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Identification
NameToremifene
Accession NumberDB00539  (APRD00391)
TypeSmall Molecule
GroupsApproved, Investigational
DescriptionA first generation nonsteroidal selective estrogen receptor modulator (SERM) that is structurally related to tamoxifen. Like tamoxifen, it is an estrogen agonist for bone tissue and cholesterol metabolism but is antagonistic on mammary and uterine tissue. [PubChem]
Structure
Thumb
Synonyms
Toremifeno
Toremifenum
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Farestontablet60 mg/1oralG Tx, Inc.1997-06-30Not applicableUs
Farestontablet60 mg/1oralPro Strakan, Inc.1997-06-30Not applicableUs
FarestonTablets60 mgOral useOrion Corporation1996-02-14Not applicableEu
FarestonTablets60 mgOral useOrion Corporation1996-02-14Not applicableEu
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
AcapodeneNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Toremifene citrate
ThumbNot applicableDBSALT001447
Categories
UNII7NFE54O27T
CAS number89778-26-7
WeightAverage: 405.96
Monoisotopic: 405.18594223
Chemical FormulaC26H28ClNO
InChI KeyInChIKey=XFCLJVABOIYOMF-QPLCGJKRSA-N
InChI
InChI=1S/C26H28ClNO/c1-28(2)19-20-29-24-15-13-23(14-16-24)26(22-11-7-4-8-12-22)25(17-18-27)21-9-5-3-6-10-21/h3-16H,17-20H2,1-2H3/b26-25-
IUPAC Name
(2-{4-[(1Z)-4-chloro-1,2-diphenylbut-1-en-1-yl]phenoxy}ethyl)dimethylamine
SMILES
CN(C)CCOC1=CC=C(C=C1)C(=C(\CCCl)C1=CC=CC=C1)\C1=CC=CC=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as stilbenes. These are organic compounds containing a 1,2-diphenylethylene moiety. Stilbenes (C6-C2-C6 ) are derived from the common phenylpropene (C6-C3) skeleton building block. The introduction of one or more hydroxyl groups to a phenyl ring lead to stilbenoids.
KingdomOrganic compounds
Super ClassPhenylpropanoids and polyketides
ClassStilbenes
Sub ClassNot Available
Direct ParentStilbenes
Alternative Parents
Substituents
  • Stilbene
  • Diphenylmethane
  • Phenylpropene
  • Phenol ether
  • Alkyl aryl ether
  • Benzenoid
  • Monocyclic benzene moiety
  • Tertiary aliphatic amine
  • Tertiary amine
  • Ether
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Amine
  • Alkyl halide
  • Alkyl chloride
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of metastatic breast cancer in postmenopausal women with estrogen receptor-positive or receptor-unknown tumors. Toremifene is currently under investigation as a preventative agent for prostate cancer in men with high-grade prostatic intraepithelial neoplasia and no evidence of prostate cancer.
PharmacodynamicsToremifene is an antineoplastic hormonal agent primarily used in the treatment of advanced breast cancer. Toremifene is a nonsteroidal agent that has demonstrated potent antiestrogenic properties in animal test systems. The antiestrogenic effects may be related to its ability to compete with estrogen for binding sites in target tissues such as breast. Toremifene inhibits the induction of rat mammary carcinoma induced by dimethylbenzanthracene (DMBA) and causes the regression of already established DMBA-induced tumors. In this rat model, Toremifene appears to exert its antitumor effects by binding the estrogen receptors. In cytosols derived from human breast adenocarcinomas, Toremifene competes with estradiol for estrogen receptor protein.
Mechanism of actionToremifene is a nonsteroidal triphenylethylene derivative. Toremifene binds to estrogen receptors and may exert estrogenic, antiestrogenic, or both activities, depending upon the duration of treatment, animal species, gender, target organ, or endpoint selected. The antitumor effect of toremifene in breast cancer is believed to be mainly due to its antiestrogenic effects, in other words, its ability to compete with estrogen for binding sites in the cancer, blocking the growth-stimulating effects of estrogen in the tumor. Toremifene may also inhibit tumor growth through other mechanisms, such as induction of apoptosis, regulation of oncogene expression, and growth factors.
Related Articles
AbsorptionWell absorbed
Volume of distribution
  • 580 L
Protein bindingToremifen is primarily bound to albumin (92%), 2% bound to α1-acid glycoprotein, and 6% bound to β1-globulin in the serum.
Metabolism

Hepatic. Mainly by CYP3A4 to N-demethyltoremifene, which exhibits antiestrogenic effects but has weak antitumor potency in vivo.

SubstrateEnzymesProduct
Toremifene
N-desmethyltoremifeneDetails
Route of eliminationToremifene is extensively metabolized, principally by CYP3A4 to N-demethyltoremifene, which is also antiestrogenic but with weak in vivo antitumor potency.
Half life5 days
Clearance
  • 5 L/h
ToxicityNot Available
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+0.7488
Caco-2 permeable+0.8266
P-glycoprotein substrateSubstrate0.7067
P-glycoprotein inhibitor IInhibitor0.79
P-glycoprotein inhibitor IINon-inhibitor0.5917
Renal organic cation transporterInhibitor0.7552
CYP450 2C9 substrateNon-substrate0.7502
CYP450 2D6 substrateNon-substrate0.759
CYP450 3A4 substrateSubstrate0.7574
CYP450 1A2 substrateInhibitor0.8683
CYP450 2C9 inhibitorNon-inhibitor0.882
CYP450 2D6 inhibitorInhibitor0.7217
CYP450 2C19 inhibitorNon-inhibitor0.7443
CYP450 3A4 inhibitorNon-inhibitor0.8824
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.5128
Ames testNon AMES toxic0.7545
CarcinogenicityNon-carcinogens0.616
BiodegradationNot ready biodegradable0.9601
Rat acute toxicity2.3467 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Strong inhibitor0.7708
hERG inhibition (predictor II)Inhibitor0.5086
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Gtx inc
Packagers
Dosage forms
FormRouteStrength
Tabletoral60 mg/1
TabletsOral use60 mg
Prices
Unit descriptionCostUnit
Fareston 60 mg tablet11.84USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US4696949 No1992-09-292009-09-29Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point108-110 °CNot Available
logP6.8Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.000409 mg/mLALOGPS
logP5.65ALOGPS
logP6.27ChemAxon
logS-6ALOGPS
pKa (Strongest Basic)8.76ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area12.47 Å2ChemAxon
Rotatable Bond Count9ChemAxon
Refractivity133.41 m3·mol-1ChemAxon
Polarizability46.49 Å3ChemAxon
Number of Rings3ChemAxon
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 Reference

Reijo Toivola, Tuomas Huuhtanen, “Toremifene crystallization method.” U.S. Patent US20070093556, issued April 26, 2007.

