitotane.
ModafinilThe serum concentration of Clofibrate can be decreased when it is combined with Modafinil.
NafcillinThe serum concentration of Clofibrate can be decreased when it is combined with Nafcillin.
NefazodoneThe metabolism of Clofibrate can be decreased when combined with Nefazodone.
NelfinavirThe metabolism of Clofibrate can be decreased when combined with Nelfinavir.
NetupitantThe serum concentration of Clofibrate can be increased when it is combined with Netupitant.
NevirapineThe metabolism of Clofibrate can be decreased when combined with Nevirapine.
NilotinibThe metabolism of Clofibrate can be decreased when combined with Nilotinib.
NintedanibThe serum concentration of Nintedanib can be decreased when it is combined with Clofibrate.
OlaparibThe metabolism of Clofibrate can be decreased when combined with Olaparib.
OsimertinibThe serum concentration of Clofibrate can be increased when it is combined with Osimertinib.
PalbociclibThe serum concentration of Clofibrate can be increased when it is combined with Palbociclib.
PentobarbitalThe metabolism of Clofibrate can be increased when combined with Pentobarbital.
PhenindioneClofibrate may increase the anticoagulant activities of Phenindione.
PhenobarbitalThe metabolism of Clofibrate can be increased when combined with Phenobarbital.
PhenprocoumonClofibrate may increase the anticoagulant activities of Phenprocoumon.
PhenytoinThe metabolism of Clofibrate can be increased when combined with Phenytoin.
PosaconazoleThe metabolism of Clofibrate can be decreased when combined with Posaconazole.
PrimidoneThe metabolism of Clofibrate can be increased when combined with Primidone.
RaltegravirRaltegravir may increase the myopathic rhabdomyolysis activities of Clofibrate.
RanolazineThe metabolism of Clofibrate can be decreased when combined with Ranolazine.
RifabutinThe metabolism of Clofibrate can be increased when combined with Rifabutin.
RifampicinThe metabolism of Clofibrate can be increased when combined with Rifampicin.
RifapentineThe metabolism of Clofibrate can be increased when combined with Rifapentine.
RitonavirThe metabolism of Clofibrate can be decreased when combined with Ritonavir.
SaquinavirThe metabolism of Clofibrate can be decreased when combined with Saquinavir.
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Clofibrate.
SildenafilThe metabolism of Clofibrate can be decreased when combined with Sildenafil.
SiltuximabThe serum concentration of Clofibrate can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Clofibrate can be increased when it is combined with Simeprevir.
St. John's WortThe serum concentration of Clofibrate can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Clofibrate can be increased when it is combined with Stiripentol.
SulfisoxazoleThe metabolism of Clofibrate can be decreased when combined with Sulfisoxazole.
TelaprevirThe metabolism of Clofibrate can be decreased when combined with Telaprevir.
TelithromycinThe metabolism of Clofibrate can be decreased when combined with Telithromycin.
TiclopidineThe metabolism of Clofibrate can be decreased when combined with Ticlopidine.
TocilizumabThe serum concentration of Clofibrate can be decreased when it is combined with Tocilizumab.
TolazamideClofibrate may increase the hypoglycemic activities of Tolazamide.
TolbutamideClofibrate may increase the hypoglycemic activities of Tolbutamide.
Ursodeoxycholic acidThe therapeutic efficacy of Ursodeoxycholic acid can be decreased when used in combination with Clofibrate.
VenlafaxineThe metabolism of Clofibrate can be decreased when combined with Venlafaxine.
VerapamilThe metabolism of Clofibrate can be decreased when combined with Verapamil.
VoriconazoleThe metabolism of Clofibrate can be decreased when combined with Voriconazole.
WarfarinClofibrate may increase the anticoagulant activities of Warfarin.
ZiprasidoneThe metabolism of Clofibrate can be decreased when combined with Ziprasidone.
Food Interactions
  • Take with food, since it may reduce gastric irritation.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Zinc ion binding
Specific Function:
Ligand-activated transcription factor. Key regulator of lipid metabolism. Activated by the endogenous ligand 1-palmitoyl-2-oleoyl-sn-glycerol-3-phosphocholine (16:0/18:1-GPC). Activated by oleylethanolamide, a naturally occurring lipid that regulates satiety. Receptor for peroxisome proliferators such as hypolipidemic drugs and fatty acids. Regulates the peroxisomal beta-oxidation pathway of fa...
