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Identification
NameSulfinpyrazone
Accession NumberDB01138  (APRD00620)
TypeSmall Molecule
GroupsApproved
DescriptionA uricosuric drug that is used to reduce the serum urate levels in gout therapy. It lacks anti-inflammatory, analgesic, and diuretic properties. [PubChem]
Structure
Thumb
Synonyms
1,2-Diphenyl-3,5-dioxo-4-(2-phenylsulfinylethyl)pyrazolidine
1,2-Diphenyl-4-(2'-phenylsulfinethyl)-3,5-pyrazolidinedione
4-(2-Benzenesulfinylethyl)-1,2-diphenylpyrazolidine-3,5-dione
Anturane (tn)
Sulfinpyrazone
Sulfoxyphenylpyrazolidine
External Identifiers
  • USAF GE-13
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Antazone Tab 100mgtablet100 mgoralIcn Canada Ltd.1980-12-312005-04-26Canada
Antazone Tab 200mgtablet200 mgoralIcn Canada Ltd.1980-12-312005-04-26Canada
Anturan 100mgtablet100 mgoralNovartis Pharmaceuticals Canada Inc1959-12-311999-08-04Canada
Anturan 200mgtablet200 mgoralNovartis Pharmaceuticals Canada Inc1961-12-311999-08-04Canada
Novo-pyrazone Tab 100mgtablet100 mgoralNovopharm Limited1979-12-312005-08-10Canada
Novo-pyrazone Tab 200mgtablet200 mgoralNovopharm Limited1979-12-312005-08-10Canada
Nu-sulfinpyrazone Tab 100mgtablet100 mgoralNu Pharm Inc1993-12-312008-02-20Canada
Nu-sulfinpyrazone Tab 200mgtablet200 mgoralNu Pharm Inc1993-12-312012-09-04Canada
Sulfinpyrazonetablet200 mgoralAa Pharma Inc1978-12-31Not applicableCanada
Sulfinpyrazone 100 Tabtablet100 mgoralPro Doc Limitee1979-12-312003-07-31Canada
Sulfinpyrazone 200 Tabtablet200 mgoralPro Doc Limitee1979-12-312003-07-31Canada
Sulfinpyrazone Tablets 100mgtablet100 mgoralLaboratoires Confab IncNot applicableNot applicableCanada
Sulfinpyrazone Tablets 200mgtablet200 mgoralLaboratoires Confab IncNot applicableNot applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo Sulfinpyrazone Tab 100mgtablet100 mgoralApotex Inc1978-12-312008-02-19Canada
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
AnturaneNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIV6OFU47K3W
CAS number57-96-5
WeightAverage: 404.482
Monoisotopic: 404.119463206
Chemical FormulaC23H20N2O3S
InChI KeyInChIKey=MBGGBVCUIVRRBF-UHFFFAOYSA-N
InChI
InChI=1S/C23H20N2O3S/c26-22-21(16-17-29(28)20-14-8-3-9-15-20)23(27)25(19-12-6-2-7-13-19)24(22)18-10-4-1-5-11-18/h1-15,21H,16-17H2
IUPAC Name
4-[2-(benzenesulfinyl)ethyl]-1,2-diphenylpyrazolidine-3,5-dione
SMILES
O=C1C(CCS(=O)C2=CC=CC=C2)C(=O)N(N1C1=CC=CC=C1)C1=CC=CC=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as benzene and substituted derivatives. These are aromatic compounds containing one monocyclic ring system consisting of benzene.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassNot Available
Direct ParentBenzene and substituted derivatives
Alternative Parents
Substituents
  • 1,3-dicarbonyl compound
  • Pyrazolidinone
  • Monocyclic benzene moiety
  • Pyrazolidine
  • Sulfoxide
  • Carboxylic acid hydrazide
  • Carboxamide group
  • Azacycle
  • Organoheterocyclic compound
  • Sulfinyl compound
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organosulfur compound
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the treatment of gout and gouty arthritis.
PharmacodynamicsSulfinpyrazone's pharmacologic activity is the potentiation of the urinary excretion of uric acid. It is useful for reducing the blood urate levels in patients with chronic tophaceous gout and acute intermittent gout, and for promoting the resorption of tophi.
Mechanism of actionSulfinpyrazone is an oral uricosuric agent (pyrazolone derivative) used to treat chronic or intermittent gouty arthritis. Sulfinpyrazone competitively inhibits the reabsorption of uric acid at the proximal convoluted tubule, thereby facilitating urinary excretion of uric acid and decreasing plasma urate concentrations. This is likely done through inhibition of the urate anion transporter (hURAT1) as well as the human organic anion transporter 4 (hOAT4). Sulfinpyrazone is not intended for the treatment of acute attacks because it lacks therapeutically useful analgesic and anti-inflammatory effects. Sulfinpyrazone and its sulfide metabolite possess COX inhibitory effects. Sulfinpyrazone has also been shown to be a UDP-glucuronsyltransferase inhibitor and a very potent CYP2C9 inhibitor. Sulfinpyrazone is also known to be a cystic fibrosis transmembrane conductance regulator (CFTR) inhibitor as well as an inhibitor of several multridrug resistance proteins (MRPs).
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein binding98-99%
Metabolism
SubstrateEnzymesProduct
Sulfinpyrazone
Sulfinpyrazone sulfideDetails
Sulfinpyrazone
Sulfinpyrazone sulfoneDetails
Route of eliminationNot Available
Half lifeApproximately 4-6 hours
ClearanceNot Available
ToxicitySymptoms of overdose include nausea, vomiting, diarrhea, epigastric pain, ataxia, labored respiration, convulsions, coma. Possible symptoms, seen after overdosage with other pyrazolone derivatives: anemia, jaundice, and ulceration.
