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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
ZelborafTablet240 mgOralHoffmann La Roche Limited2012-03-05Not applicableCanada
ZelborafTablet, film coated240 mgOralRoche Registration Ltd2012-02-17Not applicableEu
ZelborafTablet, film coated240 mg/1OralGenentech, Inc.2011-08-17Not applicableUs
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 KeyGPXBXXGIAQBQNI-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
Pharmacology
IndicationTreatment of unresectable or metastatic melanoma in patients with the BRAF-V600 mutation.
Structured Indications
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.
TargetKindPharmacological actionActionsOrganismUniProt ID
Serine/threonine-protein kinase B-rafProteinyes
inhibitor
HumanP15056 details
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
Interactions
Drug Interactions
DrugInteractionDrug group
AcenocoumarolThe serum concentration of Acenocoumarol can be increased when it is combined with Vemurafenib.Approved
AcetaminophenThe serum concentration of Acetaminophen can be increased when it is combined with Vemurafenib.Approved
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Vemurafenib.Approved
AlbendazoleThe serum concentration of Albendazole can be increased when it is combined with Vemurafenib.Approved, Vet Approved
AlfuzosinAlfuzosin may increase the QTc-prolonging activities of Vemurafenib.Approved, Investigational
AlmotriptanThe serum concentration of Almotriptan can be increased when it is combined with Vemurafenib.Approved, Investigational
AlosetronThe serum concentration of Alosetron can be increased when it is combined with Vemurafenib.Approved, Withdrawn
AmantadineAmantadine may increase the QTc-prolonging activities of Vemurafenib.Approved
AminophenazoneThe serum concentration of Aminophenazone can be increased when it is combined with Vemurafenib.Approved, Withdrawn
AminophyllineThe serum concentration of Aminophylline can be increased when it is combined with Vemurafenib.Approved
AmiodaroneThe serum concentration of Vemurafenib can be increased when it is combined with Amiodarone.Approved, Investigational
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Vemurafenib.Approved
AmoxapineAmoxapine may increase the QTc-prolonging activities of Vemurafenib.Approved
AnagrelideThe serum concentration of Anagrelide can be increased when it is combined with Vemurafenib.Approved
AntipyrineThe serum concentration of Antipyrine can be increased when it is combined with Vemurafenib.Approved
AnvirzelAnvirzel may decrease the cardiotoxic activities of Vemurafenib.Investigational
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Vemurafenib.Approved
ApomorphineApomorphine may increase the QTc-prolonging activities of Vemurafenib.Approved, Investigational
AprepitantThe serum concentration of Aprepitant can be increased when it is combined with Vemurafenib.Approved, Investigational
ArformoterolArformoterol may increase the QTc-prolonging activities of Vemurafenib.Approved, Investigational
AripiprazoleThe serum concentration of Aripiprazole can be decreased when it is combined with Vemurafenib.Approved, Investigational
Arsenic trioxideArsenic trioxide may increase the QTc-prolonging activities of Vemurafenib.Approved, Investigational
ArtemetherArtemether may increase the QTc-prolonging activities of Vemurafenib.Approved
ASA404The serum concentration of ASA404 can be increased when it is combined with Vemurafenib.Investigational
AsenapineThe serum concentration of Asenapine can be increased when it is combined with Vemurafenib.Approved
AtazanavirThe serum concentration of Vemurafenib can be increased when it is combined with Atazanavir.Approved, Investigational
AtomoxetineAtomoxetine may increase the QTc-prolonging activities of Vemurafenib.Approved
AV650The serum concentration of AV650 can be increased when it is combined with Vemurafenib.Approved, Investigational
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Vemurafenib.Approved, Investigational
AzelastineThe serum concentration of Azelastine can be increased when it is combined with Vemurafenib.Approved
AzithromycinAzithromycin may increase the QTc-prolonging activities of Vemurafenib.Approved
BedaquilineBedaquiline may increase the QTc-prolonging activities of Vemurafenib.Approved
BendamustineThe serum concentration of Bendamustine can be increased when it is combined with Vemurafenib.Approved, Investigational
Benzyl alcoholThe serum concentration of Benzyl alcohol can be increased when it is combined with Vemurafenib.Approved
BetaxololThe serum concentration of Betaxolol can be increased when it is combined with Vemurafenib.Approved
BevacizumabBevacizumab may increase the cardiotoxic activities of Vemurafenib.Approved, Investigational
BexaroteneThe serum concentration of Vemurafenib can be decreased when it is combined with Bexarotene.Approved, Investigational
BoceprevirThe serum concentration of Vemurafenib can be increased when it is combined with Boceprevir.Approved
