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Identification
NameVemurafenib
Accession NumberDB08881
TypeSmall Molecule
GroupsApproved
DescriptionVemurafenib is a BRAF enzyme inhibitor developed by Plexxikon and Genentech for the treatment of late-stage melanoma. [Wikipedia] The cobas® 4800 BRAF B600 mutation test provided by Roche Molecular Systems is the diagnostic test to confirm eligibility for treatment. FDA approved on August 17, 2011 under the company Hoffmann La Roche.
Structure
Thumb
Synonyms
BRAF(V600E) Kinase Inhibitor RO5185426
PLX4032
Zelboraf
External Identifiers
  • RG7204
  • RO5185426
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Zelboraftablet, film coated240 mg/1oralGenentech, Inc.2011-08-17Not applicableUs
Zelboraftablet240 mgoralHoffmann La Roche Limited2012-03-05Not applicableCanada
ZelborafFilm-coated tablet240 mgOral useRoche Registration Ltd2012-02-17Not applicableEu
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNII207SMY3FQT
CAS number918504-65-1
WeightAverage: 489.922
Monoisotopic: 489.072546264
Chemical FormulaC23H18ClF2N3O3S
InChI KeyInChIKey=GPXBXXGIAQBQNI-UHFFFAOYSA-N
InChI
InChI=1S/C23H18ClF2N3O3S/c1-2-9-33(31,32)29-19-8-7-18(25)20(21(19)26)22(30)17-12-28-23-16(17)10-14(11-27-23)13-3-5-15(24)6-4-13/h3-8,10-12,29H,2,9H2,1H3,(H,27,28)
IUPAC Name
N-{3-[5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluorophenyl}propane-1-sulfonamide
SMILES
CCCS(=O)(=O)NC1=C(F)C(C(=O)C2=CNC3=NC=C(C=C23)C2=CC=C(Cl)C=C2)=C(F)C=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenylpyridines. These are polycyclic aromatic compounds containing a benzene ring linked to a pyridine ring through a CC or CN bond.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassPyridines and derivatives
Sub ClassPhenylpyridines
Direct ParentPhenylpyridines
Alternative Parents
Substituents
  • 3-phenylpyridine
  • Sulfanilide
  • Pyrrolopyridine
  • Acetophenone
  • Aryl ketone
  • Benzoyl
  • Halobenzene
  • Fluorobenzene
  • Chlorobenzene
  • Benzenoid
  • Substituted pyrrole
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl fluoride
  • Aryl chloride
  • Heteroaromatic compound
  • Vinylogous amide
  • Vinylogous halide
  • Aminosulfonyl compound
  • Sulfonyl
  • Sulfonic acid derivative
  • Sulfonamide
  • Pyrrole
  • Ketone
  • Azacycle
  • Hydrocarbon derivative
  • Organosulfur compound
  • Organooxygen compound
  • Organonitrogen compound
  • Organofluoride
  • Organochloride
  • Organohalogen compound
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationTreatment of unresectable or metastatic melanoma in patients with the BRAF-V600 mutation.
PharmacodynamicsNot Available
Mechanism of actionVemurafenib is an orally available inhibitor of mutated BRAF-serine-threonine kinase. It is especially potent against the BRAF V600E mutation. This mutation involves the substitution of glutamic acid for valine at codon 600. The BRAF oncogene, most of which have the V600E mutation, activates mitogen-activated kinase (MAPK) pathway which results in cell growth, proliferation, and metastasis. Vemurafenib blocks these downstream processes to inhibit tumour growth and eventually trigger apoptosis. Vemurafenib does not have antitumour effects against melanoma cell lines with the wild-type BRAF mutation.
Related Articles
AbsorptionAfter oral administration of vemurafenib, it is well absorbed. Bioavailability is unknown. Peak concentrations are reached in 3 hours when an oral dose of 960 mg twice daily for 15 days has been given to patients. Exposure is highly variable between different patients. Gastrointestinal fluid content, pH, volumes, motility, transition time and bile composition may be factors affecting exposure. It is unknown how food affects the absorption of vemurafenib. Time to steady state = 15 - 22 days
Volume of distribution

106 L

Protein binding>99% protein bound to serum albumin and alpha-1 acid glycoprotein.
Metabolism

Vemurafenib is metabolized by CYP3A4 and the metabolites make up 5% of the components in plasma. The parent compound makes up for the remaining 95%.

Route of eliminationExcreted via feces (94%) and urine (1%).