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+0.9961
Blood Brain Barrier+0.9776
Caco-2 permeable-0.5583
P-glycoprotein substrateNon-substrate0.9163
P-glycoprotein inhibitor INon-inhibitor0.858
P-glycoprotein inhibitor IINon-inhibitor0.6257
Renal organic cation transporterNon-inhibitor0.8111
CYP450 2C9 substrateNon-substrate0.5504
CYP450 2D6 substrateNon-substrate0.8878
CYP450 3A4 substrateSubstrate0.5146
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorInhibitor0.8949
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorInhibitor0.796
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6332
Ames testNon AMES toxic0.6195
CarcinogenicityNon-carcinogens0.6932
BiodegradationNot ready biodegradable0.9577
Rat acute toxicity3.0218 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9712
hERG inhibition (predictor II)Non-inhibitor0.8418
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Tabletoral100 mg
Tabletoral200 mg
Prices
Unit descriptionCostUnit
Apo-Sulfinpyrazone 200 mg Tablet0.31USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point136-137 °CPhysProp
water solubility31.2 mg/LNot Available
logP2.30HANSCH,C ET AL. (1995)
pKa3.25SANGSTER (1994)
Predicted Properties
PropertyValueSource
Water Solubility0.323 mg/mLALOGPS
logP2.92ALOGPS
logP3.19ChemAxon
logS-3.1ALOGPS
pKa (Strongest Acidic)3.41ChemAxon
pKa (Strongest Basic)-6.7ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area57.69 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity113.62 m3·mol-1ChemAxon
Polarizability42.15 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
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
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesM04AB02
AHFS Codes
  • 40:40.00
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Sulfinpyrazone can be increased when it is combined with Abiraterone.
AcebutololThe serum concentration of Acebutolol can be increased when it is combined with Sulfinpyrazone.
AcenocoumarolThe metabolism of Acenocoumarol can be decreased when combined with Sulfinpyrazone.
AcetaminophenThe serum concentration of Acetaminophen can be increased when it is combined with Sulfinpyrazone.
Acetylsalicylic acidThe serum concentration of Acetylsalicylic acid can be increased when it is combined with Sulfinpyrazone.
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Sulfinpyrazone.
AldosteroneThe serum concentration of Aldosterone can be increased when it is combined with Sulfinpyrazone.
AlitretinoinThe serum concentration of Alitretinoin can be increased when it is combined with Sulfinpyrazone.
AmbrisentanThe serum concentration of Ambrisentan can be increased when it is combined with Sulfinpyrazone.
AmiodaroneThe metabolism of Sulfinpyrazone can be decreased when combined with Amiodarone.
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Sulfinpyrazone.
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Sulfinpyrazone.
AprepitantThe serum concentration of Sulfinpyrazone can be increased when it is combined with Aprepitant.
AripiprazoleThe serum concentration of Aripiprazole can be decreased when it is combined with Sulfinpyrazone.
Arsenic trioxideThe serum concentration of Arsenic trioxide can be increased when it is combined with Sulfinpyrazone.
AtazanavirThe metabolism of Sulfinpyrazone can be decreased when combined with Atazanavir.
AtazanavirThe serum concentration of Atazanavir can be increased when it is combined with Sulfinpyrazone.
AtenololThe serum concentration of Atenolol can be increased when it is combined with Sulfinpyrazone.
AtomoxetineThe metabolism of Sulfinpyrazone can be decreased when combined with Atomoxetine.
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Sulfinpyrazone.
BetamethasoneThe serum concentration of Betamethasone can be increased when it is combined with Sulfinpyrazone.
BexaroteneThe serum concentration of Sulfinpyrazone can be decreased when it is combined with Bexarotene.
BoceprevirThe metabolism of Sulfinpyrazone can be decreased when combined with Boceprevir.
BoceprevirThe serum concentration of Boceprevir can be increased when it is combined with Sulfinpyrazone.
BortezomibThe metabolism of Sulfinpyrazone can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Sulfinpyrazone can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Sulfinpyrazone.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Sulfinpyrazone.
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Sulfinpyrazone.
CabazitaxelThe serum concentration of Cabazitaxel can be increased when it is combined with Sulfinpyrazone.
CaffeineThe serum concentration of Caffeine can be increased when it is combined with Sulfinpyrazone.
CamptothecinThe serum concentration of Camptothecin can be increased when it is combined with Sulfinpyrazone.
CanagliflozinThe serum concentration of Canagliflozin can be increased when it is combined with Sulfinpyrazone.
CapecitabineThe metabolism of Sulfinpyrazone can be decreased when combined with Capecitabine.
CarbamazepineThe metabolism of Sulfinpyrazone can be increased when combined with Carbamazepine.
CarbamazepineThe serum concentration of Carbamazepine can be increased when it is combined with Sulfinpyrazone.
CarfilzomibThe serum concentration of Carfilzomib can be increased when it is combined with Sulfinpyrazone.
CelecoxibThe metabolism of Sulfinpyrazone can be decreased when combined with Celecoxib.
CeritinibThe serum concentration of Sulfinpyrazone can be increased when it is combined with Ceritinib.
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Sulfinpyrazone.
ChlorpromazineThe serum concentration of Chlorpromazine can be increased when it is combined with Sulfinpyrazone.
CholecalciferolThe metabolism of Sulfinpyrazone can be decreased when combined with Cholecalciferol.
CimetidineThe serum concentration of Cimetidine can be increased when it is combined with Sulfinpyrazone.
CiprofloxacinThe serum concentration of Ciprofloxacin can be increased when it is combined with Sulfinpyrazone.
CisplatinThe serum concentration of Cisplatin can be increased when it is combined with Sulfinpyrazone.
CitalopramThe serum concentration of Citalopram can be increased when it is combined with Sulfinpyrazone.