BortezomibThe serum concentration of Bortezomib can be increased when it is combined with Vemurafenib.Approved, Investigational
BosentanThe serum concentration of Vemurafenib can be decreased when it is combined with Bosentan.Approved, Investigational
BromazepamThe serum concentration of Bromazepam can be increased when it is combined with Vemurafenib.Approved, Illicit
BupivacaineThe serum concentration of Bupivacaine can be increased when it is combined with Vemurafenib.Approved, Investigational
BupropionThe serum concentration of Bupropion can be increased when it is combined with Vemurafenib.Approved
BuserelinBuserelin may increase the QTc-prolonging activities of Vemurafenib.Approved
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Vemurafenib.Approved
CaffeineThe serum concentration of Caffeine can be increased when it is combined with Vemurafenib.Approved
CarbamazepineThe serum concentration of Vemurafenib can be decreased when it is combined with Carbamazepine.Approved, Investigational
CarmustineThe serum concentration of Carmustine can be increased when it is combined with Vemurafenib.Approved
CarvedilolThe serum concentration of Carvedilol can be increased when it is combined with Vemurafenib.Approved, Investigational
CeritinibThe serum concentration of Vemurafenib can be increased when it is combined with Ceritinib.Approved
ChloroquineChloroquine may increase the QTc-prolonging activities of Vemurafenib.Approved, Vet Approved
ChlorpromazineThe serum concentration of Chlorpromazine can be increased when it is combined with Vemurafenib.Approved, Vet Approved
ChlorzoxazoneThe serum concentration of Chlorzoxazone can be increased when it is combined with Vemurafenib.Approved
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Vemurafenib.Approved
CinacalcetThe serum concentration of Cinacalcet can be increased when it is combined with Vemurafenib.Approved
CinnarizineThe serum concentration of Cinnarizine can be increased when it is combined with Vemurafenib.Approved
CiprofloxacinCiprofloxacin may increase the QTc-prolonging activities of Vemurafenib.Approved, Investigational
CisaprideThe serum concentration of Cisapride can be increased when it is combined with Vemurafenib.Approved, Investigational, Withdrawn
CitalopramCitalopram may increase the QTc-prolonging activities of Vemurafenib.Approved
ClarithromycinThe serum concentration of Vemurafenib can be increased when it is combined with Clarithromycin.Approved
ClemastineThe metabolism of Vemurafenib can be decreased when combined with Clemastine.Approved
ClenbuterolThe serum concentration of Clenbuterol can be increased when it is combined with Vemurafenib.Approved, Vet Approved
ClevidipineThe serum concentration of Clevidipine can be increased when it is combined with Vemurafenib.Approved
ClomipramineThe serum concentration of Clomipramine can be increased when it is combined with Vemurafenib.Approved, Vet Approved
ClonidineThe serum concentration of Clonidine can be increased when it is combined with Vemurafenib.Approved
ClopidogrelThe serum concentration of Clopidogrel can be increased when it is combined with Vemurafenib.Approved, Nutraceutical
ClotrimazoleThe metabolism of Vemurafenib can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe serum concentration of Clozapine can be increased when it is combined with Vemurafenib.Approved
CobicistatThe serum concentration of Vemurafenib can be increased when it is combined with Cobicistat.Approved
ConivaptanThe serum concentration of Vemurafenib can be increased when it is combined with Conivaptan.Approved, Investigational
Conjugated Equine EstrogensThe serum concentration of Conjugated Equine Estrogens can be increased when it is combined with Vemurafenib.Approved
CrizotinibCrizotinib may increase the QTc-prolonging activities of Vemurafenib.Approved
CyclobenzaprineThe serum concentration of Cyclobenzaprine can be increased when it is combined with Vemurafenib.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Vemurafenib.Approved, Investigational
CyclosporineThe metabolism of Vemurafenib can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
DabrafenibThe serum concentration of Vemurafenib can be decreased when it is combined with Dabrafenib.Approved
DacarbazineThe serum concentration of Dacarbazine can be increased when it is combined with Vemurafenib.Approved, Investigational
DapagliflozinThe serum concentration of Dapagliflozin can be increased when it is combined with Vemurafenib.Approved
DarunavirThe serum concentration of Vemurafenib can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Dasatinib can be increased when it is combined with Vemurafenib.Approved, Investigational
DaunorubicinThe serum concentration of Daunorubicin can be increased when it is combined with Vemurafenib.Approved
DeferasiroxThe serum concentration of Vemurafenib can be decreased when it is combined with Deferasirox.Approved, Investigational
DegarelixDegarelix may increase the QTc-prolonging activities of Vemurafenib.Approved