US20070093556
General References
  1. Price N, Sartor O, Hutson T, Mariani S: Role of 5a-reductase inhibitors and selective estrogen receptor modulators as potential chemopreventive agents for prostate cancer. Clin Prostate Cancer. 2005 Mar;3(4):211-4. [PubMed:15882476 ]
  2. Taneja SS, Smith MR, Dalton JT, Raghow S, Barnette G, Steiner M, Veverka KA: Toremifene--a promising therapy for the prevention of prostate cancer and complications of androgen deprivation therapy. Expert Opin Investig Drugs. 2006 Mar;15(3):293-305. [PubMed:16503765 ]
  3. Thompson IM: Chemoprevention of prostate cancer: agents and study designs. J Urol. 2007 Sep;178(3 Pt 2):S9-S13. Epub 2007 Jul 20. [PubMed:17644117 ]
  4. Ariazi EA, Ariazi JL, Cordera F, Jordan VC: Estrogen receptors as therapeutic targets in breast cancer. Curr Top Med Chem. 2006;6(3):181-202. [PubMed:16515478 ]
  5. Musa MA, Khan MO, Cooperwood JS: Medicinal chemistry and emerging strategies applied to the development of selective estrogen receptor modulators (SERMs). Curr Med Chem. 2007;14(11):1249-61. [PubMed:17504144 ]
External Links
ATC CodesL02BA02
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Toremifene can be increased when it is combined with Abiraterone.
AcenocoumarolToremifene may increase the anticoagulant activities of Acenocoumarol.
AcetaminophenThe serum concentration of Toremifene can be increased when it is combined with Acetaminophen.
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Toremifene.
AfatinibThe serum concentration of Toremifene can be increased when it is combined with Afatinib.
AlbendazoleThe serum concentration of Toremifene can be increased when it is combined with Albendazole.
AldosteroneThe serum concentration of Toremifene can be decreased when it is combined with Aldosterone.
AlectinibThe serum concentration of Toremifene can be increased when it is combined with Alectinib.
AlfentanilThe serum concentration of Toremifene can be increased when it is combined with Alfentanil.
AlfuzosinAlfuzosin may increase the QTc-prolonging activities of Toremifene.
AmantadineThe serum concentration of Toremifene can be increased when it is combined with Amantadine.
Aminohippuric acidThe serum concentration of Toremifene can be increased when it is combined with Aminohippuric acid.
AmiodaroneThe risk or severity of adverse effects can be increased when Amiodarone is combined with Toremifene.
AmiodaroneToremifene may increase the QTc-prolonging activities of Amiodarone.
AmitriptylineThe serum concentration of Toremifene can be increased when it is combined with Amitriptyline.
AmlodipineThe serum concentration of Toremifene can be increased when it is combined with Amlodipine.
AmoxapineAmoxapine may increase the QTc-prolonging activities of Toremifene.
AmprenavirThe serum concentration of Toremifene can be decreased when it is combined with Amprenavir.
AmsacrineThe serum concentration of Toremifene can be increased when it is combined with Amsacrine.
AnagrelideAnagrelide may increase the QTc-prolonging activities of Toremifene.
ApomorphineApomorphine may increase the QTc-prolonging activities of Toremifene.
AprepitantThe serum concentration of Toremifene can be increased when it is combined with Aprepitant.
ArformoterolArformoterol may increase the QTc-prolonging activities of Toremifene.
AripiprazoleAripiprazole may increase the QTc-prolonging activities of Toremifene.
Arsenic trioxideToremifene may increase the QTc-prolonging activities of Arsenic trioxide.
ArtemetherToremifene may increase the QTc-prolonging activities of Artemether.
AsenapineToremifene may increase the QTc-prolonging activities of Asenapine.
AstemizoleThe serum concentration of Toremifene can be increased when it is combined with Astemizole.
AtazanavirThe risk or severity of adverse effects can be increased when Atazanavir is combined with Toremifene.
AtenololThe serum concentration of Toremifene can be increased when it is combined with Atenolol.
AtomoxetineThe metabolism of Toremifene can be decreased when combined with Atomoxetine.
AtorvastatinThe serum concentration of Toremifene can be increased when it is combined with Atorvastatin.
AzelastineThe serum concentration of Toremifene can be increased when it is combined with Azelastine.
AzithromycinAzithromycin may increase the QTc-prolonging activities of Toremifene.
BedaquilineBedaquiline may increase the QTc-prolonging activities of Toremifene.
BendroflumethiazideBendroflumethiazide may increase the hypercalcemic activities of Toremifene.
BenzocaineThe serum concentration of Toremifene can be increased when it is combined with Benzocaine.
BepridilThe serum concentration of Toremifene can be increased when it is combined with Bepridil.
BevacizumabBevacizumab may increase the cardiotoxic activities of Toremifene.
BexaroteneThe serum concentration of Toremifene can be decreased when it is combined with Bexarotene.
BiperidenThe serum concentration of Toremifene can be increased when it is combined with Biperiden.
BoceprevirThe risk or severity of adverse effects can be increased when Boceprevir is combined with Toremifene.