ClarithromycinThe metabolism of Sulfinpyrazone can be decreased when combined with Clarithromycin.
ClarithromycinThe serum concentration of Clarithromycin can be increased when it is combined with Sulfinpyrazone.
ClemastineThe metabolism of Sulfinpyrazone can be decreased when combined with Clemastine.
ClobazamThe serum concentration of Clobazam can be increased when it is combined with Sulfinpyrazone.
ClomifeneThe serum concentration of Clomifene can be increased when it is combined with Sulfinpyrazone.
ClonidineThe serum concentration of Clonidine can be increased when it is combined with Sulfinpyrazone.
ClopidogrelThe serum concentration of Clopidogrel can be increased when it is combined with Sulfinpyrazone.
ClopidogrelThe metabolism of Sulfinpyrazone can be decreased when combined with Clopidogrel.
ClotrimazoleThe metabolism of Sulfinpyrazone can be decreased when combined with Clotrimazole.
ClozapineThe serum concentration of Clozapine can be increased when it is combined with Sulfinpyrazone.
CobicistatThe metabolism of Sulfinpyrazone can be decreased when combined with Cobicistat.
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Sulfinpyrazone.
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Sulfinpyrazone.
ConivaptanThe serum concentration of Sulfinpyrazone can be increased when it is combined with Conivaptan.
Conjugated Equine EstrogensThe serum concentration of Conjugated Equine Estrogens can be increased when it is combined with Sulfinpyrazone.
CrizotinibThe metabolism of Sulfinpyrazone can be decreased when combined with Crizotinib.
CrizotinibThe serum concentration of Crizotinib can be increased when it is combined with Sulfinpyrazone.
CyclosporineThe serum concentration of Cyclosporine can be decreased when it is combined with Sulfinpyrazone.
CyclosporineThe metabolism of Sulfinpyrazone can be decreased when combined with Cyclosporine.
Dabigatran etexilateSulfinpyrazone may increase the anticoagulant activities of Dabigatran etexilate.
DabrafenibThe serum concentration of Sulfinpyrazone can be decreased when it is combined with Dabrafenib.
DabrafenibThe serum concentration of Dabrafenib can be increased when it is combined with Sulfinpyrazone.
DactinomycinThe serum concentration of Dactinomycin can be increased when it is combined with Sulfinpyrazone.
DapagliflozinThe serum concentration of Dapagliflozin can be increased when it is combined with Sulfinpyrazone.
DarunavirThe metabolism of Sulfinpyrazone can be decreased when combined with Darunavir.
DasatinibThe serum concentration of Sulfinpyrazone can be increased when it is combined with Dasatinib.
DaunorubicinThe serum concentration of Daunorubicin can be increased when it is combined with Sulfinpyrazone.
DebrisoquinThe serum concentration of Debrisoquin can be increased when it is combined with Sulfinpyrazone.
DeferasiroxThe serum concentration of Sulfinpyrazone can be decreased when it is combined with Deferasirox.
DelavirdineThe metabolism of Sulfinpyrazone can be decreased when combined with Delavirdine.
DexamethasoneThe serum concentration of Sulfinpyrazone can be decreased when it is combined with Dexamethasone.
DexamethasoneThe serum concentration of Dexamethasone can be increased when it is combined with Sulfinpyrazone.
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Sulfinpyrazone.
DicoumarolThe metabolism of Dicoumarol can be decreased when combined with Sulfinpyrazone.
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be increased when it is combined with Sulfinpyrazone.
DigitoxinThe serum concentration of Digitoxin can be increased when it is combined with Sulfinpyrazone.
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Sulfinpyrazone.
DihydroergotamineThe metabolism of Sulfinpyrazone can be decreased when combined with Dihydroergotamine.
DihydrotestosteroneThe serum concentration of Dihydrotestosterone can be increased when it is combined with Sulfinpyrazone.
DiltiazemThe metabolism of Sulfinpyrazone can be decreased when combined with Diltiazem.
DiltiazemThe serum concentration of Diltiazem can be increased when it is combined with Sulfinpyrazone.
DipyridamoleThe serum concentration of Dipyridamole can be increased when it is combined with Sulfinpyrazone.
DocetaxelThe serum concentration of Docetaxel can be increased when it is combined with Sulfinpyrazone.
DomperidoneThe serum concentration of Domperidone can be increased when it is combined with Sulfinpyrazone.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Sulfinpyrazone.
DoxycyclineThe metabolism of Sulfinpyrazone can be decreased when combined with Doxycycline.
DronedaroneThe metabolism of Sulfinpyrazone can be decreased when combined with Dronedarone.
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Sulfinpyrazone.
EfavirenzThe serum concentration of Sulfinpyrazone can be decreased when it is combined with Efavirenz.
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Sulfinpyrazone.
EnzalutamideThe serum concentration of Sulfinpyrazone can be decreased when it is combined with Enzalutamide.
EpinastineThe serum concentration of Epinastine can be increased when it is combined with Sulfinpyrazone.
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Sulfinpyrazone.
ErythromycinThe metabolism of Sulfinpyrazone can be decreased when combined with Erythromycin.
ErythromycinThe serum concentration of Erythromycin can be increased when it is combined with Sulfinpyrazone.
Eslicarbazepine acetateThe serum concentration of Sulfinpyrazone can be decreased when it is combined with Eslicarbazepine acetate.
EstradiolThe serum concentration of Estradiol can be increased when it is combined with Sulfinpyrazone.
EstriolThe serum concentration of Estriol can be increased when it is combined with Sulfinpyrazone.
EstroneThe serum concentration of Estrone can be increased when it is combined with Sulfinpyrazone.
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be increased when it is combined with Sulfinpyrazone.