DelavirdineThe metabolism of Vemurafenib can be decreased when combined with Delavirdine.Approved
DesfluraneDesflurane may increase the QTc-prolonging activities of Vemurafenib.Approved
DesipramineThe serum concentration of Desipramine can be increased when it is combined with Vemurafenib.Approved
DeslanosideDeslanoside may decrease the cardiotoxic activities of Vemurafenib.Approved
DexamethasoneThe serum concentration of Vemurafenib can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DexfenfluramineThe serum concentration of Dexfenfluramine can be increased when it is combined with Vemurafenib.Approved, Illicit, Withdrawn
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Vemurafenib.Approved, Illicit, Vet Approved
DiclofenacThe serum concentration of Diclofenac can be increased when it is combined with Vemurafenib.Approved, Vet Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Vemurafenib.Approved
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Vemurafenib.Approved
DihydroergotamineThe metabolism of Vemurafenib can be decreased when combined with Dihydroergotamine.Approved
DiltiazemThe metabolism of Vemurafenib can be decreased when combined with Diltiazem.Approved
DinoprostoneThe serum concentration of Dinoprostone can be increased when it is combined with Vemurafenib.Approved
DiphenhydramineThe serum concentration of Diphenhydramine can be increased when it is combined with Vemurafenib.Approved
DisopyramideDisopyramide may increase the QTc-prolonging activities of Vemurafenib.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Vemurafenib.Approved, Investigational
DofetilideDofetilide may increase the QTc-prolonging activities of Vemurafenib.Approved
DolasetronDolasetron may increase the QTc-prolonging activities of Vemurafenib.Approved
DomperidoneThe serum concentration of Domperidone can be increased when it is combined with Vemurafenib.Approved, Investigational, Vet Approved
DoxepinThe serum concentration of Doxepin can be increased when it is combined with Vemurafenib.Approved
DoxycyclineThe metabolism of Vemurafenib can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneDronedarone may increase the QTc-prolonging activities of Vemurafenib.Approved
DroperidolDroperidol may increase the QTc-prolonging activities of Vemurafenib.Approved, Vet Approved
DuloxetineThe serum concentration of Duloxetine can be increased when it is combined with Vemurafenib.Approved
EfavirenzThe serum concentration of Vemurafenib can be decreased when it is combined with Efavirenz.Approved, Investigational
EliglustatVemurafenib may increase the QTc-prolonging activities of Eliglustat.Approved
EltrombopagThe serum concentration of Eltrombopag can be increased when it is combined with Vemurafenib.Approved
EnzalutamideThe serum concentration of Vemurafenib can be decreased when it is combined with Enzalutamide.Approved
ErgotamineThe serum concentration of Ergotamine can be increased when it is combined with Vemurafenib.Approved
EribulinEribulin may increase the QTc-prolonging activities of Vemurafenib.Approved, Investigational
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Vemurafenib.Approved, Investigational
ErythromycinErythromycin may increase the QTc-prolonging activities of Vemurafenib.Approved, Vet Approved
EscitalopramEscitalopram may increase the QTc-prolonging activities of Vemurafenib.Approved, Investigational
Eslicarbazepine acetateThe serum concentration of Vemurafenib can be decreased when it is combined with Eslicarbazepine acetate.Approved
EstradiolThe serum concentration of Estradiol can be increased when it is combined with Vemurafenib.Approved, Investigational, Vet Approved
EstroneThe serum concentration of Estrone can be increased when it is combined with Vemurafenib.Approved
Estrone sulfateThe serum concentration of Estrone sulfate can be increased when it is combined with Vemurafenib.Approved
EthanolThe serum concentration of Ethanol can be increased when it is combined with Vemurafenib.Approved
EtoposideThe serum concentration of Etoposide can be increased when it is combined with Vemurafenib.Approved
EtoricoxibThe serum concentration of Etoricoxib can be increased when it is combined with Vemurafenib.Approved, Investigational
EtravirineThe serum concentration of Vemurafenib can be decreased when it is combined with Etravirine.Approved
EzogabineEzogabine may increase the QTc-prolonging activities of Vemurafenib.Approved
FamotidineFamotidine may increase the QTc-prolonging activities of Vemurafenib.Approved
FelbamateFelbamate may increase the QTc-prolonging activities of Vemurafenib.Approved
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Vemurafenib.Approved
FingolimodFingolimod may increase the QTc-prolonging activities of Vemurafenib.Approved, Investigational
FlecainideFlecainide may increase the QTc-prolonging activities of Vemurafenib.Approved, Withdrawn
FluconazoleFluconazole may increase the QTc-prolonging activities of Vemurafenib.Approved