BortezomibThe metabolism of Toremifene can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Toremifene can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Toremifene can be increased when it is combined with Bosutinib.
BromocriptineThe serum concentration of Toremifene can be increased when it is combined with Bromocriptine.
BuprenorphineThe serum concentration of Toremifene can be increased when it is combined with Buprenorphine.
BuserelinBuserelin may increase the QTc-prolonging activities of Toremifene.
BuspironeThe serum concentration of Toremifene can be increased when it is combined with Buspirone.
CabazitaxelThe serum concentration of Toremifene can be increased when it is combined with Cabazitaxel.
CaffeineThe serum concentration of Toremifene can be increased when it is combined with Caffeine.
CanagliflozinThe serum concentration of Toremifene can be increased when it is combined with Canagliflozin.
CandesartanThe serum concentration of Toremifene can be increased when it is combined with Candesartan.
CaptoprilThe serum concentration of Toremifene can be increased when it is combined with Captopril.
CarbamazepineThe serum concentration of Toremifene can be decreased when it is combined with Carbamazepine.
CarvedilolThe serum concentration of Toremifene can be increased when it is combined with Carvedilol.
CaspofunginThe serum concentration of Toremifene can be increased when it is combined with Caspofungin.
CeritinibThe risk or severity of adverse effects can be increased when Ceritinib is combined with Toremifene.
ChloroquineChloroquine may increase the QTc-prolonging activities of Toremifene.
ChlorothiazideChlorothiazide may increase the hypercalcemic activities of Toremifene.
ChlorpromazineChlorpromazine may increase the QTc-prolonging activities of Toremifene.
ChlorpropamideThe serum concentration of Toremifene can be increased when it is combined with Chlorpropamide.
ChlorprothixeneThe serum concentration of Toremifene can be increased when it is combined with Chlorprothixene.
ChlorthalidoneChlorthalidone may increase the hypercalcemic activities of Toremifene.
CholesterolThe serum concentration of Toremifene can be increased when it is combined with Cholesterol.
Cholic AcidThe serum concentration of Toremifene can be decreased when it is combined with Cholic Acid.
CilazaprilThe serum concentration of Toremifene can be increased when it is combined with Cilazapril.
CimetidineThe serum concentration of Toremifene can be decreased when it is combined with Cimetidine.
CiprofloxacinCiprofloxacin may increase the QTc-prolonging activities of Toremifene.
CisaprideToremifene may increase the QTc-prolonging activities of Cisapride.
CitalopramCitalopram may increase the QTc-prolonging activities of Toremifene.
ClarithromycinThe risk or severity of adverse effects can be increased when Clarithromycin is combined with Toremifene.
ClemastineThe metabolism of Toremifene can be decreased when combined with Clemastine.
ClofazimineThe serum concentration of Toremifene can be increased when it is combined with Clofazimine.
ClomipramineThe serum concentration of Toremifene can be increased when it is combined with Clomipramine.
ClotrimazoleThe metabolism of Toremifene can be decreased when combined with Clotrimazole.
ClozapineClozapine may increase the QTc-prolonging activities of Toremifene.
CobicistatThe risk or severity of adverse effects can be increased when Cobicistat is combined with Toremifene.
ColchicineThe serum concentration of Toremifene can be increased when it is combined with Colchicine.
ColforsinThe serum concentration of Toremifene can be increased when it is combined with Colforsin.
ConivaptanThe serum concentration of Toremifene can be increased when it is combined with Conivaptan.
CrizotinibCrizotinib may increase the QTc-prolonging activities of Toremifene.
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Toremifene.
CyclosporineThe metabolism of Toremifene can be decreased when combined with Cyclosporine.
Cyproterone acetateThe serum concentration of Toremifene can be decreased when it is combined with Cyproterone acetate.
DabrafenibThe serum concentration of Toremifene can be decreased when it is combined with Dabrafenib.
DaclatasvirThe serum concentration of Toremifene can be increased when it is combined with Daclatasvir.
DactinomycinThe serum concentration of Toremifene can be increased when it is combined with Dactinomycin.
DarunavirThe risk or severity of adverse effects can be increased when Darunavir is combined with Toremifene.
DasatinibThe serum concentration of Toremifene can be increased when it is combined with Dasatinib.
DaunorubicinThe serum concentration of Toremifene can be decreased when it is combined with Daunorubicin.
DeferasiroxThe serum concentration of Toremifene can be decreased when it is combined with Deferasirox.
DegarelixDegarelix may increase the QTc-prolonging activities of Toremifene.
DelavirdineThe metabolism of Toremifene can be decreased when combined with Delavirdine.
DesfluraneDesflurane may increase the QTc-prolonging activities of Toremifene.
DesipramineThe serum concentration of Toremifene can be increased when it is combined with Desipramine.
DeslanosideDeslanoside may decrease the cardiotoxic activities of Toremifene.
DesloratadineThe serum concentration of Toremifene can be increased when it is combined with Desloratadine.
DexamethasoneThe serum concentration of Toremifene can be decreased when it is combined with Dexamethasone.
DextromethorphanThe serum concentration of Toremifene can be increased when it is combined with Dextromethorphan.
DiclofenacThe serum concentration of Toremifene can be increased when it is combined with Diclofenac.
DicoumarolToremifene may increase the anticoagulant activities of Dicoumarol.
DigitoxinDigitoxin may decrease the cardiotoxic activities of Toremifene.
DigoxinDigoxin may decrease the cardiotoxic activities of Toremifene.
DihydroergotamineThe metabolism of Toremifene can be decreased when combined with Dihydroergotamine.
DiltiazemThe metabolism of Toremifene can be decreased when combined with Diltiazem.
DiphenhydramineDiphenhydramine may increase the QTc-prolonging activities of Toremifene.
DipyridamoleThe serum concentration of Toremifene can be increased when it is combined with Dipyridamole.
DisopyramideDisopyramide may increase the QTc-prolonging activities of Toremifene.
