Identification

Name
Clofibrate
Accession Number
DB00636  (APRD00879)
Type
Small Molecule
Groups
Approved
Description

A 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
  • Clofibrate
  • Clofibrato
  • Clofibratum
  • ELPI
  • EPIB
  • Ethyl 2-(P-chlorophenoxy)isobutyrate
  • Ethyl chlorophenoxyisobutyrate
  • Ethyl clofibrate
  • Lipofacton
  • Liprin
External IDs
AY-61123 / ICI 28257 / ICI-28257 / NSC-79389
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
International/Other Brands
Alufibrate (The Central) / Atromid-S / Binograc (Kotobuki Seiyaku) / Clobrate (Johnson) / Clofibrate (Banner) / Hisunsero (Newai Chem) / Koliva (Golden Horse) / Myanlin (Sinton)
Categories
UNII
HPN91K7FU3
CAS number
637-07-0
Weight
Average: 242.699
Monoisotopic: 242.070972053
Chemical Formula
C12H15ClO3
InChI Key
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

Pharmacology

Indication

For Primary Dysbetalipoproteinemia (Type III hyperlipidemia) that does not respond adequately to diet. This helps control high cholesterol and high triglyceride levels.

Structured Indications
Not Available
Pharmacodynamics

Clofibrate 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 action

Clofibrate 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.

TargetActionsOrganism
APeroxisome proliferator-activated receptor alpha
agonist
Human
Absorption

Completely 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 distribution
Not Available
Protein binding

Highly 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 elimination
Not Available
Half life

Half-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.