FlunarizineThe serum concentration of Flunarizine can be increased when it is combined with Vemurafenib.Approved
FlunitrazepamThe serum concentration of Flunitrazepam can be increased when it is combined with Vemurafenib.Approved, Illicit
FluorouracilThe serum concentration of Fluorouracil can be increased when it is combined with Vemurafenib.Approved
FluoxetineThe serum concentration of Fluoxetine can be increased when it is combined with Vemurafenib.Approved, Vet Approved
FlupentixolFlupentixol may increase the QTc-prolonging activities of Vemurafenib.Approved, Withdrawn
FlutamideThe serum concentration of Flutamide can be increased when it is combined with Vemurafenib.Approved
FluvoxamineThe serum concentration of Fluvoxamine can be increased when it is combined with Vemurafenib.Approved, Investigational
FormoterolFormoterol may increase the QTc-prolonging activities of Vemurafenib.Approved, Investigational
FosamprenavirThe metabolism of Vemurafenib can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Vemurafenib can be increased when it is combined with Fosaprepitant.Approved
FoscarnetFoscarnet may increase the QTc-prolonging activities of Vemurafenib.Approved
FosphenytoinThe serum concentration of Vemurafenib can be decreased when it is combined with Fosphenytoin.Approved
FrovatriptanThe serum concentration of Frovatriptan can be increased when it is combined with Vemurafenib.Approved, Investigational
Fusidic AcidThe serum concentration of Vemurafenib can be increased when it is combined with Fusidic Acid.Approved
Gadobenic acidGadobenic acid may increase the QTc-prolonging activities of Vemurafenib.Approved
GalantamineGalantamine may increase the QTc-prolonging activities of Vemurafenib.Approved
GemifloxacinGemifloxacin may increase the QTc-prolonging activities of Vemurafenib.Approved, Investigational
GenisteinThe serum concentration of Genistein can be increased when it is combined with Vemurafenib.Investigational
GoserelinGoserelin may increase the QTc-prolonging activities of Vemurafenib.Approved
GranisetronGranisetron may increase the QTc-prolonging activities of Vemurafenib.Approved, Investigational
GrepafloxacinThe serum concentration of Grepafloxacin can be increased when it is combined with Vemurafenib.Withdrawn
GuanabenzThe serum concentration of Guanabenz can be increased when it is combined with Vemurafenib.Approved
HaloperidolThe serum concentration of Haloperidol can be increased when it is combined with Vemurafenib.Approved
HesperetinThe serum concentration of Hesperetin can be increased when it is combined with Vemurafenib.Approved
HexobarbitalThe serum concentration of Hexobarbital can be increased when it is combined with Vemurafenib.Approved
HistrelinHistrelin may increase the QTc-prolonging activities of Vemurafenib.Approved
HydrocodoneThe serum concentration of Hydrocodone can be decreased when it is combined with Vemurafenib.Approved, Illicit
HydroxyzineHydroxyzine may increase the QTc-prolonging activities of Vemurafenib.Approved
IbandronateIbandronate may increase the QTc-prolonging activities of Vemurafenib.Approved, Investigational
IbutilideIbutilide may increase the QTc-prolonging activities of Vemurafenib.Approved
IdelalisibThe serum concentration of Vemurafenib can be increased when it is combined with Idelalisib.Approved
IloperidoneThe serum concentration of Iloperidone can be increased when it is combined with Vemurafenib.Approved
ImatinibThe serum concentration of Imatinib can be increased when it is combined with Vemurafenib.Approved
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Vemurafenib.Approved
ImiquimodThe serum concentration of Imiquimod can be increased when it is combined with Vemurafenib.Approved, Investigational
IndacaterolIndacaterol may increase the QTc-prolonging activities of Vemurafenib.Approved
IndapamideIndapamide may increase the QTc-prolonging activities of Vemurafenib.Approved
IndinavirThe serum concentration of Vemurafenib can be increased when it is combined with Indinavir.Approved
IpilimumabIpilimumab may increase the hepatotoxic activities of Vemurafenib.Approved
IsavuconazoniumThe metabolism of Vemurafenib can be decreased when combined with Isavuconazonium.Approved, Investigational
IsofluraneIsoflurane may increase the QTc-prolonging activities of Vemurafenib.Approved, Vet Approved
IsradipineIsradipine may increase the QTc-prolonging activities of Vemurafenib.Approved
ItraconazoleThe serum concentration of Vemurafenib can be increased when it is combined with Itraconazole.Approved, Investigational
IvabradineIvabradine may increase the QTc-prolonging activities of Vemurafenib.Approved
IvacaftorThe serum concentration of Vemurafenib can be increased when it is combined with Ivacaftor.Approved
IxazomibThe serum concentration of Ixazomib can be increased when it is combined with Vemurafenib.Approved
KetoconazoleThe serum concentration of Vemurafenib can be increased when it is combined with Ketoconazole.Approved, Investigational