Ethyl biscoumacetateThe metabolism of Ethyl biscoumacetate can be decreased when combined with Sulfinpyrazone.
EtoposideThe serum concentration of Etoposide can be increased when it is combined with Sulfinpyrazone.
EtravirineThe serum concentration of Sulfinpyrazone can be decreased when it is combined with Etravirine.
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Sulfinpyrazone.
EzetimibeThe serum concentration of Ezetimibe can be increased when it is combined with Sulfinpyrazone.
FelodipineThe metabolism of Sulfinpyrazone can be decreased when combined with Felodipine.
FesoterodineThe serum concentration of Fesoterodine can be increased when it is combined with Sulfinpyrazone.
FexofenadineThe serum concentration of Fexofenadine can be increased when it is combined with Sulfinpyrazone.
FidaxomicinThe serum concentration of Fidaxomicin can be increased when it is combined with Sulfinpyrazone.
FloxuridineThe metabolism of Sulfinpyrazone can be decreased when combined with Floxuridine.
FluconazoleThe metabolism of Sulfinpyrazone can be decreased when combined with Fluconazole.
FluorouracilThe metabolism of Sulfinpyrazone can be decreased when combined with Fluorouracil.
Fluticasone furoateThe serum concentration of Fluticasone furoate can be increased when it is combined with Sulfinpyrazone.
FluvastatinThe metabolism of Sulfinpyrazone can be decreased when combined with Fluvastatin.
FluvoxamineThe metabolism of Sulfinpyrazone can be decreased when combined with Fluvoxamine.
FosamprenavirThe metabolism of Sulfinpyrazone can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Sulfinpyrazone can be increased when it is combined with Fosaprepitant.
FosphenytoinThe metabolism of Sulfinpyrazone can be increased when combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Sulfinpyrazone can be increased when it is combined with Fusidic Acid.
GefitinibThe serum concentration of Gefitinib can be increased when it is combined with Sulfinpyrazone.
GemcitabineThe serum concentration of Gemcitabine can be increased when it is combined with Sulfinpyrazone.
GemfibrozilThe metabolism of Sulfinpyrazone can be decreased when combined with Gemfibrozil.
GrazoprevirThe serum concentration of Grazoprevir can be increased when it is combined with Sulfinpyrazone.
GrepafloxacinThe serum concentration of Grepafloxacin can be increased when it is combined with Sulfinpyrazone.
HaloperidolThe serum concentration of Haloperidol can be increased when it is combined with Sulfinpyrazone.
HydrocortisoneThe serum concentration of Hydrocortisone can be increased when it is combined with Sulfinpyrazone.
IbuprofenThe serum concentration of Ibuprofen can be increased when it is combined with Sulfinpyrazone.
IdelalisibThe serum concentration of Sulfinpyrazone can be increased when it is combined with Idelalisib.
ImatinibThe metabolism of Sulfinpyrazone can be decreased when combined with Imatinib.
ImatinibThe serum concentration of Imatinib can be increased when it is combined with Sulfinpyrazone.
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Sulfinpyrazone.
IndacaterolThe serum concentration of Indacaterol can be increased when it is combined with Sulfinpyrazone.
IndinavirThe serum concentration of Indinavir can be increased when it is combined with Sulfinpyrazone.
IndinavirThe metabolism of Sulfinpyrazone can be decreased when combined with Indinavir.
IndomethacinThe serum concentration of Indomethacin can be increased when it is combined with Sulfinpyrazone.
IrbesartanThe metabolism of Sulfinpyrazone can be decreased when combined with Irbesartan.
IrinotecanThe serum concentration of Irinotecan can be increased when it is combined with Sulfinpyrazone.
IsavuconazoniumThe metabolism of Sulfinpyrazone can be decreased when combined with Isavuconazonium.
IsradipineThe metabolism of Sulfinpyrazone can be decreased when combined with Isradipine.
ItraconazoleThe metabolism of Sulfinpyrazone can be decreased when combined with Itraconazole.
IvacaftorThe serum concentration of Sulfinpyrazone can be increased when it is combined with Ivacaftor.
IvermectinThe serum concentration of Ivermectin can be increased when it is combined with Sulfinpyrazone.
KetazolamThe serum concentration of Ketazolam can be increased when it is combined with Sulfinpyrazone.
KetoconazoleThe serum concentration of Ketoconazole can be increased when it is combined with Sulfinpyrazone.
KetoconazoleThe metabolism of Sulfinpyrazone can be decreased when combined with Ketoconazole.
LamivudineThe serum concentration of Lamivudine can be increased when it is combined with Sulfinpyrazone.
LamotrigineThe serum concentration of Lamotrigine can be increased when it is combined with Sulfinpyrazone.
LansoprazoleThe serum concentration of Lansoprazole can be increased when it is combined with Sulfinpyrazone.
LapatinibThe metabolism of Sulfinpyrazone can be decreased when combined with Lapatinib.
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Sulfinpyrazone.
LeflunomideThe metabolism of Sulfinpyrazone can be decreased when combined with Leflunomide.
LenalidomideThe serum concentration of Lenalidomide can be increased when it is combined with Sulfinpyrazone.
LenvatinibThe serum concentration of Lenvatinib can be increased when it is combined with Sulfinpyrazone.
LevetiracetamThe serum concentration of Levetiracetam can be increased when it is combined with Sulfinpyrazone.
LevofloxacinThe serum concentration of Levofloxacin can be increased when it is combined with Sulfinpyrazone.
LevomilnacipranThe serum concentration of Levomilnacipran can be increased when it is combined with Sulfinpyrazone.
LinagliptinThe serum concentration of Linagliptin can be increased when it is combined with Sulfinpyrazone.
LoperamideThe serum concentration of Loperamide can be increased when it is combined with Sulfinpyrazone.