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Toremifene.
DofetilideDofetilide may increase the QTc-prolonging activities of Toremifene.
DolasetronDolasetron may increase the QTc-prolonging activities of Toremifene.
DomperidoneToremifene may increase the QTc-prolonging activities of Domperidone.
DoxazosinThe serum concentration of Toremifene can be increased when it is combined with Doxazosin.
DoxepinThe serum concentration of Toremifene can be increased when it is combined with Doxepin.
DoxorubicinThe serum concentration of Toremifene can be decreased when it is combined with Doxorubicin.
DoxycyclineThe metabolism of Toremifene can be decreased when combined with Doxycycline.
DronabinolThe serum concentration of Toremifene can be increased when it is combined with Dronabinol.
DronedaroneToremifene may increase the QTc-prolonging activities of Dronedarone.
DroperidolDroperidol may increase the QTc-prolonging activities of Toremifene.
EfavirenzThe serum concentration of Toremifene can be decreased when it is combined with Efavirenz.
ElbasvirThe serum concentration of Toremifene can be increased when it is combined with Elbasvir.
EliglustatToremifene may increase the QTc-prolonging activities of Eliglustat.
EnalaprilThe serum concentration of Toremifene can be increased when it is combined with Enalapril.
EnzalutamideThe serum concentration of Toremifene can be decreased when it is combined with Enzalutamide.
ErgonovineThe serum concentration of Toremifene can be increased when it is combined with Ergonovine.
ErgotamineThe serum concentration of Toremifene can be increased when it is combined with Ergotamine.
EribulinEribulin may increase the QTc-prolonging activities of Toremifene.
ErythromycinErythromycin may increase the QTc-prolonging activities of Toremifene.
EscitalopramToremifene may increase the QTc-prolonging activities of Escitalopram.
Eslicarbazepine acetateThe serum concentration of Toremifene can be decreased when it is combined with Eslicarbazepine acetate.
EstramustineThe serum concentration of Toremifene can be increased when it is combined with Estramustine.
EstriolThe serum concentration of Toremifene can be decreased when it is combined with Estriol.
EstroneThe serum concentration of Toremifene can be decreased when it is combined with Estrone.
Ethyl biscoumacetateToremifene may increase the anticoagulant activities of Ethyl biscoumacetate.
EtoposideThe serum concentration of Toremifene can be increased when it is combined with Etoposide.
EtravirineThe serum concentration of Toremifene can be decreased when it is combined with Etravirine.
EzogabineEzogabine may increase the QTc-prolonging activities of Toremifene.
FamotidineFamotidine may increase the QTc-prolonging activities of Toremifene.
FelbamateFelbamate may increase the QTc-prolonging activities of Toremifene.
FelodipineThe serum concentration of Toremifene can be increased when it is combined with Felodipine.
FentanylThe serum concentration of Toremifene can be increased when it is combined with Fentanyl.
FexofenadineThe serum concentration of Toremifene can be increased when it is combined with Fexofenadine.
FidaxomicinThe serum concentration of Toremifene can be increased when it is combined with Fidaxomicin.
FingolimodFingolimod may increase the QTc-prolonging activities of Toremifene.
FlecainideFlecainide may increase the QTc-prolonging activities of Toremifene.
FluconazoleThe metabolism of Toremifene can be decreased when combined with Fluconazole.
FluoxetineFluoxetine may increase the QTc-prolonging activities of Toremifene.
FlupentixolToremifene may increase the QTc-prolonging activities of Flupentixol.
FluphenazineThe serum concentration of Toremifene can be increased when it is combined with Fluphenazine.
FlurazepamThe serum concentration of Toremifene can be increased when it is combined with Flurazepam.
FluvoxamineThe metabolism of Toremifene can be decreased when combined with Fluvoxamine.
FormoterolFormoterol may increase the QTc-prolonging activities of Toremifene.
FosamprenavirThe metabolism of Toremifene can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Toremifene can be increased when it is combined with Fosaprepitant.
FoscarnetFoscarnet may increase the QTc-prolonging activities of Toremifene.
FosphenytoinThe serum concentration of Toremifene can be decreased when it is combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Toremifene can be increased when it is combined with Fusidic Acid.
Gadobenic acidGadobenic acid may increase the QTc-prolonging activities of Toremifene.
GalantamineGalantamine may increase the QTc-prolonging activities of Toremifene.
GefitinibThe serum concentration of Toremifene can be increased when it is combined with Gefitinib.
GemifloxacinGemifloxacin may increase the QTc-prolonging activities of Toremifene.
GenisteinThe serum concentration of Toremifene can be increased when it is combined with Genistein.
GlyburideThe serum concentration of Toremifene can be increased when it is combined with Glyburide.
GlycerolThe serum concentration of Toremifene can be increased when it is combined with Glycerol.
GoserelinGoserelin may increase the QTc-prolonging activities of Toremifene.
Gramicidin DThe serum concentration of Toremifene can be increased when it is combined with Gramicidin D.
GranisetronGranisetron may increase the QTc-prolonging activities of Toremifene.
GrepafloxacinThe serum concentration of Toremifene can be increased when it is combined with Grepafloxacin.
HaloperidolHaloperidol may increase the QTc-prolonging activities of Toremifene.
HistrelinHistrelin may increase the QTc-prolonging activities of Toremifene.
HydrochlorothiazideHydrochlorothiazide may increase the hypercalcemic activities of Toremifene.
HydrocortisoneThe serum concentration of Toremifene can be increased when it is combined with Hydrocortisone.
HydroflumethiazideHydroflumethiazide may increase the hypercalcemic activities of Toremifene.
HydroxyzineHydroxyzine may increase the QTc-prolonging activities of Toremifene.
IbandronateIbandronate may increase the QTc-prolonging activities of Toremifene.
IbutilideIbutilide may increase the QTc-prolonging activities of Toremifene.
IdelalisibThe serum concentration of Toremifene can be increased when it is combined with Idelalisib.