Half lifeElimination half-life = 57 hours (range of 30-120 hours)
Clearance

Total body clearance = 31 L/day

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+0.745
Caco-2 permeable-0.6222
P-glycoprotein substrateNon-substrate0.6215
P-glycoprotein inhibitor INon-inhibitor0.5884
P-glycoprotein inhibitor IINon-inhibitor0.699
Renal organic cation transporterNon-inhibitor0.864
CYP450 2C9 substrateNon-substrate0.7628
CYP450 2D6 substrateNon-substrate0.8038
CYP450 3A4 substrateSubstrate0.5645
CYP450 1A2 substrateInhibitor0.5762
CYP450 2C9 inhibitorInhibitor0.5987
CYP450 2D6 inhibitorNon-inhibitor0.7329
CYP450 2C19 inhibitorInhibitor0.6508
CYP450 3A4 inhibitorInhibitor0.7061
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.9553
Ames testNon AMES toxic0.6323
CarcinogenicityNon-carcinogens0.7229
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.5179 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.6688
hERG inhibition (predictor II)Non-inhibitor0.5302
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Film-coated tabletOral use240 mg
Tabletoral240 mg
Tablet, film coatedoral240 mg/1
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US7504509 No2006-10-222026-10-22Us
US7863288 No2009-06-202029-06-20Us
US8143271 No2006-06-212026-06-21Us
US8470818 No2006-08-022026-08-02Us
US8741920 No2010-07-272030-07-27Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point272°CMSDS
water solubility<1 mg/mL MSDS
logP5.1MSDS
Predicted Properties
PropertyValueSource
Water Solubility0.000362 mg/mLALOGPS
logP4.95ALOGPS
logP4.62ChemAxon
logS-6.1ALOGPS
pKa (Strongest Acidic)7.17ChemAxon
pKa (Strongest Basic)3.2ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area91.92 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity121.97 m3·mol-1ChemAxon
Polarizability48.1 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis ReferenceNot Available
General References
  1. Jordan EJ, Kelly CM: Vemurafenib for the treatment of melanoma. Expert Opin Pharmacother. 2012 Dec;13(17):2533-43. doi: 10.1517/14656566.2012.737780. Epub 2012 Oct 24. [PubMed:23094782 ]
External Links
ATC CodesL01XE15
AHFS Codes
  • 10:00
PDB EntriesNot Available
FDA labelDownload (304 KB)
MSDSDownload (51 KB)
Interactions
Drug Interactions
Drug
AcenocoumarolThe serum concentration of Acenocoumarol can be increased when it is combined with Vemurafenib.
AcetaminophenThe serum concentration of Acetaminophen can be increased when it is combined with Vemurafenib.
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Vemurafenib.
AlbendazoleThe serum concentration of Albendazole can be increased when it is combined with Vemurafenib.
AlfuzosinAlfuzosin may increase the QTc-prolonging activities of Vemurafenib.
AlmotriptanThe serum concentration of Almotriptan can be increased when it is combined with Vemurafenib.
AlosetronThe serum concentration of Alosetron can be increased when it is combined with Vemurafenib.
AmantadineAmantadine may increase the QTc-prolonging activities of Vemurafenib.
AminophenazoneThe serum concentration of Aminophenazone can be increased when it is combined with Vemurafenib.
AminophyllineThe serum concentration of Aminophylline can be increased when it is combined with Vemurafenib.
AmiodaroneThe serum concentration of Vemurafenib can be increased when it is combined with Amiodarone.
AmiodaroneVemurafenib may increase the QTc-prolonging activities of Amiodarone.
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Vemurafenib.
AmitriptylineAmitriptyline may increase the QTc-prolonging activities of Vemurafenib.
AmoxapineAmoxapine may increase the QTc-prolonging activities of Vemurafenib.
AnagrelideAnagrelide may increase the QTc-prolonging activities of Vemurafenib.
AntipyrineThe serum concentration of Antipyrine can be increased when it is combined with Vemurafenib.
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Vemurafenib.
ApomorphineApomorphine may increase the QTc-prolonging activities of Vemurafenib.
AprepitantThe serum concentration of Vemurafenib can be increased when it is combined with Aprepitant.
ArformoterolArformoterol may increase the QTc-prolonging activities of Vemurafenib.
AripiprazoleThe serum concentration of Aripiprazole can be decreased when it is combined with Vemurafenib.
AripiprazoleAripiprazole may increase the QTc-prolonging activities of Vemurafenib.
Arsenic trioxideArsenic trioxide may increase the QTc-prolonging activities of Vemurafenib.
ArtemetherArtemether may increase the QTc-prolonging activities of Vemurafenib.
ASA404The serum concentration of ASA404 can be increased when it is combined with Vemurafenib.
AsenapineAsenapine may increase the QTc-prolonging activities of Vemurafenib.
AtazanavirThe serum concentration of Vemurafenib can be increased when it is combined with Atazanavir.
AtomoxetineThe metabolism of Vemurafenib can be decreased when combined with Atomoxetine.
AV650The serum concentration of AV650 can be increased when it is combined with Vemurafenib.
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Vemurafenib.
AzelastineThe serum concentration of Azelastine can be increased when it is combined with Vemurafenib.
AzithromycinAzithromycin may increase the QTc-prolonging activities of Vemurafenib.
BedaquilineBedaquiline may increase the QTc-prolonging activities of Vemurafenib.
BendamustineThe serum concentration of Bendamustine can be increased when it is combined with Vemurafenib.
Benzyl alcoholThe serum concentration of Benzyl alcohol can be increased when it is combined with Vemurafenib.
BetaxololThe serum concentration of Betaxolol can be increased when it is combined with Vemurafenib.
BevacizumabBevacizumab may increase the cardiotoxic activities of Vemurafenib.
BexaroteneThe serum concentration of Vemurafenib can be decreased when it is combined with Bexarotene.
BoceprevirThe serum concentration of Vemurafenib can be increased when it is combined with Boceprevir.
BortezomibThe serum concentration of Bortezomib can be increased when it is combined with Vemurafenib.
BortezomibThe metabolism of Vemurafenib can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Vemurafenib can be decreased when it is combined with Bosentan.
BromazepamThe serum concentration of Bromazepam can be increased when it is combined with Vemurafenib.
BupivacaineThe serum concentration of Bupivacaine can be increased when it is combined with Vemurafenib.
BupropionThe serum concentration of Bupropion can be increased when it is combined with Vemurafenib.
BuserelinBuserelin may increase the QTc-prolonging activities of Vemurafenib.
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Vemurafenib.
CaffeineThe serum concentration of Caffeine can be increased when it is combined with Vemurafenib.
CarbamazepineThe serum concentration of Carbamazepine can be increased when it is combined with Vemurafenib.
CarbamazepineThe serum concentration of Vemurafenib can be decreased when it is combined with Carbamazepine.