LopinavirThe metabolism of Sulfinpyrazone can be decreased when combined with Lopinavir.
LosartanThe serum concentration of Losartan can be increased when it is combined with Sulfinpyrazone.
LosartanThe metabolism of Sulfinpyrazone can be decreased when combined with Losartan.
LovastatinThe metabolism of Sulfinpyrazone can be decreased when combined with Lovastatin.
LuliconazoleThe serum concentration of Sulfinpyrazone can be increased when it is combined with Luliconazole.
LumacaftorThe serum concentration of Sulfinpyrazone can be decreased when it is combined with Lumacaftor.
MannitolThe serum concentration of Mannitol can be increased when it is combined with Sulfinpyrazone.
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Sulfinpyrazone.
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Sulfinpyrazone.
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Sulfinpyrazone.
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Sulfinpyrazone.
MifepristoneThe metabolism of Sulfinpyrazone can be decreased when combined with Mifepristone.
MirabegronThe serum concentration of Mirabegron can be increased when it is combined with Sulfinpyrazone.
MitotaneThe serum concentration of Sulfinpyrazone can be decreased when it is combined with Mitotane.
MitoxantroneThe serum concentration of Mitoxantrone can be increased when it is combined with Sulfinpyrazone.
ModafinilThe serum concentration of Sulfinpyrazone can be decreased when it is combined with Modafinil.
MorphineThe serum concentration of Morphine can be increased when it is combined with Sulfinpyrazone.
Mycophenolate mofetilThe serum concentration of Mycophenolate mofetil can be increased when it is combined with Sulfinpyrazone.
NadololThe serum concentration of Nadolol can be increased when it is combined with Sulfinpyrazone.
NafcillinThe serum concentration of Sulfinpyrazone can be decreased when it is combined with Nafcillin.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Sulfinpyrazone.
NaloxoneThe serum concentration of Naloxone can be increased when it is combined with Sulfinpyrazone.
NefazodoneThe metabolism of Sulfinpyrazone can be decreased when combined with Nefazodone.
NelfinavirThe metabolism of Sulfinpyrazone can be decreased when combined with Nelfinavir.
NelfinavirThe serum concentration of Nelfinavir can be increased when it is combined with Sulfinpyrazone.
NetupitantThe serum concentration of Sulfinpyrazone can be increased when it is combined with Netupitant.
NevirapineThe metabolism of Sulfinpyrazone can be decreased when combined with Nevirapine.
NicardipineThe serum concentration of Nicardipine can be increased when it is combined with Sulfinpyrazone.
NicardipineThe metabolism of Sulfinpyrazone can be decreased when combined with Nicardipine.
NifedipineThe serum concentration of Nifedipine can be increased when it is combined with Sulfinpyrazone.
NilotinibThe metabolism of Sulfinpyrazone can be decreased when combined with Nilotinib.
NilotinibThe serum concentration of Nilotinib can be increased when it is combined with Sulfinpyrazone.
NintedanibThe serum concentration of Nintedanib can be decreased when it is combined with Sulfinpyrazone.
NizatidineThe serum concentration of Nizatidine can be increased when it is combined with Sulfinpyrazone.
OlanzapineThe serum concentration of Olanzapine can be increased when it is combined with Sulfinpyrazone.
OlaparibThe metabolism of Sulfinpyrazone can be decreased when combined with Olaparib.
OmbitasvirThe serum concentration of Ombitasvir can be increased when it is combined with Sulfinpyrazone.
OmeprazoleThe metabolism of Sulfinpyrazone can be decreased when combined with Omeprazole.
OsimertinibThe serum concentration of Sulfinpyrazone can be increased when it is combined with Osimertinib.
PaclitaxelThe serum concentration of Paclitaxel can be increased when it is combined with Sulfinpyrazone.
PalbociclibThe serum concentration of Sulfinpyrazone can be increased when it is combined with Palbociclib.
PanobinostatThe serum concentration of Panobinostat can be increased when it is combined with Sulfinpyrazone.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Sulfinpyrazone.
PentobarbitalThe metabolism of Sulfinpyrazone can be increased when combined with Pentobarbital.
PhenindioneThe metabolism of Phenindione can be decreased when combined with Sulfinpyrazone.
PhenobarbitalThe metabolism of Sulfinpyrazone can be increased when combined with Phenobarbital.
PhenobarbitalThe serum concentration of Phenobarbital can be increased when it is combined with Sulfinpyrazone.
PhenprocoumonThe metabolism of Phenprocoumon can be decreased when combined with Sulfinpyrazone.
PhenytoinThe metabolism of Sulfinpyrazone can be increased when combined with Phenytoin.
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Sulfinpyrazone.
PioglitazoneThe metabolism of Sulfinpyrazone can be decreased when combined with Pioglitazone.
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Sulfinpyrazone.
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Sulfinpyrazone.
PonatinibThe serum concentration of Ponatinib can be increased when it is combined with Sulfinpyrazone.
PosaconazoleThe metabolism of Sulfinpyrazone can be decreased when combined with Posaconazole.
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Sulfinpyrazone.
PrazosinThe serum concentration of Prazosin can be increased when it is combined with Sulfinpyrazone.
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Sulfinpyrazone.
PrednisoneThe serum concentration of Prednisone can be increased when it is combined with Sulfinpyrazone.
PrimidoneThe metabolism of Sulfinpyrazone can be increased when combined with Primidone.
ProgesteroneThe serum concentration of Progesterone can be increased when it is combined with Sulfinpyrazone.
PropranololThe serum concentration of Propranolol can be increased when it is combined with Sulfinpyrazone.
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Sulfinpyrazone.
PyrimethamineThe metabolism of Sulfinpyrazone can be decreased when combined with Pyrimethamine.