LapatinibLapatinib may increase the QTc-prolonging activities of Vemurafenib.Approved, Investigational
LeflunomideThe serum concentration of Leflunomide can be increased when it is combined with Vemurafenib.Approved, Investigational
LenvatinibLenvatinib may increase the QTc-prolonging activities of Vemurafenib.Approved
LeuprolideLeuprolide may increase the QTc-prolonging activities of Vemurafenib.Approved, Investigational
LevobupivacaineThe serum concentration of Levobupivacaine can be increased when it is combined with Vemurafenib.Approved
LevofloxacinLevofloxacin may increase the QTc-prolonging activities of Vemurafenib.Approved, Investigational
LidocaineThe serum concentration of Lidocaine can be increased when it is combined with Vemurafenib.Approved, Vet Approved
LithiumLithium may increase the QTc-prolonging activities of Vemurafenib.Approved
LomefloxacinThe serum concentration of Lomefloxacin can be increased when it is combined with Vemurafenib.Approved
LopinavirThe serum concentration of Vemurafenib can be increased when it is combined with Lopinavir.Approved
LorcaserinThe serum concentration of Lorcaserin can be increased when it is combined with Vemurafenib.Approved
LovastatinThe metabolism of Vemurafenib can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Vemurafenib can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Vemurafenib can be decreased when it is combined with Lumacaftor.Approved
LumefantrineLumefantrine may increase the QTc-prolonging activities of Vemurafenib.Approved
LumiracoxibThe serum concentration of Lumiracoxib can be increased when it is combined with Vemurafenib.Approved, Investigational
MalathionThe serum concentration of Malathion can be increased when it is combined with Vemurafenib.Approved, Investigational
MaprotilineThe serum concentration of Maprotiline can be increased when it is combined with Vemurafenib.Approved
MefloquineMefloquine may increase the QTc-prolonging activities of Vemurafenib.Approved
MelatoninThe serum concentration of Melatonin can be increased when it is combined with Vemurafenib.Approved, Nutraceutical, Vet Approved
MenadioneThe serum concentration of Menadione can be increased when it is combined with Vemurafenib.Approved, Nutraceutical
MephenytoinThe serum concentration of Mephenytoin can be increased when it is combined with Vemurafenib.Investigational, Withdrawn
MethadoneThe serum concentration of Methadone can be increased when it is combined with Vemurafenib.Approved
MethotrimeprazineMethotrimeprazine may increase the QTc-prolonging activities of Vemurafenib.Approved
MethoxyfluraneThe serum concentration of Methoxyflurane can be increased when it is combined with Vemurafenib.Approved, Vet Approved
MetoclopramideMetoclopramide may increase the QTc-prolonging activities of Vemurafenib.Approved, Investigational
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Vemurafenib.Approved, Investigational
MetronidazoleMetronidazole may increase the QTc-prolonging activities of Vemurafenib.Approved
MexiletineThe serum concentration of Mexiletine can be increased when it is combined with Vemurafenib.Approved
MianserinThe serum concentration of Mianserin can be increased when it is combined with Vemurafenib.Approved
MifepristoneMifepristone may increase the QTc-prolonging activities of Vemurafenib.Approved, Investigational
MirabegronMirabegron may increase the QTc-prolonging activities of Vemurafenib.Approved
MirtazapineThe serum concentration of Mirtazapine can be increased when it is combined with Vemurafenib.Approved
MitotaneThe serum concentration of Vemurafenib can be decreased when it is combined with Mitotane.Approved
ModafinilThe serum concentration of Vemurafenib can be decreased when it is combined with Modafinil.Approved, Investigational
MoexiprilMoexipril may increase the QTc-prolonging activities of Vemurafenib.Approved
MoxifloxacinMoxifloxacin may increase the QTc-prolonging activities of Vemurafenib.Approved, Investigational
muraglitazarThe serum concentration of muraglitazar can be increased when it is combined with Vemurafenib.Investigational
NabumetoneThe serum concentration of Nabumetone can be increased when it is combined with Vemurafenib.Approved
NafcillinThe serum concentration of Vemurafenib can be decreased when it is combined with Nafcillin.Approved
NaproxenThe serum concentration of Naproxen can be increased when it is combined with Vemurafenib.Approved, Vet Approved
NefazodoneThe serum concentration of Vemurafenib can be increased when it is combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Vemurafenib can be increased when it is combined with Nelfinavir.Approved
NetupitantThe serum concentration of Vemurafenib can be increased when it is combined with Netupitant.Approved
NevirapineThe serum concentration of Vemurafenib can be decreased when it is combined with Nevirapine.Approved
NicardipineNicardipine may increase the QTc-prolonging activities of Vemurafenib.Approved
NicotineThe serum concentration of Nicotine can be increased when it is combined with Vemurafenib.Approved