IloperidoneToremifene may increase the QTc-prolonging activities of Iloperidone.
ImatinibThe metabolism of Toremifene can be decreased when combined with Imatinib.
ImipramineThe serum concentration of Toremifene can be increased when it is combined with Imipramine.
IndacaterolIndacaterol may increase the QTc-prolonging activities of Toremifene.
IndapamideIndapamide may increase the hypercalcemic activities of Toremifene.
IndinavirThe risk or severity of adverse effects can be increased when Indinavir is combined with Toremifene.
IndomethacinThe serum concentration of Toremifene can be increased when it is combined with Indomethacin.
IsavuconazoniumThe metabolism of Toremifene can be decreased when combined with Isavuconazonium.
IsofluraneIsoflurane may increase the QTc-prolonging activities of Toremifene.
IsradipineThe metabolism of Toremifene can be decreased when combined with Isradipine.
ItraconazoleThe risk or severity of adverse effects can be increased when Itraconazole is combined with Toremifene.
IvabradineIvabradine may increase the QTc-prolonging activities of Toremifene.
IvacaftorThe serum concentration of Toremifene can be increased when it is combined with Ivacaftor.
IvermectinThe serum concentration of Toremifene can be increased when it is combined with Ivermectin.
KetamineThe serum concentration of Toremifene can be increased when it is combined with Ketamine.
KetoconazoleThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Toremifene.
LansoprazoleThe serum concentration of Toremifene can be increased when it is combined with Lansoprazole.
LapatinibThe serum concentration of Toremifene can be increased when it is combined with Lapatinib.
LenvatinibLenvatinib may increase the QTc-prolonging activities of Toremifene.
LeuprolideLeuprolide may increase the QTc-prolonging activities of Toremifene.
LevofloxacinLevofloxacin may increase the QTc-prolonging activities of Toremifene.
LevothyroxineThe serum concentration of Toremifene can be decreased when it is combined with Levothyroxine.
LidocaineThe serum concentration of Toremifene can be increased when it is combined with Lidocaine.
LiothyronineThe serum concentration of Toremifene can be decreased when it is combined with Liothyronine.
LiotrixThe serum concentration of Toremifene can be decreased when it is combined with Liotrix.
LisinoprilThe serum concentration of Toremifene can be increased when it is combined with Lisinopril.
LithiumLithium may increase the QTc-prolonging activities of Toremifene.
LomitapideThe serum concentration of Toremifene can be increased when it is combined with Lomitapide.
LoperamideThe serum concentration of Toremifene can be increased when it is combined with Loperamide.
LopinavirThe risk or severity of adverse effects can be increased when Lopinavir is combined with Toremifene.
LopinavirToremifene may increase the QTc-prolonging activities of Lopinavir.
LoratadineThe serum concentration of Toremifene can be increased when it is combined with Loratadine.
LosartanThe serum concentration of Toremifene can be increased when it is combined with Losartan.
LovastatinThe metabolism of Toremifene can be decreased when combined with Lovastatin.
LuliconazoleThe serum concentration of Toremifene can be increased when it is combined with Luliconazole.
LumacaftorThe serum concentration of Toremifene can be decreased when it is combined with Lumacaftor.
LumefantrineToremifene may increase the QTc-prolonging activities of Lumefantrine.
MaprotilineThe serum concentration of Toremifene can be increased when it is combined with Maprotiline.
MebendazoleThe serum concentration of Toremifene can be increased when it is combined with Mebendazole.
MefloquineThe serum concentration of Toremifene can be increased when it is combined with Mefloquine.
Megestrol acetateThe serum concentration of Toremifene can be increased when it is combined with Megestrol acetate.
MeprobamateThe serum concentration of Toremifene can be increased when it is combined with Meprobamate.
MethadoneMethadone may increase the QTc-prolonging activities of Toremifene.
MethotrimeprazineMethotrimeprazine may increase the QTc-prolonging activities of Toremifene.
MethyclothiazideMethyclothiazide may increase the hypercalcemic activities of Toremifene.
MetoclopramideMetoclopramide may increase the QTc-prolonging activities of Toremifene.
MetolazoneMetolazone may increase the hypercalcemic activities of Toremifene.
MetoprololThe serum concentration of Toremifene can be increased when it is combined with Metoprolol.
MetronidazoleMetronidazole may increase the QTc-prolonging activities of Toremifene.
MexiletineThe metabolism of Toremifene can be decreased when combined with Mexiletine.
MibefradilThe serum concentration of Toremifene can be increased when it is combined with Mibefradil.
MiconazoleThe serum concentration of Toremifene can be increased when it is combined with Miconazole.
MidazolamThe serum concentration of Toremifene can be decreased when it is combined with Midazolam.
MifepristoneMifepristone may increase the QTc-prolonging activities of Toremifene.
MirabegronMirabegron may increase the QTc-prolonging activities of Toremifene.
MirtazapineMirtazapine may increase the QTc-prolonging activities of Toremifene.
MitomycinThe serum concentration of Toremifene can be increased when it is combined with Mitomycin.
MitotaneThe serum concentration of Toremifene can be decreased when it is combined with Mitotane.
MitoxantroneThe serum concentration of Toremifene can be decreased when it is combined with Mitoxantrone.
ModafinilThe serum concentration of Toremifene can be decreased when it is combined with Modafinil.
MoexiprilMoexipril may increase the QTc-prolonging activities of Toremifene.
MorphineThe serum concentration of Toremifene can be increased when it is combined with Morphine.
MoxifloxacinMoxifloxacin may increase the QTc-prolonging activities of Toremifene.
NafcillinThe serum concentration of Toremifene can be decreased when it is combined with Nafcillin.
NaltrexoneThe serum concentration of Toremifene can be increased when it is combined with Naltrexone.
NaringeninThe serum concentration of Toremifene can be increased when it is combined with Naringenin.
NefazodoneThe risk or severity of adverse effects can be increased when Nefazodone is combined with Toremifene.