QuetiapineThe serum concentration of Quetiapine can be increased when it is combined with Sulfinpyrazone.
QuinidineThe serum concentration of Quinidine can be increased when it is combined with Sulfinpyrazone.
QuinineThe serum concentration of Quinine can be increased when it is combined with Sulfinpyrazone.
QuinineThe metabolism of Sulfinpyrazone can be decreased when combined with Quinine.
RabeprazoleThe metabolism of Sulfinpyrazone can be decreased when combined with Rabeprazole.
RanitidineThe serum concentration of Ranitidine can be increased when it is combined with Sulfinpyrazone.
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Sulfinpyrazone.
RanolazineThe metabolism of Sulfinpyrazone can be decreased when combined with Ranolazine.
ReserpineThe serum concentration of Reserpine can be increased when it is combined with Sulfinpyrazone.
RifabutinThe metabolism of Sulfinpyrazone can be increased when combined with Rifabutin.
RifampicinThe metabolism of Sulfinpyrazone can be increased when combined with Rifampicin.
RifampicinThe serum concentration of Rifampicin can be increased when it is combined with Sulfinpyrazone.
RifapentineThe metabolism of Sulfinpyrazone can be increased when combined with Rifapentine.
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Sulfinpyrazone.
RisperidoneThe serum concentration of Risperidone can be increased when it is combined with Sulfinpyrazone.
RitonavirThe metabolism of Sulfinpyrazone can be decreased when combined with Ritonavir.
RitonavirThe serum concentration of Ritonavir can be increased when it is combined with Sulfinpyrazone.
RivaroxabanThe serum concentration of Rivaroxaban can be increased when it is combined with Sulfinpyrazone.
RomidepsinThe serum concentration of Romidepsin can be increased when it is combined with Sulfinpyrazone.
RosiglitazoneThe metabolism of Sulfinpyrazone can be decreased when combined with Rosiglitazone.
Salicylic acidThe serum concentration of Salicylic acid can be increased when it is combined with Sulfinpyrazone.
SaquinavirThe metabolism of Sulfinpyrazone can be decreased when combined with Saquinavir.
SaquinavirThe serum concentration of Saquinavir can be increased when it is combined with Sulfinpyrazone.
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Sulfinpyrazone.
SecobarbitalThe metabolism of Sulfinpyrazone can be increased when combined with Secobarbital.
SelexipagThe serum concentration of Selexipag can be increased when it is combined with Sulfinpyrazone.
SildenafilThe metabolism of Sulfinpyrazone can be decreased when combined with Sildenafil.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Sulfinpyrazone.
SiltuximabThe serum concentration of Sulfinpyrazone can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Sulfinpyrazone can be increased when it is combined with Simeprevir.
SitagliptinThe serum concentration of Sitagliptin can be increased when it is combined with Sulfinpyrazone.
SofosbuvirThe serum concentration of Sofosbuvir can be increased when it is combined with Sulfinpyrazone.
SorafenibThe serum concentration of Sorafenib can be increased when it is combined with Sulfinpyrazone.
SorafenibThe metabolism of Sulfinpyrazone can be decreased when combined with Sorafenib.
SparfloxacinThe serum concentration of Sparfloxacin can be increased when it is combined with Sulfinpyrazone.
SphingosineThe serum concentration of Sphingosine can be increased when it is combined with Sulfinpyrazone.
St. John's WortThe serum concentration of Sulfinpyrazone can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Sulfinpyrazone can be increased when it is combined with Stiripentol.
SulfadiazineThe metabolism of Sulfinpyrazone can be decreased when combined with Sulfadiazine.
SulfamethoxazoleThe metabolism of Sulfinpyrazone can be decreased when combined with Sulfamethoxazole.
SulfisoxazoleThe metabolism of Sulfinpyrazone can be decreased when combined with Sulfisoxazole.
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Sulfinpyrazone.
TamoxifenThe serum concentration of Tamoxifen can be increased when it is combined with Sulfinpyrazone.
TamoxifenThe metabolism of Sulfinpyrazone can be decreased when combined with Tamoxifen.
Taurocholic AcidThe serum concentration of Taurocholic Acid can be increased when it is combined with Sulfinpyrazone.
Technetium Tc-99m sestamibiThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Sulfinpyrazone.
TelaprevirThe metabolism of Sulfinpyrazone can be decreased when combined with Telaprevir.
TelaprevirThe serum concentration of Telaprevir can be increased when it is combined with Sulfinpyrazone.
TelithromycinThe metabolism of Sulfinpyrazone can be decreased when combined with Telithromycin.
TemsirolimusThe serum concentration of Temsirolimus can be increased when it is combined with Sulfinpyrazone.
TeriflunomideThe metabolism of Sulfinpyrazone can be decreased when combined with Teriflunomide.
TicagrelorThe serum concentration of Ticagrelor can be increased when it is combined with Sulfinpyrazone.
TicagrelorThe metabolism of Sulfinpyrazone can be decreased when combined with Ticagrelor.
TiclopidineThe metabolism of Sulfinpyrazone can be decreased when combined with Ticlopidine.
TimololThe serum concentration of Timolol can be increased when it is combined with Sulfinpyrazone.
TocilizumabThe serum concentration of Sulfinpyrazone can be decreased when it is combined with Tocilizumab.
TolbutamideThe metabolism of Sulfinpyrazone can be decreased when combined with Tolbutamide.
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Sulfinpyrazone.
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Sulfinpyrazone.
ToremifeneThe serum concentration of Toremifene can be increased when it is combined with Sulfinpyrazone.
Trastuzumab emtansineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Sulfinpyrazone.
TrimethoprimThe metabolism of Sulfinpyrazone can be decreased when combined with Trimethoprim.