CarmustineThe serum concentration of Carmustine can be increased when it is combined with Vemurafenib.
CarvedilolThe serum concentration of Carvedilol can be increased when it is combined with Vemurafenib.
CeritinibThe serum concentration of Vemurafenib can be increased when it is combined with Ceritinib.
ChloroquineChloroquine may increase the QTc-prolonging activities of Vemurafenib.
ChlorpromazineThe serum concentration of Chlorpromazine can be increased when it is combined with Vemurafenib.
ChlorpromazineChlorpromazine may increase the QTc-prolonging activities of Vemurafenib.
ChlorzoxazoneThe serum concentration of Chlorzoxazone can be increased when it is combined with Vemurafenib.
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Vemurafenib.
CinacalcetThe serum concentration of Cinacalcet can be increased when it is combined with Vemurafenib.
CinnarizineThe serum concentration of Cinnarizine can be increased when it is combined with Vemurafenib.
CiprofloxacinCiprofloxacin may increase the QTc-prolonging activities of Vemurafenib.
CisaprideCisapride may increase the QTc-prolonging activities of Vemurafenib.
CitalopramCitalopram may increase the QTc-prolonging activities of Vemurafenib.
ClarithromycinThe serum concentration of Vemurafenib can be increased when it is combined with Clarithromycin.
ClemastineThe metabolism of Vemurafenib can be decreased when combined with Clemastine.
ClenbuterolThe serum concentration of Clenbuterol can be increased when it is combined with Vemurafenib.
ClevidipineThe serum concentration of Clevidipine can be increased when it is combined with Vemurafenib.
ClomipramineThe serum concentration of Clomipramine can be increased when it is combined with Vemurafenib.
ClomipramineClomipramine may increase the QTc-prolonging activities of Vemurafenib.
ClonidineThe serum concentration of Clonidine can be increased when it is combined with Vemurafenib.
ClopidogrelThe serum concentration of Clopidogrel can be increased when it is combined with Vemurafenib.
ClotrimazoleThe metabolism of Vemurafenib can be decreased when combined with Clotrimazole.
ClozapineThe serum concentration of Clozapine can be increased when it is combined with Vemurafenib.
ClozapineClozapine may increase the QTc-prolonging activities of Vemurafenib.
CobicistatThe serum concentration of Vemurafenib can be increased when it is combined with Cobicistat.
ConivaptanThe serum concentration of Vemurafenib 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 Vemurafenib.
CrizotinibCrizotinib may increase the QTc-prolonging activities of Vemurafenib.
CyclobenzaprineThe serum concentration of Cyclobenzaprine can be increased when it is combined with Vemurafenib.
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Vemurafenib.
CyclosporineThe metabolism of Vemurafenib can be decreased when combined with Cyclosporine.
DabrafenibThe serum concentration of Vemurafenib can be decreased when it is combined with Dabrafenib.
DacarbazineThe serum concentration of Dacarbazine can be increased when it is combined with Vemurafenib.
DapagliflozinThe serum concentration of Dapagliflozin can be increased when it is combined with Vemurafenib.
DarunavirThe serum concentration of Vemurafenib can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Vemurafenib can be increased when it is combined with Dasatinib.
DaunorubicinThe serum concentration of Daunorubicin can be increased when it is combined with Vemurafenib.
DeferasiroxThe serum concentration of Vemurafenib can be decreased when it is combined with Deferasirox.
DegarelixDegarelix may increase the QTc-prolonging activities of Vemurafenib.
DelavirdineThe metabolism of Vemurafenib can be decreased when combined with Delavirdine.
DesfluraneDesflurane may increase the QTc-prolonging activities of Vemurafenib.
DesipramineThe serum concentration of Desipramine can be increased when it is combined with Vemurafenib.
DesipramineDesipramine may increase the QTc-prolonging activities of Vemurafenib.
DeslanosideDeslanoside may decrease the cardiotoxic activities of Vemurafenib.
DexamethasoneThe serum concentration of Vemurafenib can be decreased when it is combined with Dexamethasone.
DexfenfluramineThe serum concentration of Dexfenfluramine can be increased when it is combined with Vemurafenib.
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Vemurafenib.
DiclofenacThe serum concentration of Diclofenac can be increased when it is combined with Vemurafenib.
DigitoxinDigitoxin may decrease the cardiotoxic activities of Vemurafenib.
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Vemurafenib.
DigoxinDigoxin may decrease the cardiotoxic activities of Vemurafenib.
DihydroergotamineThe metabolism of Vemurafenib can be decreased when combined with Dihydroergotamine.
DiltiazemThe metabolism of Vemurafenib can be decreased when combined with Diltiazem.
DinoprostoneThe serum concentration of Dinoprostone can be increased when it is combined with Vemurafenib.
DiphenhydramineThe serum concentration of Diphenhydramine can be increased when it is combined with Vemurafenib.
DiphenhydramineDiphenhydramine may increase the QTc-prolonging activities of Vemurafenib.
DisopyramideDisopyramide may increase the QTc-prolonging activities of Vemurafenib.
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Vemurafenib.
DofetilideDofetilide may increase the QTc-prolonging activities of Vemurafenib.
DolasetronDolasetron may increase the QTc-prolonging activities of Vemurafenib.
DomperidoneDomperidone may increase the QTc-prolonging activities of Vemurafenib.
DoxepinThe serum concentration of Doxepin can be increased when it is combined with Vemurafenib.
DoxepinDoxepin may increase the QTc-prolonging activities of Vemurafenib.
DoxycyclineThe metabolism of Vemurafenib can be decreased when combined with Doxycycline.