NelfinavirThe risk or severity of adverse effects can be increased when Nelfinavir is combined with Toremifene.
NeostigmineThe serum concentration of Toremifene can be increased when it is combined with Neostigmine.
NetupitantThe serum concentration of Toremifene can be increased when it is combined with Netupitant.
NevirapineThe serum concentration of Toremifene can be decreased when it is combined with Nevirapine.
NicardipineThe serum concentration of Toremifene can be increased when it is combined with Nicardipine.
NifedipineThe serum concentration of Toremifene can be decreased when it is combined with Nifedipine.
NilotinibToremifene may increase the QTc-prolonging activities of Nilotinib.
NisoldipineThe serum concentration of Toremifene can be increased when it is combined with Nisoldipine.
NitrazepamThe serum concentration of Toremifene can be increased when it is combined with Nitrazepam.
NitrendipineThe serum concentration of Toremifene can be increased when it is combined with Nitrendipine.
NorethisteroneThe serum concentration of Toremifene can be decreased when it is combined with Norethisterone.
NorfloxacinNorfloxacin may increase the QTc-prolonging activities of Toremifene.
NortriptylineNortriptyline may increase the QTc-prolonging activities of Toremifene.
OctreotideOctreotide may increase the QTc-prolonging activities of Toremifene.
OfloxacinOfloxacin may increase the QTc-prolonging activities of Toremifene.
OlanzapineOlanzapine may increase the QTc-prolonging activities of Toremifene.
OlaparibThe metabolism of Toremifene can be decreased when combined with Olaparib.
OlodaterolOlodaterol may increase the QTc-prolonging activities of Toremifene.
OmeprazoleThe serum concentration of Toremifene can be increased when it is combined with Omeprazole.
OndansetronOndansetron may increase the QTc-prolonging activities of Toremifene.
OsimertinibThe serum concentration of Toremifene can be increased when it is combined with Osimertinib.
OspemifeneThe risk or severity of adverse effects can be increased when Toremifene is combined with Ospemifene.
OuabainOuabain may decrease the cardiotoxic activities of Toremifene.
OxytocinOxytocin may increase the QTc-prolonging activities of Toremifene.
P-NitrophenolThe serum concentration of Toremifene can be increased when it is combined with P-Nitrophenol.
PaclitaxelThe serum concentration of Toremifene can be increased when it is combined with Paclitaxel.
PalbociclibThe serum concentration of Toremifene can be increased when it is combined with Palbociclib.
PaliperidoneToremifene may increase the QTc-prolonging activities of Paliperidone.
Palmitic AcidThe serum concentration of Toremifene can be increased when it is combined with Palmitic Acid.
PanobinostatPanobinostat may increase the QTc-prolonging activities of Toremifene.
PantoprazoleThe serum concentration of Toremifene can be increased when it is combined with Pantoprazole.
ParoxetineThe serum concentration of Toremifene can be increased when it is combined with Paroxetine.
PasireotidePasireotide may increase the QTc-prolonging activities of Toremifene.
PazopanibPazopanib may increase the QTc-prolonging activities of Toremifene.
Peginterferon alfa-2bThe serum concentration of Toremifene can be increased when it is combined with Peginterferon alfa-2b.
PentamidinePentamidine may increase the QTc-prolonging activities of Toremifene.
PentobarbitalThe serum concentration of Toremifene can be decreased when it is combined with Pentobarbital.
PerflutrenPerflutren may increase the QTc-prolonging activities of Toremifene.
PerindoprilThe serum concentration of Toremifene can be increased when it is combined with Perindopril.
PhenindioneToremifene may increase the anticoagulant activities of Phenindione.
PhenobarbitalThe serum concentration of Toremifene can be decreased when it is combined with Phenobarbital.
PhenprocoumonToremifene may increase the anticoagulant activities of Phenprocoumon.
PhenytoinThe serum concentration of Toremifene can be decreased when it is combined with Phenytoin.
PimozideToremifene may increase the QTc-prolonging activities of Pimozide.
Platelet Activating FactorThe serum concentration of Toremifene can be decreased when it is combined with Platelet Activating Factor.
PolythiazidePolythiazide may increase the hypercalcemic activities of Toremifene.
PonatinibThe serum concentration of Toremifene can be increased when it is combined with Ponatinib.
PosaconazoleThe risk or severity of adverse effects can be increased when Posaconazole is combined with Toremifene.
PravastatinThe serum concentration of Toremifene can be increased when it is combined with Pravastatin.
PrazosinThe serum concentration of Toremifene can be increased when it is combined with Prazosin.
PrednisoneThe serum concentration of Toremifene can be increased when it is combined with Prednisone.
PrimaquinePrimaquine may increase the QTc-prolonging activities of Toremifene.
PrimidoneThe serum concentration of Toremifene can be decreased when it is combined with Primidone.
ProbenecidThe serum concentration of Toremifene can be increased when it is combined with Probenecid.
ProcainamideToremifene may increase the QTc-prolonging activities of Procainamide.
ProgesteroneThe serum concentration of Toremifene can be decreased when it is combined with Progesterone.
PromazinePromazine may increase the QTc-prolonging activities of Toremifene.
PromethazineThe serum concentration of Toremifene can be increased when it is combined with Promethazine.
PropafenonePropafenone may increase the QTc-prolonging activities of Toremifene.
PropofolPropofol may increase the QTc-prolonging activities of Toremifene.
PropranololThe serum concentration of Toremifene can be increased when it is combined with Propranolol.
ProtriptylineThe serum concentration of Toremifene can be increased when it is combined with Protriptyline.
QuercetinThe serum concentration of Toremifene can be increased when it is combined with Quercetin.
QuetiapineToremifene may increase the QTc-prolonging activities of Quetiapine.
QuinacrineThe serum concentration of Toremifene can be increased when it is combined with Quinacrine.
QuinethazoneQuinethazone may increase the hypercalcemic activities of Toremifene.