NifedipineThe serum concentration of Nifedipine can be increased when it is combined with Vemurafenib.Approved
NilotinibNilotinib may increase the QTc-prolonging activities of Vemurafenib.Approved, Investigational
NimodipineThe serum concentration of Nimodipine can be decreased when it is combined with Vemurafenib.Approved
Nitric OxideThe serum concentration of Nitric Oxide can be increased when it is combined with Vemurafenib.Approved
NorfloxacinNorfloxacin may increase the QTc-prolonging activities of Vemurafenib.Approved
NortriptylineThe serum concentration of Nortriptyline can be increased when it is combined with Vemurafenib.Approved
OctreotideOctreotide may increase the QTc-prolonging activities of Vemurafenib.Approved, Investigational
OfloxacinOfloxacin may increase the QTc-prolonging activities of Vemurafenib.Approved
OlanzapineThe serum concentration of Olanzapine can be increased when it is combined with Vemurafenib.Approved, Investigational
OlaparibThe metabolism of Vemurafenib can be decreased when combined with Olaparib.Approved
OlodaterolOlodaterol may increase the QTc-prolonging activities of Vemurafenib.Approved
OmeprazoleThe serum concentration of Omeprazole can be increased when it is combined with Vemurafenib.Approved, Investigational, Vet Approved
OndansetronThe serum concentration of Ondansetron can be increased when it is combined with Vemurafenib.Approved
OsimertinibThe serum concentration of Vemurafenib can be increased when it is combined with Osimertinib.Approved
OuabainOuabain may decrease the cardiotoxic activities of Vemurafenib.Approved
OxaliplatinThe serum concentration of Oxaliplatin can be increased when it is combined with Vemurafenib.Approved, Investigational
OxtriphyllineThe serum concentration of Oxtriphylline can be increased when it is combined with Vemurafenib.Approved
OxytocinOxytocin may increase the QTc-prolonging activities of Vemurafenib.Approved, Vet Approved
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Vemurafenib.Approved, Vet Approved
PalbociclibThe serum concentration of Vemurafenib can be increased when it is combined with Palbociclib.Approved
PaliperidonePaliperidone may increase the QTc-prolonging activities of Vemurafenib.Approved
PalonosetronThe serum concentration of Palonosetron can be increased when it is combined with Vemurafenib.Approved, Investigational
PanobinostatPanobinostat may increase the QTc-prolonging activities of Vemurafenib.Approved, Investigational
PantoprazoleThe serum concentration of Pantoprazole can be increased when it is combined with Vemurafenib.Approved
ParoxetineParoxetine may increase the QTc-prolonging activities of Vemurafenib.Approved, Investigational
PasireotidePasireotide may increase the QTc-prolonging activities of Vemurafenib.Approved
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Vemurafenib.Approved
PentamidineThe serum concentration of Pentamidine can be increased when it is combined with Vemurafenib.Approved
PentobarbitalThe serum concentration of Vemurafenib can be decreased when it is combined with Pentobarbital.Approved, Vet Approved
PentoxifyllineThe serum concentration of Pentoxifylline can be increased when it is combined with Vemurafenib.Approved, Investigational
PerflutrenPerflutren may increase the QTc-prolonging activities of Vemurafenib.Approved
PerphenazineThe serum concentration of Perphenazine can be increased when it is combined with Vemurafenib.Approved
PhenacetinThe serum concentration of Phenacetin can be increased when it is combined with Vemurafenib.Withdrawn
PhenobarbitalThe serum concentration of Vemurafenib can be decreased when it is combined with Phenobarbital.Approved
PhenytoinThe serum concentration of Vemurafenib can be decreased when it is combined with Phenytoin.Approved, Vet Approved
PimozideThe serum concentration of Pimozide can be increased when it is combined with Vemurafenib.Approved
PipotiazineThe serum concentration of Pipotiazine can be increased when it is combined with Vemurafenib.Approved
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Vemurafenib.Approved
PosaconazoleThe serum concentration of Vemurafenib can be increased when it is combined with Posaconazole.Approved, Investigational, Vet Approved
PraziquantelThe serum concentration of Praziquantel can be increased when it is combined with Vemurafenib.Approved, Vet Approved
PrimaquineThe serum concentration of Primaquine can be increased when it is combined with Vemurafenib.Approved
PrimidoneThe serum concentration of Vemurafenib can be decreased when it is combined with Primidone.Approved, Vet Approved
ProcainamideProcainamide may increase the QTc-prolonging activities of Vemurafenib.Approved
ProgesteroneThe serum concentration of Progesterone can be increased when it is combined with Vemurafenib.Approved, Vet Approved
ProguanilThe serum concentration of Proguanil can be increased when it is combined with Vemurafenib.Approved
PromazineThe serum concentration of Promazine can be increased when it is combined with Vemurafenib.Approved, Vet Approved