Clearance
Not Available
Toxicity

Oral, 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
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AcenocoumarolClofibrate may increase the anticoagulant activities of Acenocoumarol.Approved
AcetohexamideClofibrate may increase the hypoglycemic activities of Acetohexamide.Withdrawn
AcipimoxAcipimox may increase the myopathic rhabdomyolysis activities of Clofibrate.Approved
AmiodaroneThe metabolism of Clofibrate can be decreased when combined with Amiodarone.Approved, Investigational
AprepitantThe serum concentration of Clofibrate can be increased when it is combined with Aprepitant.Approved, Investigational
AripiprazoleThe serum concentration of Aripiprazole can be decreased when it is combined with Clofibrate.Approved, Investigational
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.Approved
AtazanavirThe metabolism of Clofibrate can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Clofibrate can be decreased when combined with Atomoxetine.Approved
BoceprevirThe metabolism of Clofibrate can be decreased when combined with Boceprevir.Withdrawn
BortezomibThe metabolism of Clofibrate can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Clofibrate can be decreased when it is combined with Bosentan.Approved, Investigational
CarbamazepineThe metabolism of Clofibrate can be increased when combined with Carbamazepine.Approved, Investigational
CarbutamideClofibrate may increase the hypoglycemic activities of Carbutamide.Experimental
CeritinibThe serum concentration of Clofibrate can be increased when it is combined with Ceritinib.Approved
Chenodeoxycholic acidThe therapeutic efficacy of Chenodeoxycholic acid can be decreased when used in combination with Clofibrate.Approved
ChlorpropamideClofibrate may increase the hypoglycemic activities of Chlorpropamide.Approved
CholestyramineCholestyramine can cause a decrease in the absorption of Clofibrate resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
CiprofibrateThe risk or severity of adverse effects can be increased when Ciprofibrate is combined with Clofibrate.Approved
ClarithromycinThe metabolism of Clofibrate can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Clofibrate can be decreased when combined with Clemastine.Approved
ClorindioneClofibrate may increase the anticoagulant activities of Clorindione.Experimental
ClotrimazoleThe metabolism of Clofibrate can be decreased when combined with Clotrimazole.Approved, Vet Approved
CobicistatThe metabolism of Clofibrate can be decreased when combined with Cobicistat.Approved
ColchicineClofibrate may increase the myopathic rhabdomyolysis activities of Colchicine.Approved
ColesevelamColesevelam can cause a decrease in the absorption of Clofibrate resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
ColestipolColestipol can cause a decrease in the absorption of Clofibrate resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
ConivaptanThe serum concentration of Clofibrate can be increased when it is combined with Conivaptan.Approved, Investigational
CrizotinibThe metabolism of Clofibrate can be decreased when combined with Crizotinib.Approved
CyclosporineCyclosporine may increase the nephrotoxic activities of Clofibrate.Approved, Investigational, Vet Approved
DabrafenibThe serum concentration of Clofibrate can be decreased when it is combined with Dabrafenib.Approved
DarunavirThe metabolism of Clofibrate can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Clofibrate can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Clofibrate can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Clofibrate can be decreased when combined with Delavirdine.Approved
DicoumarolClofibrate may increase the anticoagulant activities of Dicoumarol.Approved
DihydroergotamineThe metabolism of Clofibrate can be decreased when combined with Dihydroergotamine.Approved
DiltiazemThe metabolism of Clofibrate can be decreased when combined with Diltiazem.Approved
DiphenadioneClofibrate may increase the anticoagulant activities of Diphenadione.Experimental
DoxycyclineThe metabolism of Clofibrate can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Clofibrate can be decreased when combined with Dronedarone.Approved
EnzalutamideThe serum concentration of Clofibrate can be decreased when it is combined with Enzalutamide.Approved
ErythromycinThe metabolism of Clofibrate can be decreased when combined with Erythromycin.Approved, Vet Approved
Ethyl biscoumacetateClofibrate may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
FluconazoleThe metabolism of Clofibrate can be decreased when combined with Fluconazole.Approved
FluindioneClofibrate may increase the anticoagulant activities of Fluindione.Investigational
FluvoxamineThe metabolism of Clofibrate can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Clofibrate can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Clofibrate can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Clofibrate can be increased when combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Clofibrate can be increased when it is combined with Fusidic Acid.Approved
GlibornurideClofibrate may increase the hypoglycemic activities of Glibornuride.Withdrawn
GliclazideClofibrate may increase the hypoglycemic activities of Gliclazide.Approved
GlipizideClofibrate may increase the hypoglycemic activities of Glipizide.Approved
GliquidoneClofibrate may increase the hypoglycemic activities of Gliquidone.Approved
GlisoxepideClofibrate may increase the hypoglycemic activities of Glisoxepide.Approved
GlyburideClofibrate may increase the hypoglycemic activities of Glyburide.Approved
IdelalisibThe serum concentration of Clofibrate can be increased when it is combined with Idelalisib.Approved
ImatinibThe metabolism of Clofibrate can be decreased when combined with Imatinib.Approved
IndinavirThe metabolism of Clofibrate can be decreased when combined with Indinavir.Approved
IsavuconazoniumThe metabolism of Clofibrate can be decreased when combined with Isavuconazonium.Approved, Investigational
IsradipineThe metabolism of Clofibrate can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Clofibrate can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Clofibrate can be increased when it is combined with Ivacaftor.Approved
KetoconazoleThe metabolism of Clofibrate can be decreased when combined with Ketoconazole.Approved, Investigational
LopinavirThe metabolism of Clofibrate can be decreased when combined with Lopinavir.Approved
LovastatinThe metabolism of Clofibrate can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Clofibrate can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Clofibrate can be increased when combined with Lumacaftor.Approved
MetahexamideClofibrate may increase the hypoglycemic activities of Metahexamide.Experimental
MifepristoneThe serum concentration of Clofibrate can be increased when it is combined with Mifepristone.Approved, Investigational
MitotaneThe serum concentration of Clofibrate can be decreased when it is combined with Mitotane.Approved
NefazodoneThe metabolism of Clofibrate can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Clofibrate can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Clofibrate can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Clofibrate can be increased when combined with Nevirapine.Approved
NilotinibThe metabolism of Clofibrate can be decreased when combined with Nilotinib.Approved, Investigational
OlaparibThe metabolism of Clofibrate can be decreased when combined with Olaparib.Approved
OsimertinibThe serum concentration of Clofibrate can be increased when it is combined with Osimertinib.Approved
PalbociclibThe serum concentration of Clofibrate can be increased when it is combined with Palbociclib.Approved
PentobarbitalThe metabolism of Clofibrate can be increased when combined with Pentobarbital.Approved, Vet Approved
PhenindioneClofibrate may increase the anticoagulant activities of Phenindione.Approved
PhenobarbitalThe metabolism of Clofibrate can be increased when combined with Phenobarbital.Approved
PhenprocoumonClofibrate may increase the anticoagulant activities of Phenprocoumon.Approved
PhenytoinThe metabolism of Clofibrate can be increased when combined with Phenytoin.Approved, Vet Approved
PosaconazoleThe metabolism of Clofibrate can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PrimidoneThe metabolism of Clofibrate can be increased when combined with Primidone.Approved, Vet Approved
RaltegravirRaltegravir may increase the myopathic rhabdomyolysis activities of Clofibrate.Approved
RanolazineThe metabolism of Clofibrate can be decreased when combined with Ranolazine.Approved, Investigational
RifabutinThe metabolism of Clofibrate can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Clofibrate can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Clofibrate can be increased when combined with Rifapentine.Approved
RitonavirThe metabolism of Clofibrate can be decreased when combined with Ritonavir.Approved, Investigational
SaquinavirThe metabolism of Clofibrate can be decreased when combined with Saquinavir.Approved, Investigational
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Clofibrate.Approved
SildenafilThe metabolism of Clofibrate can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Clofibrate can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Clofibrate can be increased when it is combined with Simeprevir.Approved
St. John's WortThe serum concentration of Clofibrate can be decreased when it is combined with St. John's Wort.Nutraceutical
StiripentolThe serum concentration of Clofibrate can be increased when it is combined with Stiripentol.Approved
SulfisoxazoleThe metabolism of Clofibrate can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
TelaprevirThe metabolism of Clofibrate can be decreased when combined with Telaprevir.Withdrawn
TelithromycinThe metabolism of Clofibrate can be decreased when combined with Telithromycin.Approved
TiclopidineThe metabolism of Clofibrate can be decreased when combined with Ticlopidine.Approved
TioclomarolClofibrate may increase the anticoagulant activities of Tioclomarol.Experimental
TocilizumabThe serum concentration of Clofibrate can be decreased when it is combined with Tocilizumab.Approved
TolazamideClofibrate may increase the hypoglycemic activities of Tolazamide.Approved
Ursodeoxycholic acidThe therapeutic efficacy of Ursodeoxycholic acid can be decreased when used in combination with Clofibrate.Approved, Investigational
VenlafaxineThe metabolism of Clofibrate can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Clofibrate can be decreased when combined with Verapamil.Approved
VoriconazoleThe metabolism of Clofibrate can be decreased when combined with Voriconazole.Approved, Investigational
WarfarinClofibrate may increase the anticoagulant activities of Warfarin.Approved
ZiprasidoneThe metabolism of Clofibrate can be decreased when combined with Ziprasidone.Approved
Food Interactions
  • Take with food, since it may reduce gastric irritation.