DronedaroneDronedarone may increase the QTc-prolonging activities of Vemurafenib.
DroperidolDroperidol may increase the QTc-prolonging activities of Vemurafenib.
DuloxetineThe serum concentration of Duloxetine can be increased when it is combined with Vemurafenib.
EfavirenzThe serum concentration of Vemurafenib can be decreased when it is combined with Efavirenz.
EliglustatVemurafenib may increase the QTc-prolonging activities of Eliglustat.
EltrombopagThe serum concentration of Eltrombopag can be increased when it is combined with Vemurafenib.
EnzalutamideThe serum concentration of Vemurafenib can be decreased when it is combined with Enzalutamide.
ErgotamineThe serum concentration of Ergotamine can be increased when it is combined with Vemurafenib.
EribulinEribulin may increase the QTc-prolonging activities of Vemurafenib.
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Vemurafenib.
ErythromycinErythromycin may increase the QTc-prolonging activities of Vemurafenib.
EscitalopramEscitalopram may increase the QTc-prolonging activities of Vemurafenib.
Eslicarbazepine acetateThe serum concentration of Vemurafenib can be decreased when it is combined with Eslicarbazepine acetate.
EstradiolThe serum concentration of Estradiol can be increased when it is combined with Vemurafenib.
EstroneThe serum concentration of Estrone can be increased when it is combined with Vemurafenib.
Estrone sulfateThe serum concentration of Estrone sulfate can be increased when it is combined with Vemurafenib.
EthanolThe serum concentration of Ethanol can be increased when it is combined with Vemurafenib.
EtoposideThe serum concentration of Etoposide can be increased when it is combined with Vemurafenib.
EtoricoxibThe serum concentration of Etoricoxib can be increased when it is combined with Vemurafenib.
EtravirineThe serum concentration of Vemurafenib can be decreased when it is combined with Etravirine.
EzogabineEzogabine may increase the QTc-prolonging activities of Vemurafenib.
FamotidineFamotidine may increase the QTc-prolonging activities of Vemurafenib.
FelbamateFelbamate may increase the QTc-prolonging activities of Vemurafenib.
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Vemurafenib.
FingolimodFingolimod may increase the QTc-prolonging activities of Vemurafenib.
FlecainideFlecainide may increase the QTc-prolonging activities of Vemurafenib.
FluconazoleThe metabolism of Vemurafenib can be decreased when combined with Fluconazole.
FlunarizineThe serum concentration of Flunarizine can be increased when it is combined with Vemurafenib.
FlunitrazepamThe serum concentration of Flunitrazepam can be increased when it is combined with Vemurafenib.
FluorouracilThe serum concentration of Fluorouracil can be increased when it is combined with Vemurafenib.
FluoxetineFluoxetine may increase the QTc-prolonging activities of Vemurafenib.
FlupentixolFlupentixol may increase the QTc-prolonging activities of Vemurafenib.
FlutamideThe serum concentration of Flutamide can be increased when it is combined with Vemurafenib.
FluvoxamineThe serum concentration of Fluvoxamine can be increased when it is combined with Vemurafenib.
FluvoxamineThe metabolism of Vemurafenib can be decreased when combined with Fluvoxamine.
FormoterolFormoterol may increase the QTc-prolonging activities of Vemurafenib.
FosamprenavirThe metabolism of Vemurafenib can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Vemurafenib can be increased when it is combined with Fosaprepitant.
FoscarnetFoscarnet may increase the QTc-prolonging activities of Vemurafenib.
FosphenytoinThe serum concentration of Vemurafenib can be decreased when it is combined with Fosphenytoin.
FrovatriptanThe serum concentration of Frovatriptan can be increased when it is combined with Vemurafenib.
Fusidic AcidThe serum concentration of Vemurafenib can be increased when it is combined with Fusidic Acid.
Gadobenic acidGadobenic acid may increase the QTc-prolonging activities of Vemurafenib.
GalantamineGalantamine may increase the QTc-prolonging activities of Vemurafenib.
GemifloxacinGemifloxacin may increase the QTc-prolonging activities of Vemurafenib.
GenisteinThe serum concentration of Genistein can be increased when it is combined with Vemurafenib.
GoserelinGoserelin may increase the QTc-prolonging activities of Vemurafenib.
GranisetronGranisetron may increase the QTc-prolonging activities of Vemurafenib.
GrepafloxacinThe serum concentration of Grepafloxacin can be increased when it is combined with Vemurafenib.
GuanabenzThe serum concentration of Guanabenz can be increased when it is combined with Vemurafenib.
HaloperidolThe serum concentration of Haloperidol can be increased when it is combined with Vemurafenib.
HaloperidolHaloperidol may increase the QTc-prolonging activities of Vemurafenib.
HesperetinThe serum concentration of Hesperetin can be increased when it is combined with Vemurafenib.
HexobarbitalThe serum concentration of Hexobarbital can be increased when it is combined with Vemurafenib.
HistrelinHistrelin may increase the QTc-prolonging activities of Vemurafenib.
HydrocodoneThe serum concentration of Hydrocodone can be decreased when it is combined with Vemurafenib.
HydroxyzineHydroxyzine may increase the QTc-prolonging activities of Vemurafenib.
IbandronateIbandronate may increase the QTc-prolonging activities of Vemurafenib.
IbutilideIbutilide may increase the QTc-prolonging activities of Vemurafenib.
IdelalisibThe serum concentration of Vemurafenib can be increased when it is combined with Idelalisib.
IloperidoneIloperidone may increase the QTc-prolonging activities of Vemurafenib.
ImatinibThe serum concentration of Imatinib can be increased when it is combined with Vemurafenib.