PromethazinePromethazine may increase the QTc-prolonging activities of Vemurafenib.Approved
PropafenoneThe serum concentration of Propafenone can be increased when it is combined with Vemurafenib.Approved
PropofolThe serum concentration of Propofol can be increased when it is combined with Vemurafenib.Approved, Investigational, Vet Approved
PropranololThe serum concentration of Propranolol can be increased when it is combined with Vemurafenib.Approved, Investigational
ProtriptylineProtriptyline may increase the QTc-prolonging activities of Vemurafenib.Approved
PyrazinamideThe serum concentration of Pyrazinamide can be increased when it is combined with Vemurafenib.Approved
QuetiapineQuetiapine may increase the QTc-prolonging activities of Vemurafenib.Approved
QuinidineQuinidine may increase the QTc-prolonging activities of Vemurafenib.Approved
QuinineThe serum concentration of Quinine can be increased when it is combined with Vemurafenib.Approved
RamelteonThe serum concentration of Ramelteon can be increased when it is combined with Vemurafenib.Approved, Investigational
RanitidineThe serum concentration of Ranitidine can be increased when it is combined with Vemurafenib.Approved
RanolazineRanolazine may increase the QTc-prolonging activities of Vemurafenib.Approved, Investigational
RasagilineThe serum concentration of Rasagiline can be increased when it is combined with Vemurafenib.Approved
ResveratrolThe serum concentration of Resveratrol can be increased when it is combined with Vemurafenib.Experimental, Investigational
RifabutinThe serum concentration of Vemurafenib can be decreased when it is combined with Rifabutin.Approved
RifampicinThe serum concentration of Vemurafenib can be decreased when it is combined with Rifampicin.Approved
RifapentineThe serum concentration of Vemurafenib can be decreased when it is combined with Rifapentine.Approved
RilpivirineRilpivirine may increase the QTc-prolonging activities of Vemurafenib.Approved
RiluzoleThe serum concentration of Riluzole can be increased when it is combined with Vemurafenib.Approved, Investigational
RisperidoneRisperidone may increase the QTc-prolonging activities of Vemurafenib.Approved, Investigational
RitonavirThe serum concentration of Vemurafenib can be increased when it is combined with Ritonavir.Approved, Investigational
RizatriptanThe serum concentration of Rizatriptan can be increased when it is combined with Vemurafenib.Approved
RofecoxibThe serum concentration of Rofecoxib can be increased when it is combined with Vemurafenib.Investigational, Withdrawn
RolapitantThe serum concentration of Vemurafenib can be increased when it is combined with Rolapitant.Approved
RopiniroleThe serum concentration of Ropinirole can be increased when it is combined with Vemurafenib.Approved, Investigational
RopivacaineThe serum concentration of Ropivacaine can be increased when it is combined with Vemurafenib.Approved
RotigotineThe serum concentration of Rotigotine can be increased when it is combined with Vemurafenib.Approved
SalbutamolSalbutamol may increase the QTc-prolonging activities of Vemurafenib.Approved, Vet Approved
SalmeterolSalmeterol may increase the QTc-prolonging activities of Vemurafenib.Approved
SaquinavirThe serum concentration of Vemurafenib can be increased when it is combined with Saquinavir.Approved, Investigational
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Vemurafenib.Approved
SelegilineThe serum concentration of Selegiline can be increased when it is combined with Vemurafenib.Approved, Investigational, Vet Approved
SertralineThe serum concentration of Sertraline can be increased when it is combined with Vemurafenib.Approved
SevofluraneSevoflurane may increase the QTc-prolonging activities of Vemurafenib.Approved, Vet Approved
SildenafilThe metabolism of Vemurafenib can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Vemurafenib can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Vemurafenib can be increased when it is combined with Simeprevir.Approved
SolifenacinSolifenacin may increase the QTc-prolonging activities of Vemurafenib.Approved
SorafenibSorafenib may increase the QTc-prolonging activities of Vemurafenib.Approved, Investigational
SotalolSotalol may increase the QTc-prolonging activities of Vemurafenib.Approved
St. John's WortThe serum concentration of Vemurafenib can be decreased when it is combined with St. John's Wort.Nutraceutical
StiripentolThe serum concentration of Vemurafenib can be increased when it is combined with Stiripentol.Approved
SulfamethoxazoleSulfamethoxazole may increase the QTc-prolonging activities of Vemurafenib.Approved
SulfisoxazoleSulfisoxazole may increase the QTc-prolonging activities of Vemurafenib.Approved, Vet Approved
SunitinibSunitinib may increase the QTc-prolonging activities of Vemurafenib.Approved, Investigational
TacrineThe serum concentration of Tacrine can be increased when it is combined with Vemurafenib.Withdrawn