Gene Name:
PPARA
Uniprot ID:
Q07869
Molecular Weight:
52224.595 Da
References
  1. Barclay TB, Peters JM, Sewer MB, Ferrari L, Gonzalez FJ, Morgan ET: Modulation of cytochrome P-450 gene expression in endotoxemic mice is tissue specific and peroxisome proliferator-activated receptor-alpha dependent. J Pharmacol Exp Ther. 1999 Sep;290(3):1250-7. [PubMed:10454501 ]
  2. Murata M, Kaji H, Takahashi Y, Iida K, Mizuno I, Okimura Y, Abe H, Chihara K: Stimulation by eicosapentaenoic acids of leptin mRNA expression and its secretion in mouse 3T3-L1 adipocytes in vitro. Biochem Biophys Res Commun. 2000 Apr 13;270(2):343-8. [PubMed:10753628 ]
  3. Hunt MC, Lindquist PJ, Peters JM, Gonzalez FJ, Diczfalusy U, Alexson SE: Involvement of the peroxisome proliferator-activated receptor alpha in regulating long-chain acyl-CoA thioesterases. J Lipid Res. 2000 May;41(5):814-23. [PubMed:10787442 ]
  4. Casas F, Domenjoud L, Rochard P, Hatier R, Rodier A, Daury L, Bianchi A, Kremarik-Bouillaud P, Becuwe P, Keller J, Schohn H, Wrutniak-Cabello C, Cabello G, Dauca M: A 45 kDa protein related to PPARgamma2, induced by peroxisome proliferators, is located in the mitochondrial matrix. FEBS Lett. 2000 Jul 28;478(1-2):4-8. [PubMed:10922459 ]
  5. Komuves LG, Hanley K, Lefebvre AM, Man MQ, Ng DC, Bikle DD, Williams ML, Elias PM, Auwerx J, Feingold KR: Stimulation of PPARalpha promotes epidermal keratinocyte differentiation in vivo. J Invest Dermatol. 2000 Sep;115(3):353-60. [PubMed:10951268 ]
  6. Gelosa P, Banfi C, Gianella A, Brioschi M, Pignieri A, Nobili E, Castiglioni L, Cimino M, Tremoli E, Sironi L: Peroxisome proliferator-activated receptor {alpha} agonism prevents renal damage and the oxidative stress and inflammatory processes affecting the brains of stroke-prone rats. J Pharmacol Exp Ther. 2010 Nov;335(2):324-31. doi: 10.1124/jpet.110.171090. Epub 2010 Jul 29. [PubMed:20671072 ]
  7. Palkar PS, Anderson CR, Ferry CH, Gonzalez FJ, Peters JM: Effect of prenatal peroxisome proliferator-activated receptor alpha (PPARalpha) agonism on postnatal development. Toxicology. 2010 Sep 30;276(1):79-84. doi: 10.1016/j.tox.2010.07.008. Epub 2010 Jul 15. [PubMed:20637823 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinducer
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. 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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Glutathione transferase activity
Specific Function:
Conjugation of reduced glutathione to a wide number of exogenous and endogenous hydrophobic electrophiles.
Gene Name:
GSTA2
Uniprot ID:
P09210
Molecular Weight:
25663.675 Da
References
  1. Foliot A, Touchard D, Mallet L: Inhibition of liver glutathione S-transferase activity in rats by hypolipidemic drugs related or unrelated to clofibrate. Biochem Pharmacol. 1986 May 15;35(10):1685-90. [PubMed:3707598 ]
  2. Foliot A, Touchard D, Celier C: Impairment of hepatic glutathione S-transferase activity as a cause of reduced biliary sulfobromophthalein excretion in clofibrate-treated rats. Biochem Pharmacol. 1984 Sep 15;33(18):2829-34. [PubMed:6477642 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Steroid hydroxylase activity
Specific Function:
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic or carcinogenic forms.
Gene Name:
CYP2E1
Uniprot ID:
P05181
Molecular Weight:
56848.42 Da
References
  1. 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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Vitamin d 24-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.
Gene Name:
CYP1A1
Uniprot ID:
P04798
Molecular Weight:
58164.815 Da
References
  1. 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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Constitutes the major nicotine C-oxidase. Acts as a 1,4-cineole 2-exo-monooxygenase. Possesses low phenacetin O-deethylation activity.
Gene Name:
CYP2A6
Uniprot ID:
P11509
Molecular Weight:
56501.005 Da
References
  1. 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 ]
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. 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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinducer
General Function:
Leukotriene-b4 20-monooxygenase activity
Specific Function:
Catalyzes the omega- and (omega-1)-hydroxylation of various fatty acids such as laurate, myristate and palmitate. Has little activity toward prostaglandins A1 and E1. Oxidizes arachidonic acid to 20-hydroxyeicosatetraenoic acid (20-HETE).
Gene Name:
CYP4A11
Uniprot ID:
Q02928
Molecular Weight:
59347.31 Da
References
  1. 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 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23