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Sulfinpyrazone.
UmeclidiniumThe serum concentration of Umeclidinium can be increased when it is combined with Sulfinpyrazone.
Valproic AcidThe metabolism of Sulfinpyrazone can be decreased when combined with Valproic Acid.
ValsartanThe metabolism of Sulfinpyrazone can be decreased when combined with Valsartan.
VecuroniumThe serum concentration of Vecuronium can be increased when it is combined with Sulfinpyrazone.
VenlafaxineThe metabolism of Sulfinpyrazone can be decreased when combined with Venlafaxine.
VenlafaxineThe serum concentration of Venlafaxine can be increased when it is combined with Sulfinpyrazone.
VerapamilThe metabolism of Sulfinpyrazone can be decreased when combined with Verapamil.
VerapamilThe serum concentration of Verapamil can be increased when it is combined with Sulfinpyrazone.
VinblastineThe serum concentration of Vinblastine can be increased when it is combined with Sulfinpyrazone.
VincristineThe serum concentration of Vincristine can be increased when it is combined with Sulfinpyrazone.
VismodegibThe serum concentration of Vismodegib can be increased when it is combined with Sulfinpyrazone.
VoriconazoleThe metabolism of Sulfinpyrazone can be decreased when combined with Voriconazole.
WarfarinThe metabolism of Warfarin can be decreased when combined with Sulfinpyrazone.
ZafirlukastThe metabolism of Sulfinpyrazone can be decreased when combined with Zafirlukast.
ZidovudineThe serum concentration of Zidovudine can be increased when it is combined with Sulfinpyrazone.
ZiprasidoneThe metabolism of Sulfinpyrazone can be decreased when combined with Ziprasidone.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Transporter activity
Specific Function:
Mediates export of organic anions and drugs from the cytoplasm. Mediates ATP-dependent transport of glutathione and glutathione conjugates, leukotriene C4, estradiol-17-beta-o-glucuronide, methotrexate, antiviral drugs and other xenobiotics. Confers resistance to anticancer drugs. Hydrolyzes ATP with low efficiency.
Gene Name:
ABCC1
Uniprot ID:
P33527
Molecular Weight:
171589.5 Da
References
  1. Evers R, de Haas M, Sparidans R, Beijnen J, Wielinga PR, Lankelma J, Borst P: Vinblastine and sulfinpyrazone export by the multidrug resistance protein MRP2 is associated with glutathione export. Br J Cancer. 2000 Aug;83(3):375-83. [PubMed:10917554 ]
  2. Morrow CS, Smitherman PK, Diah SK, Schneider E, Townsend AJ: Coordinated action of glutathione S-transferases (GSTs) and multidrug resistance protein 1 (MRP1) in antineoplastic drug detoxification. Mechanism of GST A1-1- and MRP1-associated resistance to chlorambucil in MCF7 breast carcinoma cells. J Biol Chem. 1998 Aug 7;273(32):20114-20. [PubMed:9685354 ]
  3. Bakos E, Evers R, Sinko E, Varadi A, Borst P, Sarkadi B: Interactions of the human multidrug resistance proteins MRP1 and MRP2 with organic anions. Mol Pharmacol. 2000 Apr;57(4):760-8. [PubMed:10727523 ]
  4. Depeille P, Cuq P, Mary S, Passagne I, Evrard A, Cupissol D, Vian L: Glutathione S-transferase M1 and multidrug resistance protein 1 act in synergy to protect melanoma cells from vincristine effects. Mol Pharmacol. 2004 Apr;65(4):897-905. [PubMed:15044619 ]
  5. Raggers RJ, van Helvoort A, Evers R, van Meer G: The human multidrug resistance protein MRP1 translocates sphingolipid analogs across the plasma membrane. J Cell Sci. 1999 Feb;112 ( Pt 3):415-22. [PubMed:9885294 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
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. Bakos E, Evers R, Sinko E, Varadi A, Borst P, Sarkadi B: Interactions of the human multidrug resistance proteins MRP1 and MRP2 with organic anions. Mol Pharmacol. 2000 Apr;57(4):760-8. [PubMed:10727523 ]
  2. Evers R, de Haas M, Sparidans R, Beijnen J, Wielinga PR, Lankelma J, Borst P: Vinblastine and sulfinpyrazone export by the multidrug resistance protein MRP2 is associated with glutathione export. Br J Cancer. 2000 Aug;83(3):375-83. [PubMed:10917554 ]
  3. Morrow CS, Smitherman PK, Townsend AJ: Role of multidrug-resistance protein 2 in glutathione S-transferase P1-1-mediated resistance to 4-nitroquinoline 1-oxide toxicities in HepG2 cells. Mol Carcinog. 2000 Nov;29(3):170-8. [PubMed:11108662 ]
  4. Ito K, Oleschuk CJ, Westlake C, Vasa MZ, Deeley RG, Cole SP: Mutation of Trp1254 in the multispecific organic anion transporter, multidrug resistance protein 2 (MRP2) (ABCC2), alters substrate specificity and results in loss of methotrexate transport activity. J Biol Chem. 2001 Oct 12;276(41):38108-14. Epub 2001 Aug 10. [PubMed:11500505 ]
  5. Flanagan SD, Cummins CL, Susanto M, Liu X, Takahashi LH, Benet LZ: Comparison of furosemide and vinblastine secretion from cell lines overexpressing multidrug resistance protein (P-glycoprotein) and multidrug resistance-associated proteins (MRP1 and MRP2). Pharmacology. 2002;64(3):126-34. [PubMed:11834888 ]
  6. Hagos Y, Stein D, Ugele B, Burckhardt G, Bahn A: Human renal organic anion transporter 4 operates as an asymmetric urate transporter. J Am Soc Nephrol. 2007 Feb;18(2):430-9. Epub 2007 Jan 17. [PubMed:17229912 ]

Enzymes

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. 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. 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 ]
  2. 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
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. 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 ]
  2. 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
substrate
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. 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 ]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
no
General Function:
Transporter activity
Specific Function:
FABP are thought to play a role in the intracellular transport of long-chain fatty acids and their acyl-CoA esters. FABP2 is probably involved in triglyceride-rich lipoprotein synthesis. Binds saturated long-chain fatty acids with a high affinity, but binds with a lower affinity to unsaturated long-chain fatty acids. FABP2 may also help maintain energy homeostasis by functioning as a lipid sensor.