ImatinibThe metabolism of Vemurafenib can be decreased when combined with Imatinib.
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Vemurafenib.
ImipramineImipramine may increase the QTc-prolonging activities of Vemurafenib.
ImiquimodThe serum concentration of Imiquimod can be increased when it is combined with Vemurafenib.
IndacaterolIndacaterol may increase the QTc-prolonging activities of Vemurafenib.
IndapamideIndapamide may increase the QTc-prolonging activities of Vemurafenib.
IndinavirThe serum concentration of Vemurafenib can be increased when it is combined with Indinavir.
IpilimumabIpilimumab may increase the hepatotoxic activities of Vemurafenib.
IsavuconazoniumThe metabolism of Vemurafenib can be decreased when combined with Isavuconazonium.
IsofluraneIsoflurane may increase the QTc-prolonging activities of Vemurafenib.
IsradipineThe metabolism of Vemurafenib can be decreased when combined with Isradipine.
ItraconazoleThe serum concentration of Vemurafenib can be increased when it is combined with Itraconazole.
IvabradineIvabradine may increase the QTc-prolonging activities of Vemurafenib.
IvacaftorThe serum concentration of Vemurafenib can be increased when it is combined with Ivacaftor.
IxazomibThe serum concentration of Ixazomib can be increased when it is combined with Vemurafenib.
KetoconazoleThe serum concentration of Vemurafenib can be increased when it is combined with Ketoconazole.
LapatinibLapatinib may increase the QTc-prolonging activities of Vemurafenib.
LeflunomideThe serum concentration of Leflunomide can be increased when it is combined with Vemurafenib.
LenvatinibLenvatinib may increase the QTc-prolonging activities of Vemurafenib.
LeuprolideLeuprolide may increase the QTc-prolonging activities of Vemurafenib.
LevobupivacaineThe serum concentration of Levobupivacaine can be increased when it is combined with Vemurafenib.
LevofloxacinLevofloxacin may increase the QTc-prolonging activities of Vemurafenib.
LidocaineThe serum concentration of Lidocaine can be increased when it is combined with Vemurafenib.
LithiumLithium may increase the QTc-prolonging activities of Vemurafenib.
LomefloxacinThe serum concentration of Lomefloxacin can be increased when it is combined with Vemurafenib.
LopinavirThe serum concentration of Vemurafenib can be increased when it is combined with Lopinavir.
LopinavirVemurafenib may increase the QTc-prolonging activities of Lopinavir.
LorcaserinThe serum concentration of Lorcaserin can be increased when it is combined with Vemurafenib.
LovastatinThe metabolism of Vemurafenib can be decreased when combined with Lovastatin.
LuliconazoleThe serum concentration of Vemurafenib can be increased when it is combined with Luliconazole.
LumefantrineLumefantrine may increase the QTc-prolonging activities of Vemurafenib.
LumiracoxibThe serum concentration of Lumiracoxib can be increased when it is combined with Vemurafenib.
MalathionThe serum concentration of Malathion can be increased when it is combined with Vemurafenib.
MaprotilineThe serum concentration of Maprotiline can be increased when it is combined with Vemurafenib.
MaprotilineMaprotiline may increase the QTc-prolonging activities of Vemurafenib.
MefloquineMefloquine may increase the QTc-prolonging activities of Vemurafenib.
MelatoninThe serum concentration of Melatonin can be increased when it is combined with Vemurafenib.
MenadioneThe serum concentration of Menadione can be increased when it is combined with Vemurafenib.
MephenytoinThe serum concentration of Mephenytoin can be increased when it is combined with Vemurafenib.
MethadoneThe serum concentration of Methadone can be increased when it is combined with Vemurafenib.
MethadoneMethadone may increase the QTc-prolonging activities of Vemurafenib.
MethotrimeprazineMethotrimeprazine may increase the QTc-prolonging activities of Vemurafenib.
MethoxyfluraneThe serum concentration of Methoxyflurane can be increased when it is combined with Vemurafenib.
MetoclopramideMetoclopramide may increase the QTc-prolonging activities of Vemurafenib.
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Vemurafenib.
MetronidazoleMetronidazole may increase the QTc-prolonging activities of Vemurafenib.
MexiletineThe serum concentration of Mexiletine can be increased when it is combined with Vemurafenib.
MianserinThe serum concentration of Mianserin can be increased when it is combined with Vemurafenib.
MifepristoneMifepristone may increase the QTc-prolonging activities of Vemurafenib.
MirabegronMirabegron may increase the QTc-prolonging activities of Vemurafenib.
MirtazapineThe serum concentration of Mirtazapine can be increased when it is combined with Vemurafenib.
MirtazapineMirtazapine may increase the QTc-prolonging activities of Vemurafenib.
MitotaneThe serum concentration of Vemurafenib can be decreased when it is combined with Mitotane.
ModafinilThe serum concentration of Vemurafenib can be decreased when it is combined with Modafinil.
MoexiprilMoexipril may increase the QTc-prolonging activities of Vemurafenib.
MoxifloxacinMoxifloxacin may increase the QTc-prolonging activities of Vemurafenib.
muraglitazarThe serum concentration of muraglitazar can be increased when it is combined with Vemurafenib.
NabumetoneThe serum concentration of Nabumetone can be increased when it is combined with Vemurafenib.
NafcillinThe serum concentration of Vemurafenib can be decreased when it is combined with Nafcillin.
NaproxenThe serum concentration of Naproxen can be increased when it is combined with Vemurafenib.
NefazodoneThe serum concentration of Vemurafenib can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Vemurafenib can be increased when it is combined with Nelfinavir.