QuinidineToremifene may increase the QTc-prolonging activities of Quinidine.
QuinineQuinine may increase the QTc-prolonging activities of Toremifene.
RanitidineThe serum concentration of Toremifene can be increased when it is combined with Ranitidine.
RanolazineThe serum concentration of Toremifene can be increased when it is combined with Ranolazine.
ReboxetineThe serum concentration of Toremifene can be increased when it is combined with Reboxetine.
RegorafenibThe serum concentration of Toremifene can be increased when it is combined with Regorafenib.
ReserpineThe serum concentration of Toremifene can be decreased when it is combined with Reserpine.
RifabutinThe serum concentration of Toremifene can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Toremifene can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Toremifene can be decreased when it is combined with Rifapentine.
RilpivirineThe serum concentration of Toremifene can be increased when it is combined with Rilpivirine.
RisperidoneRisperidone may increase the QTc-prolonging activities of Toremifene.
RitonavirThe risk or severity of adverse effects can be increased when Ritonavir is combined with Toremifene.
RolapitantThe serum concentration of Toremifene can be increased when it is combined with Rolapitant.
RopiniroleThe metabolism of Toremifene can be decreased when combined with Ropinirole.
SalbutamolSalbutamol may increase the QTc-prolonging activities of Toremifene.
SalmeterolSalmeterol may increase the QTc-prolonging activities of Toremifene.
SaquinavirThe risk or severity of adverse effects can be increased when Saquinavir is combined with Toremifene.
ScopolamineThe serum concentration of Toremifene can be increased when it is combined with Scopolamine.
SelegilineThe serum concentration of Toremifene can be increased when it is combined with Selegiline.
SertralineThe serum concentration of Toremifene can be increased when it is combined with Sertraline.
SevofluraneSevoflurane may increase the QTc-prolonging activities of Toremifene.
SildenafilThe metabolism of Toremifene can be decreased when combined with Sildenafil.
SiltuximabThe serum concentration of Toremifene can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Toremifene can be increased when it is combined with Simeprevir.
SimvastatinThe serum concentration of Toremifene can be increased when it is combined with Simvastatin.
SirolimusThe serum concentration of Toremifene can be decreased when it is combined with Sirolimus.
SolifenacinSolifenacin may increase the QTc-prolonging activities of Toremifene.
SorafenibThe serum concentration of Toremifene can be increased when it is combined with Sorafenib.
SotalolSotalol may increase the QTc-prolonging activities of Toremifene.
SpironolactoneThe serum concentration of Toremifene can be increased when it is combined with Spironolactone.
St. John's WortThe serum concentration of Toremifene can be decreased when it is combined with St. John's Wort.
StaurosporineThe serum concentration of Toremifene can be increased when it is combined with Staurosporine.
StiripentolThe serum concentration of Toremifene can be increased when it is combined with Stiripentol.
StreptozocinThe serum concentration of Toremifene can be decreased when it is combined with Streptozocin.
SugammadexThe therapeutic efficacy of Sugammadex can be decreased when used in combination with Toremifene.
SulfamethoxazoleSulfamethoxazole may increase the QTc-prolonging activities of Toremifene.
SulfinpyrazoneThe serum concentration of Toremifene can be increased when it is combined with Sulfinpyrazone.
SulfisoxazoleSulfisoxazole may increase the QTc-prolonging activities of Toremifene.
SumatriptanThe serum concentration of Toremifene can be increased when it is combined with Sumatriptan.
SunitinibThe serum concentration of Toremifene can be increased when it is combined with Sunitinib.
TacrineThe serum concentration of Toremifene can be increased when it is combined with Tacrine.
TacrolimusThe serum concentration of Toremifene can be decreased when it is combined with Tacrolimus.
TamoxifenThe serum concentration of Toremifene can be decreased when it is combined with Tamoxifen.
Taurocholic AcidThe serum concentration of Toremifene can be increased when it is combined with Taurocholic Acid.
TelaprevirThe risk or severity of adverse effects can be increased when Telaprevir is combined with Toremifene.
TelavancinTelavancin may increase the QTc-prolonging activities of Toremifene.
TelithromycinThe risk or severity of adverse effects can be increased when Telithromycin is combined with Toremifene.
TelmisartanThe serum concentration of Toremifene can be increased when it is combined with Telmisartan.
TemsirolimusThe serum concentration of Toremifene can be increased when it is combined with Temsirolimus.
TenofovirThe metabolism of Toremifene can be decreased when combined with Tenofovir.
TerazosinThe serum concentration of Toremifene can be increased when it is combined with Terazosin.
TerbutalineTerbutaline may increase the QTc-prolonging activities of Toremifene.
TerfenadineThe serum concentration of Toremifene can be increased when it is combined with Terfenadine.
TeriflunomideThe serum concentration of Toremifene can be decreased when it is combined with Teriflunomide.
TesmilifeneThe serum concentration of Toremifene can be decreased when it is combined with Tesmilifene.
TestosteroneThe serum concentration of Toremifene can be increased when it is combined with Testosterone.
TetrabenazineToremifene may increase the QTc-prolonging activities of Tetrabenazine.
TheophyllineThe metabolism of Toremifene can be decreased when combined with Theophylline.
ThioridazineToremifene may increase the QTc-prolonging activities of Thioridazine.
ThiothixeneThiothixene may increase the QTc-prolonging activities of Toremifene.
TicagrelorThe serum concentration of Toremifene can be increased when it is combined with Ticagrelor.
TiclopidineThe metabolism of Toremifene can be decreased when combined with Ticlopidine.
TizanidineTizanidine may increase the QTc-prolonging activities of Toremifene.
TocilizumabThe serum concentration of Toremifene can be decreased when it is combined with Tocilizumab.
TolterodineTolterodine may increase the QTc-prolonging activities of Toremifene.
TolvaptanThe serum concentration of Toremifene can be increased when it is combined with Tolvaptan.
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Toremifene.