Gene Name:
FABP2
Uniprot ID:
P12104
Molecular Weight:
15207.165 Da
References
  1. Rowland A, Knights KM, Mackenzie PI, Miners JO: Characterization of the binding of drugs to human intestinal fatty acid binding protein (IFABP): potential role of IFABP as an alternative to albumin for in vitro-in vivo extrapolation of drug kinetic parameters. Drug Metab Dispos. 2009 Jul;37(7):1395-403. doi: 10.1124/dmd.109.027656. Epub 2009 Apr 27. [PubMed:19398502 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Organic anion transmembrane transporter activity
Specific Function:
May act as an inducible transporter in the biliary and intestinal excretion of organic anions. Acts as an alternative route for the export of bile acids and glucuronides from cholestatic hepatocytes (By similarity).
Gene Name:
ABCC3
Uniprot ID:
O15438
Molecular Weight:
169341.14 Da
References
  1. Zelcer N, Saeki T, Reid G, Beijnen JH, Borst P: Characterization of drug transport by the human multidrug resistance protein 3 (ABCC3). J Biol Chem. 2001 Dec 7;276(49):46400-7. [PubMed:11581266 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Atpase activity, coupled to transmembrane movement of substances
Specific Function:
May be an organic anion pump relevant to cellular detoxification.
Gene Name:
ABCC4
Uniprot ID:
O15439
Molecular Weight:
149525.33 Da
References
  1. Chen ZS, Lee K, Walther S, Raftogianis RB, Kuwano M, Zeng H, Kruh GD: Analysis of methotrexate and folate transport by multidrug resistance protein 4 (ABCC4): MRP4 is a component of the methotrexate efflux system. Cancer Res. 2002 Jun 1;62(11):3144-50. [PubMed:12036927 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Organic anion transmembrane transporter activity
Specific Function:
Acts as a multispecific organic anion pump which can transport nucleotide analogs.
Gene Name:
ABCC5
Uniprot ID:
O15440
Molecular Weight:
160658.8 Da
References
  1. Wijnholds J, Mol CA, van Deemter L, de Haas M, Scheffer GL, Baas F, Beijnen JH, Scheper RJ, Hatse S, De Clercq E, Balzarini J, Borst P: Multidrug-resistance protein 5 is a multispecific organic anion transporter able to transport nucleotide analogs. Proc Natl Acad Sci U S A. 2000 Jun 20;97(13):7476-81. [PubMed:10840050 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Transporter activity
Specific Function:
Isoform 1: May participate directly in the active transport of drugs into subcellular organelles or influence drug distribution indirectly. Transports glutathione conjugates as leukotriene-c4 (LTC4) and N-ethylmaleimide S-glutathione (NEM-GS).Isoform 2: Inhibits TNF-alpha-mediated apoptosis through blocking one or more caspases.
Gene Name:
ABCC6
Uniprot ID:
O95255
Molecular Weight:
164904.81 Da
References
  1. Chen ZS, Hopper-Borge E, Belinsky MG, Shchaveleva I, Kotova E, Kruh GD: Characterization of the transport properties of human multidrug resistance protein 7 (MRP7, ABCC10). Mol Pharmacol. 2003 Feb;63(2):351-8. [PubMed:12527806 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
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. Honda Y, Ushigome F, Koyabu N, Morimoto S, Shoyama Y, Uchiumi T, Kuwano M, Ohtani H, Sawada Y: Effects of grapefruit juice and orange juice components on P-glycoprotein- and MRP2-mediated drug efflux. Br J Pharmacol. 2004 Dec;143(7):856-64. Epub 2004 Oct 25. [PubMed:15504753 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Transporter activity
Specific Function:
Mediates export of organic anions and drugs from the cytoplasm. Mediates ATP-dependent transport of glutathione and glutathione conjugates, leukotriene C4, estradiol-17-beta-o-glucuronide, methotrexate, antiviral drugs and other xenobiotics. Confers resistance to anticancer drugs. Hydrolyzes ATP with low efficiency.
Gene Name:
ABCC1
Uniprot ID:
P33527
Molecular Weight:
171589.5 Da
References
  1. Evers R, de Haas M, Sparidans R, Beijnen J, Wielinga PR, Lankelma J, Borst P: Vinblastine and sulfinpyrazone export by the multidrug resistance protein MRP2 is associated with glutathione export. Br J Cancer. 2000 Aug;83(3):375-83. [PubMed:10917554 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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. Flanagan SD, Cummins CL, Susanto M, Liu X, Takahashi LH, Benet LZ: Comparison of furosemide and vinblastine secretion from cell lines overexpressing multidrug resistance protein (P-glycoprotein) and multidrug resistance-associated proteins (MRP1 and MRP2). Pharmacology. 2002;64(3):126-34. [PubMed:11834888 ]
  2. Evers R, de Haas M, Sparidans R, Beijnen J, Wielinga PR, Lankelma J, Borst P: Vinblastine and sulfinpyrazone export by the multidrug resistance protein MRP2 is associated with glutathione export. Br J Cancer. 2000 Aug;83(3):375-83. [PubMed:10917554 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23