NetupitantThe serum concentration of Vemurafenib can be increased when it is combined with Netupitant.
NevirapineThe serum concentration of Vemurafenib can be decreased when it is combined with Nevirapine.
NicardipineNicardipine may increase the QTc-prolonging activities of Vemurafenib.
NicotineThe serum concentration of Nicotine can be increased when it is combined with Vemurafenib.
NifedipineThe serum concentration of Nifedipine can be increased when it is combined with Vemurafenib.
NilotinibNilotinib may increase the QTc-prolonging activities of Vemurafenib.
NimodipineThe serum concentration of Nimodipine can be decreased when it is combined with Vemurafenib.
NintedanibThe serum concentration of Nintedanib can be decreased when it is combined with Vemurafenib.
Nitric OxideThe serum concentration of Nitric Oxide can be increased when it is combined with Vemurafenib.
NorfloxacinNorfloxacin may increase the QTc-prolonging activities of Vemurafenib.
NortriptylineThe serum concentration of Nortriptyline can be increased when it is combined with Vemurafenib.
NortriptylineNortriptyline may increase the QTc-prolonging activities of Vemurafenib.
OctreotideOctreotide may increase the QTc-prolonging activities of Vemurafenib.
OfloxacinOfloxacin may increase the QTc-prolonging activities of Vemurafenib.
OlanzapineThe serum concentration of Olanzapine can be increased when it is combined with Vemurafenib.
OlanzapineOlanzapine may increase the QTc-prolonging activities of Vemurafenib.
OlaparibThe metabolism of Vemurafenib can be decreased when combined with Olaparib.
OlodaterolOlodaterol may increase the QTc-prolonging activities of Vemurafenib.
OmeprazoleThe serum concentration of Omeprazole can be increased when it is combined with Vemurafenib.
OndansetronThe serum concentration of Ondansetron can be increased when it is combined with Vemurafenib.
OndansetronOndansetron may increase the QTc-prolonging activities of Vemurafenib.
OsimertinibThe serum concentration of Vemurafenib can be increased when it is combined with Osimertinib.
OuabainOuabain may decrease the cardiotoxic activities of Vemurafenib.
OxaliplatinThe serum concentration of Oxaliplatin can be increased when it is combined with Vemurafenib.
OxtriphyllineThe serum concentration of Oxtriphylline can be increased when it is combined with Vemurafenib.
OxytocinOxytocin may increase the QTc-prolonging activities of Vemurafenib.
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Vemurafenib.
PalbociclibThe serum concentration of Vemurafenib can be increased when it is combined with Palbociclib.
PaliperidonePaliperidone may increase the QTc-prolonging activities of Vemurafenib.
PalonosetronThe serum concentration of Palonosetron can be increased when it is combined with Vemurafenib.
PanobinostatPanobinostat may increase the QTc-prolonging activities of Vemurafenib.
PantoprazoleThe serum concentration of Pantoprazole can be increased when it is combined with Vemurafenib.
ParoxetineParoxetine may increase the QTc-prolonging activities of Vemurafenib.
PasireotidePasireotide may increase the QTc-prolonging activities of Vemurafenib.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Vemurafenib.
PazopanibPazopanib may increase the QTc-prolonging activities of Vemurafenib.
PentamidineThe serum concentration of Pentamidine can be increased when it is combined with Vemurafenib.
PentamidinePentamidine may increase the QTc-prolonging activities of Vemurafenib.
PentobarbitalThe serum concentration of Vemurafenib can be decreased when it is combined with Pentobarbital.
PentoxifyllineThe serum concentration of Pentoxifylline can be increased when it is combined with Vemurafenib.
PerflutrenPerflutren may increase the QTc-prolonging activities of Vemurafenib.
PerphenazineThe serum concentration of Perphenazine can be increased when it is combined with Vemurafenib.
PhenacetinThe serum concentration of Phenacetin can be increased when it is combined with Vemurafenib.
PhenobarbitalThe serum concentration of Vemurafenib can be decreased when it is combined with Phenobarbital.
PhenytoinThe serum concentration of Vemurafenib can be decreased when it is combined with Phenytoin.
PimozidePimozide may increase the QTc-prolonging activities of Vemurafenib.
PipotiazineThe serum concentration of Pipotiazine can be increased when it is combined with Vemurafenib.
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Vemurafenib.
PosaconazoleThe serum concentration of Vemurafenib can be increased when it is combined with Posaconazole.
PraziquantelThe serum concentration of Praziquantel can be increased when it is combined with Vemurafenib.
PrimaquineThe serum concentration of Primaquine can be increased when it is combined with Vemurafenib.
PrimaquinePrimaquine may increase the QTc-prolonging activities of Vemurafenib.
PrimidoneThe serum concentration of Vemurafenib can be decreased when it is combined with Primidone.
ProcainamideProcainamide may increase the QTc-prolonging activities of Vemurafenib.
ProgesteroneThe serum concentration of Progesterone can be increased when it is combined with Vemurafenib.
ProguanilThe serum concentration of Proguanil can be increased when it is combined with Vemurafenib.
PromazineThe serum concentration of Promazine can be increased when it is combined with Vemurafenib.
PromazinePromazine may increase the QTc-prolonging activities of Vemurafenib.
PromethazinePromethazine may increase the QTc-prolonging activities of Vemurafenib.
PropafenoneThe serum concentration of Propafenone can be increased when it is combined with Vemurafenib.
PropafenonePropafenone may increase the QTc-prolonging activities of Vemurafenib.
PropofolThe serum concentration of Propofol can be increased when it is combined with Vemurafenib.
PropofolPropofol may increase the QTc-prolonging activities of Vemurafenib.