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 References
Not Available
External Links
Human Metabolome Database
HMDB14774
KEGG Drug
D00279
KEGG Compound
C06916
PubChem Compound
2796
PubChem Substance
46504748
ChemSpider
2694
BindingDB
50085047
ChEBI
3750
ChEMBL
CHEMBL565
Therapeutic Targets Database
DAP000262
PharmGKB
PA449045
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Clofibrate
ATC Codes
C10AB01 — Clofibrate
AHFS Codes
Not Available
PDB Entries
Not Available
FDA label
Not Available
MSDS
Download (62.6 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
Not AvailableCompletedPreventionCardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Heart Diseases / Myocardial Infarction (MI) / Myocardial Ischemia1

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
Prices
Not Available
Patents
Not Available

Properties

State
Liquid
Experimental Properties
PropertyValueSource
melting point (°C)118-119Jones, 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 point (°C)149 °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 RuleNoChemAxon
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)

Spectra

Mass Spec (NIST)
Download (7.78 KB)
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Mass Spectrum (Electron Ionization)MSsplash10-004i-3900000000-fc2f01df51d424557e9f
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as phenoxyacetic acid derivatives. These are compounds containing an anisole where the methane group is linked to an acetic acid or a derivative.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Phenoxyacetic acid derivatives
Direct Parent
Phenoxyacetic acid derivatives
Alternative Parents
Phenoxy compounds / Phenol ethers / Chlorobenzenes / Alkyl aryl ethers / Aryl chlorides / Carboxylic acid esters / Monocarboxylic acids and derivatives / Organochlorides / Organic oxides / Hydrocarbon derivatives
show 1 more
Substituents
Phenoxyacetate / Phenoxy compound / Phenol ether / Alkyl aryl ether / Chlorobenzene / Halobenzene / Aryl chloride / Aryl halide / Carboxylic acid ester / Carboxylic acid derivative
show 10 more
Molecular Framework
Aromatic homomonocyclic compounds
External Descriptors
ethyl ester, aromatic ether, monochlorobenzenes (CHEBI:3750)

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 oleyleth...
Gene Name
PPARA
Uniprot ID
Q07869
Uniprot Name
Peroxisome proliferator-activated receptor alpha
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
Substrate
Inducer
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. 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
Uniprot Name
Glutathione S-transferase A2
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 ...
Gene Name
CYP2E1
Uniprot ID
P05181
Uniprot Name
Cytochrome P450 2E1
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 un...
Gene Name
CYP1A1
Uniprot ID
P04798
Uniprot Name
Cytochrome P450 1A1
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. Const...
Gene Name
CYP2A6
Uniprot ID
P11509
Uniprot Name
Cytochrome P450 2A6
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 un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
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
Substrate
Inducer
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 2...
Gene Name
CYP4A11
Uniprot ID
Q02928
Uniprot Name
Cytochrome P450 4A11
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]

Drug created on June 13, 2005 07:24 / Updated on October 02, 2017 04:41