TamoxifenThe serum concentration of Tamoxifen can be increased when it is combined with Vemurafenib.Approved
TelaprevirThe serum concentration of Vemurafenib can be increased when it is combined with Telaprevir.Approved
TelavancinTelavancin may increase the QTc-prolonging activities of Vemurafenib.Approved
TelithromycinThe serum concentration of Vemurafenib can be increased when it is combined with Telithromycin.Approved
TemafloxacinThe serum concentration of Temafloxacin can be increased when it is combined with Vemurafenib.Withdrawn
TerbinafineThe serum concentration of Terbinafine can be increased when it is combined with Vemurafenib.Approved, Investigational, Vet Approved
TerbutalineTerbutaline may increase the QTc-prolonging activities of Vemurafenib.Approved
TeriflunomideThe serum concentration of Vemurafenib can be increased when it is combined with Teriflunomide.Approved
TetrabenazineTetrabenazine may increase the QTc-prolonging activities of Vemurafenib.Approved
ThalidomideThe serum concentration of Thalidomide can be increased when it is combined with Vemurafenib.Approved, Investigational, Withdrawn
TheobromineThe serum concentration of Theobromine can be increased when it is combined with Vemurafenib.Approved
TheophyllineThe serum concentration of Theophylline can be increased when it is combined with Vemurafenib.Approved
ThiabendazoleThe serum concentration of Thiabendazole can be increased when it is combined with Vemurafenib.Approved, Vet Approved
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Vemurafenib.Approved
ThiothixeneThe serum concentration of Thiothixene can be increased when it is combined with Vemurafenib.Approved
TiclopidineThe metabolism of Vemurafenib can be decreased when combined with Ticlopidine.Approved
TizanidineThe serum concentration of Tizanidine can be increased when it is combined with Vemurafenib.Approved
TocilizumabThe serum concentration of Vemurafenib can be decreased when it is combined with Tocilizumab.Approved
TolterodineTolterodine may increase the QTc-prolonging activities of Vemurafenib.Approved, Investigational
ToremifeneThe serum concentration of Toremifene can be increased when it is combined with Vemurafenib.Approved, Investigational
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Vemurafenib.Approved, Investigational
TrazodoneTrazodone may increase the QTc-prolonging activities of Vemurafenib.Approved, Investigational
TreprostinilTreprostinil may increase the QTc-prolonging activities of Vemurafenib.Approved, Investigational
TriamtereneThe serum concentration of Triamterene can be increased when it is combined with Vemurafenib.Approved
TrifluoperazineThe serum concentration of Trifluoperazine can be increased when it is combined with Vemurafenib.Approved
TrimethoprimTrimethoprim may increase the QTc-prolonging activities of Vemurafenib.Approved, Vet Approved
TrimipramineTrimipramine may increase the QTc-prolonging activities of Vemurafenib.Approved
TriptorelinTriptorelin may increase the QTc-prolonging activities of Vemurafenib.Approved, Vet Approved
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Vemurafenib.Approved
VandetanibVandetanib may increase the QTc-prolonging activities of Vemurafenib.Approved
VardenafilVardenafil may increase the QTc-prolonging activities of Vemurafenib.Approved
VenlafaxineVenlafaxine may increase the QTc-prolonging activities of Vemurafenib.Approved
VerapamilThe serum concentration of Verapamil can be increased when it is combined with Vemurafenib.Approved
VilanterolVilanterol may increase the QTc-prolonging activities of Vemurafenib.Approved
VoriconazoleThe serum concentration of Vemurafenib can be increased when it is combined with Voriconazole.Approved, Investigational
VorinostatVorinostat may increase the QTc-prolonging activities of Vemurafenib.Approved, Investigational
WarfarinThe serum concentration of Warfarin can be increased when it is combined with Vemurafenib.Approved
ZileutonThe serum concentration of Zileuton can be increased when it is combined with Vemurafenib.Approved, Investigational, Withdrawn
ZiprasidoneThe serum concentration of Ziprasidone can be increased when it is combined with Vemurafenib.Approved
ZolmitriptanThe serum concentration of Zolmitriptan can be increased when it is combined with Vemurafenib.Approved, Investigational
ZolpidemThe serum concentration of Zolpidem can be increased when it is combined with Vemurafenib.Approved
ZuclopenthixolZuclopenthixol may increase the QTc-prolonging activities of Vemurafenib.Approved, Investigational
Food InteractionsNot 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)
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
TabletOral240 mg
Tablet, film coatedOral240 mg/1
Tablet, film coatedOral240 mg
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
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

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 ]
Comments
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Drug created on May 20, 2013 00:41 / Updated on December 03, 2016 02:46