PropranololThe serum concentration of Propranolol can be increased when it is combined with Vemurafenib.
ProtriptylineProtriptyline may increase the QTc-prolonging activities of Vemurafenib.
PyrazinamideThe serum concentration of Pyrazinamide can be increased when it is combined with Vemurafenib.
QuetiapineQuetiapine may increase the QTc-prolonging activities of Vemurafenib.
QuinidineQuinidine may increase the QTc-prolonging activities of Vemurafenib.
QuinineQuinine may increase the QTc-prolonging activities of Vemurafenib.
RamelteonThe serum concentration of Ramelteon can be increased when it is combined with Vemurafenib.
RanitidineThe serum concentration of Ranitidine can be increased when it is combined with Vemurafenib.
RanolazineThe metabolism of Vemurafenib can be decreased when combined with Ranolazine.
RasagilineThe serum concentration of Rasagiline can be increased when it is combined with Vemurafenib.
ResveratrolThe serum concentration of Resveratrol can be increased when it is combined with Vemurafenib.
RifabutinThe serum concentration of Rifabutin can be increased when it is combined with Vemurafenib.
RifabutinThe serum concentration of Vemurafenib can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Vemurafenib can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Vemurafenib can be decreased when it is combined with Rifapentine.
RilpivirineRilpivirine may increase the QTc-prolonging activities of Vemurafenib.
RiluzoleThe serum concentration of Riluzole can be increased when it is combined with Vemurafenib.
RisperidoneRisperidone may increase the QTc-prolonging activities of Vemurafenib.
RitonavirThe serum concentration of Ritonavir can be increased when it is combined with Vemurafenib.
RizatriptanThe serum concentration of Rizatriptan can be increased when it is combined with Vemurafenib.
RofecoxibThe serum concentration of Rofecoxib can be increased when it is combined with Vemurafenib.
RolapitantThe serum concentration of Vemurafenib can be increased when it is combined with Rolapitant.
RopiniroleThe serum concentration of Ropinirole can be increased when it is combined with Vemurafenib.
RopivacaineThe serum concentration of Ropivacaine can be increased when it is combined with Vemurafenib.
RotigotineThe serum concentration of Rotigotine can be increased when it is combined with Vemurafenib.
SalbutamolSalbutamol may increase the QTc-prolonging activities of Vemurafenib.
SalmeterolSalmeterol may increase the QTc-prolonging activities of Vemurafenib.
SaquinavirThe serum concentration of Vemurafenib can be increased when it is combined with Saquinavir.
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Vemurafenib.
SelegilineThe serum concentration of Selegiline can be increased when it is combined with Vemurafenib.
SertralineThe serum concentration of Sertraline can be increased when it is combined with Vemurafenib.
SertralineSertraline may increase the QTc-prolonging activities of Vemurafenib.
SevofluraneSevoflurane may increase the QTc-prolonging activities of Vemurafenib.
SildenafilThe metabolism of Vemurafenib can be decreased when combined with Sildenafil.
SiltuximabThe serum concentration of Vemurafenib can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Vemurafenib can be increased when it is combined with Simeprevir.
SolifenacinSolifenacin may increase the QTc-prolonging activities of Vemurafenib.
SorafenibSorafenib may increase the QTc-prolonging activities of Vemurafenib.
SotalolSotalol may increase the QTc-prolonging activities of Vemurafenib.
St. John's WortThe serum concentration of Vemurafenib can be decreased when it is combined with St. John&#39;s Wort.
StiripentolThe serum concentration of Vemurafenib can be increased when it is combined with Stiripentol.
SulfamethoxazoleSulfamethoxazole may increase the QTc-prolonging activities of Vemurafenib.
SulfisoxazoleSulfisoxazole may increase the QTc-prolonging activities of Vemurafenib.
SunitinibSunitinib may increase the QTc-prolonging activities of Vemurafenib.
TacrineThe serum concentration of Tacrine can be increased when it is combined with Vemurafenib.
TamoxifenThe serum concentration of Tamoxifen can be increased when it is combined with Vemurafenib.
TamoxifenTamoxifen may increase the QTc-prolonging activities of Vemurafenib.
TelaprevirThe serum concentration of Vemurafenib can be increased when it is combined with Telaprevir.
TelavancinTelavancin may increase the QTc-prolonging activities of Vemurafenib.
TelithromycinThe serum concentration of Telithromycin can be increased when it is combined with Vemurafenib.
TemafloxacinThe serum concentration of Temafloxacin can be increased when it is combined with Vemurafenib.
TerbinafineThe serum concentration of Terbinafine can be increased when it is combined with Vemurafenib.
TerbutalineTerbutaline may increase the QTc-prolonging activities of Vemurafenib.
TeriflunomideThe serum concentration of Vemurafenib can be increased when it is combined with Teriflunomide.
TetrabenazineTetrabenazine may increase the QTc-prolonging activities of Vemurafenib.
ThalidomideThe serum concentration of Thalidomide can be increased when it is combined with Vemurafenib.
TheobromineThe serum concentration of Theobromine can be increased when it is combined with Vemurafenib.
TheophyllineThe serum concentration of Theophylline can be increased when it is combined with Vemurafenib.
ThiabendazoleThe serum concentration of Thiabendazole can be increased when it is combined with Vemurafenib.
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Vemurafenib.
ThioridazineThioridazine may increase the QTc-prolonging activities of Vemurafenib.
ThiothixeneThe serum concentration of Thiothixene can be increased when it is combined with Vemurafenib.
ThiothixeneThiothixene may increase the QTc-prolonging activities of Vemurafenib.