TrazodoneThe serum concentration of Toremifene can be decreased when it is combined with Trazodone.
TreprostinilTreprostinil may increase the QTc-prolonging activities of Toremifene.
TrichlormethiazideTrichlormethiazide may increase the hypercalcemic activities of Toremifene.
TrifluoperazineThe serum concentration of Toremifene can be increased when it is combined with Trifluoperazine.
TriflupromazineThe serum concentration of Toremifene can be increased when it is combined with Triflupromazine.
TrimethoprimThe serum concentration of Toremifene can be decreased when it is combined with Trimethoprim.
TrimipramineThe serum concentration of Toremifene can be increased when it is combined with Trimipramine.
TriptorelinTriptorelin may increase the QTc-prolonging activities of Toremifene.
TroleandomycinThe serum concentration of Toremifene can be increased when it is combined with Troleandomycin.
VandetanibToremifene may increase the QTc-prolonging activities of Vandetanib.
VardenafilVardenafil may increase the QTc-prolonging activities of Toremifene.
VemurafenibToremifene may increase the QTc-prolonging activities of Vemurafenib.
VenlafaxineThe metabolism of Toremifene can be decreased when combined with Venlafaxine.
VerapamilThe metabolism of Toremifene can be decreased when combined with Verapamil.
VilanterolVilanterol may increase the QTc-prolonging activities of Toremifene.
VinblastineThe serum concentration of Toremifene can be decreased when it is combined with Vinblastine.
VincristineThe serum concentration of Toremifene can be decreased when it is combined with Vincristine.
VinorelbineThe serum concentration of Toremifene can be increased when it is combined with Vinorelbine.
VoriconazoleThe risk or severity of adverse effects can be increased when Voriconazole is combined with Toremifene.
VorinostatVorinostat may increase the QTc-prolonging activities of Toremifene.
WarfarinToremifene may increase the anticoagulant activities of Warfarin.
ZimelidineThe serum concentration of Toremifene can be increased when it is combined with Zimelidine.
ZiprasidoneZiprasidone may increase the QTc-prolonging activities of Toremifene.
ZuclopenthixolToremifene may increase the QTc-prolonging activities of Zuclopenthixol.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
modulator
General Function:
Zinc ion binding
Specific Function:
Nuclear hormone receptor. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Ligand-dependent nuclear transactivation involves either direct homodimer binding to a palindromic estrogen response element (ERE) sequence or association with other DNA-binding transcription fact...
Gene Name:
ESR1
Uniprot ID:
P03372
Molecular Weight:
66215.45 Da
References
  1. Locci P, Bellocchio S, Lilli C, Marinucci L, Cagini L, Baroni T, Giustozzi G, Balducci C, Becchetti E: Synthesis and secretion of transforming growth factor-beta1 by human desmoid fibroblast cell line and its modulation by toremifene. J Interferon Cytokine Res. 2001 Nov;21(11):961-70. [PubMed:11747628 ]
  2. Liu X, Pisha E, Tonetti DA, Yao D, Li Y, Yao J, Burdette JE, Bolton JL: Antiestrogenic and DNA damaging effects induced by tamoxifen and toremifene metabolites. Chem Res Toxicol. 2003 Jul;16(7):832-7. [PubMed:12870885 ]
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  4. Jones KL, Buzdar AU: A review of adjuvant hormonal therapy in breast cancer. Endocr Relat Cancer. 2004 Sep;11(3):391-406. [PubMed:15369444 ]
  5. Shelly W, Draper MW, Krishnan V, Wong M, Jaffe RB: Selective estrogen receptor modulators: an update on recent clinical findings. Obstet Gynecol Surv. 2008 Mar;63(3):163-81. doi: 10.1097/OGX.0b013e31816400d7. [PubMed:18279543 ]
  6. Gennari L, Merlotti D, Valleggi F, Martini G, Nuti R: Selective estrogen receptor modulators for postmenopausal osteoporosis: current state of development. Drugs Aging. 2007;24(5):361-79. [PubMed:17503894 ]
  7. Lewis-Wambi JS, Jordan VC: Treatment of Postmenopausal Breast Cancer with Selective Estrogen Receptor Modulators (SERMs). Breast Dis. 2005-2006;24:93-105. [PubMed:16917142 ]
  8. Ariazi EA, Ariazi JL, Cordera F, Jordan VC: Estrogen receptors as therapeutic targets in breast cancer. Curr Top Med Chem. 2006;6(3):181-202. [PubMed:16515478 ]
  9. Taneja SS, Smith MR, Dalton JT, Raghow S, Barnette G, Steiner M, Veverka KA: Toremifene--a promising therapy for the prevention of prostate cancer and complications of androgen deprivation therapy. Expert Opin Investig Drugs. 2006 Mar;15(3):293-305. [PubMed:16503765 ]
  10. Goldstein LJ: Controversies in adjuvant endocrine treatment of premenopausal women. Clin Breast Cancer. 2006 Feb;6 Suppl 2:S36-40. [PubMed:16595024 ]
  11. Smith MR: Treatment-related osteoporosis in men with prostate cancer. Clin Cancer Res. 2006 Oct 15;12(20 Pt 2):6315s-6319s. [PubMed:17062721 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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. Taneja SS, Smith MR, Dalton JT, Raghow S, Barnette G, Steiner M, Veverka KA: Toremifene--a promising therapy for the prevention of prostate cancer and complications of androgen deprivation therapy. Expert Opin Investig Drugs. 2006 Mar;15(3):293-305. [PubMed:16503765 ]
  2. Kivisto KT, Villikka K, Nyman L, Anttila M, Neuvonen PJ: Tamoxifen and toremifene concentrations in plasma are greatly decreased by rifampin. Clin Pharmacol Ther. 1998 Dec;64(6):648-54. [PubMed:9871429 ]
  3. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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
substrate
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
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. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 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 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Rao US, Fine RL, Scarborough GA: Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92. [PubMed:7914405 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23