TiclopidineThe metabolism of Vemurafenib can be decreased when combined with Ticlopidine.
TizanidineThe serum concentration of Tizanidine can be increased when it is combined with Vemurafenib.
TizanidineTizanidine may increase the QTc-prolonging activities of Vemurafenib.
TocilizumabThe serum concentration of Vemurafenib can be decreased when it is combined with Tocilizumab.
TolterodineTolterodine may increase the QTc-prolonging activities of Vemurafenib.
ToremifeneToremifene may increase the QTc-prolonging activities of Vemurafenib.
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Vemurafenib.
TrazodoneTrazodone may increase the QTc-prolonging activities of Vemurafenib.
TreprostinilTreprostinil may increase the QTc-prolonging activities of Vemurafenib.
TriamtereneThe serum concentration of Triamterene can be increased when it is combined with Vemurafenib.
TrifluoperazineThe serum concentration of Trifluoperazine can be increased when it is combined with Vemurafenib.
TrimethoprimTrimethoprim may increase the QTc-prolonging activities of Vemurafenib.
TrimipramineTrimipramine may increase the QTc-prolonging activities of Vemurafenib.
TriptorelinTriptorelin may increase the QTc-prolonging activities of Vemurafenib.
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Vemurafenib.
VandetanibVandetanib may increase the QTc-prolonging activities of Vemurafenib.
VardenafilVardenafil may increase the QTc-prolonging activities of Vemurafenib.
VenlafaxineThe metabolism of Vemurafenib can be decreased when combined with Venlafaxine.
VerapamilThe serum concentration of Verapamil can be increased when it is combined with Vemurafenib.
VerapamilThe metabolism of Vemurafenib can be decreased when combined with Verapamil.
VilanterolVilanterol may increase the QTc-prolonging activities of Vemurafenib.
VoriconazoleThe serum concentration of Vemurafenib can be increased when it is combined with Voriconazole.
VorinostatVorinostat may increase the QTc-prolonging activities of Vemurafenib.
WarfarinThe serum concentration of Warfarin can be increased when it is combined with Vemurafenib.
ZileutonThe serum concentration of Zileuton can be increased when it is combined with Vemurafenib.
ZiprasidoneZiprasidone may increase the QTc-prolonging activities of Vemurafenib.
ZolmitriptanThe serum concentration of Zolmitriptan can be increased when it is combined with Vemurafenib.
ZolpidemThe serum concentration of Zolpidem can be increased when it is combined with Vemurafenib.
ZuclopenthixolZuclopenthixol may increase the QTc-prolonging activities of Vemurafenib.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Protein serine/threonine kinase activity
Specific Function:
Protein kinase involved in the transduction of mitogenic signals from the cell membrane to the nucleus. May play a role in the postsynaptic responses of hippocampal neuron. Phosphorylates MAP2K1, and thereby contributes to the MAP kinase signal transduction pathway.
Gene Name:
BRAF
Uniprot ID:
P15056
Molecular Weight:
84436.135 Da
References
  1. Jordan EJ, Kelly CM: Vemurafenib for the treatment of melanoma. Expert Opin Pharmacother. 2012 Dec;13(17):2533-43. doi: 10.1517/14656566.2012.737780. Epub 2012 Oct 24. [PubMed:23094782 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
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. Jordan EJ, Kelly CM: Vemurafenib for the treatment of melanoma. Expert Opin Pharmacother. 2012 Dec;13(17):2533-43. doi: 10.1517/14656566.2012.737780. Epub 2012 Oct 24. [PubMed:23094782 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Jordan EJ, Kelly CM: Vemurafenib for the treatment of melanoma. Expert Opin Pharmacother. 2012 Dec;13(17):2533-43. doi: 10.1517/14656566.2012.737780. Epub 2012 Oct 24. [PubMed:23094782 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinducer
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Jordan EJ, Kelly CM: Vemurafenib for the treatment of melanoma. Expert Opin Pharmacother. 2012 Dec;13(17):2533-43. doi: 10.1517/14656566.2012.737780. Epub 2012 Oct 24. [PubMed:23094782 ]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Toxic substance binding
Specific Function:
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloidal osmotic pressure of blood. Major zinc transporter in plasma, typically binds about 80% of all plasma zinc.
Gene Name:
ALB
Uniprot ID:
P02768
Molecular Weight:
69365.94 Da
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Not Available
Specific Function:
Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in the body. Appears to function in modulating the activity of the immune system during the acute-phase reaction.
Gene Name:
ORM1
Uniprot ID:
P02763
Molecular Weight:
23511.38 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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. Mittapalli RK, Vaidhyanathan S, Sane R, Elmquist WF: Impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on the brain distribution of a novel BRAF inhibitor: vemurafenib (PLX4032). J Pharmacol Exp Ther. 2012 Jul;342(1):33-40. doi: 10.1124/jpet.112.192195. Epub 2012 Mar 27. [PubMed:22454535 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both from mitochondria to cytosol and from cytosol to extracellular space, and cellular export of hemin, and heme. Xenobiotic transporter that may play an important role in the exclusion of xenobiotics from t...
Gene Name:
ABCG2
Uniprot ID:
Q9UNQ0
Molecular Weight:
72313.47 Da
References
  1. Mittapalli RK, Vaidhyanathan S, Sane R, Elmquist WF: Impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on the brain distribution of a novel BRAF inhibitor: vemurafenib (PLX4032). J Pharmacol Exp Ther. 2012 Jul;342(1):33-40. doi: 10.1124/jpet.112.192195. Epub 2012 Mar 27. [PubMed:22454535 ]
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Drug created on May 20, 2013 00:41 / Updated on September 29, 2016 02:27