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Identification
NameSorafenib
Accession NumberDB00398  (APRD01304, DB07438)
TypeSmall Molecule
GroupsApproved, Investigational
DescriptionSorafenib (rINN), marketed as Nexavar by Bayer, is a drug approved for the treatment of advanced renal cell carcinoma (primary kidney cancer). It has also received "Fast Track" designation by the FDA for the treatment of advanced hepatocellular carcinoma (primary liver cancer), and has since performed well in Phase III trials. Sorafenib is a small molecular inhibitor of Raf kinase, PDGF (platelet-derived growth factor), VEGF receptor 2 & 3 kinases and c Kit the receptor for Stem cell factor. A growing number of drugs target most of these pathways. The originality of Sorafenib lays in its simultaneous targeting of the Raf/Mek/Erk pathway.
Structure
Thumb
Synonyms
4-(4-((((4-Chloro-3-(trifluoromethyl)phenyl)amino)carbonyl)amino)phenoxy)-N-methyl-2-pyridinecarboxamide
N-(4-Chloro-3-(trifluoromethyl)phenyl)-n'-(4-(2-(N-methylcarbamoyl)-4-pyridyloxy)phenyl)urea
Sorafenibum
External Identifiers
  • BAY 43-9006
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
NexavarTablet, film coated200 mg/1OralBayer Health Care Pharmaceuticals Inc.2005-12-20Not applicableUs
NexavarTablet200 mgOralBayer Inc2006-07-31Not applicableCanada
NexavarTablet, film coated200 mgOralBayer Pharma Ag2006-07-19Not applicableEu
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Sorafenib Tosylate
475207-59-1
Thumb
  • InChI Key: IVDHYUQIDRJSTI-UHFFFAOYSA-N
  • Monoisotopic Mass: 636.105717532
  • Average Mass: 637.027
DBSALT000165
Categories
UNII9ZOQ3TZI87
CAS number284461-73-0
WeightAverage: 464.825
Monoisotopic: 464.08630272
Chemical FormulaC21H16ClF3N4O3
InChI KeyMLDQJTXFUGDVEO-UHFFFAOYSA-N
InChI
InChI=1S/C21H16ClF3N4O3/c1-26-19(30)18-11-15(8-9-27-18)32-14-5-2-12(3-6-14)28-20(31)29-13-4-7-17(22)16(10-13)21(23,24)25/h2-11H,1H3,(H,26,30)(H2,28,29,31)
IUPAC Name
4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)phenoxy]-N-methylpyridine-2-carboxamide
SMILES
CNC(=O)C1=NC=CC(OC2=CC=C(NC(=O)NC3=CC(=C(Cl)C=C3)C(F)(F)F)C=C2)=C1
Pharmacology
IndicationSorafenib is indicated for the treatment of unresectable hepatocellular carcinoma and advanced renal cell carcinoma.
Structured Indications
PharmacodynamicsNo large changes in QTc interval were observed. After one 28-day treatment cycle, the largest mean QTc interval change of 8.5 ms (upper bound of two-sided 90% confidence interval, 13.3 ms) was observed at 6 hours post-dose on day 1 of cycle 2.
Mechanism of actionSorafenib interacts with multiple intracellular (CRAF, BRAF and mutant BRAF) and cell surface kinases (KIT, FLT-3, VEGFR-2, VEGFR-3, and PDGFR-ß). Several of these kinases are thought to be involved in angiogenesis, thus sorafenib reduces blood flow to the tumor. Sorafenib is unique in targeting the Raf/Mek/Erk pathway. By inhibiting these kinases, genetic transcription involving cell proliferation and angiogenesis is inhibited.
TargetKindPharmacological actionActionsOrganismUniProt ID
Serine/threonine-protein kinase B-rafProteinyes
inhibitor
HumanP15056 details
RAF proto-oncogene serine/threonine-protein kinaseProteinyes
inhibitor
HumanP04049 details
Vascular endothelial growth factor receptor 3Proteinyes
antagonist
HumanP35916 details
Vascular endothelial growth factor receptor 2Proteinyes
antagonist
HumanP35968 details
Receptor-type tyrosine-protein kinase FLT3Proteinyes
antagonist
HumanP36888 details
Platelet-derived growth factor receptor betaProteinyes
antagonist
HumanP09619 details
Mast/stem cell growth factor receptor KitProteinyes
antagonist
HumanP10721 details
Fibroblast growth factor receptor 1Proteinyes
inhibitor
HumanP11362 details
Proto-oncogene tyrosine-protein kinase receptor RetProteinyes
inhibitor
HumanP07949 details
Vascular endothelial growth factor receptor 1Proteinyes
inhibitor
HumanP17948 details
Related Articles
AbsorptionThe mean relative bioavailability is 38-49% for the tablet form, when compared to an oral solution. Sorafenib reached peak plasma levels in 3 hours following oral administration. With a high-fat meal, bioavailability is reduced by 29% compared to administration in the fasted state.
Volume of distributionNot Available
Protein binding99.5% bound to plasma proteins.
Metabolism

Sorafenib is metabolized primarily in the liver, undergoing oxidative metabolism, mediated by CYP3A4, as well as glucuronidation mediated by UGT1A9. Sorafenib accounts for approximately 70-85% of the circulating analytes in plasma at steady- state. Eight metabolites of sorafenib have been identified, of which five have been detected in plasma. The main circulating metabolite of sorafenib in plasma, the pyridine N-oxide, shows in vitro potency similar to that of sorafenib. This metabolite comprises approximately 9-16% of circulating analytes at steady-state.

SubstrateEnzymesProduct
Sorafenib
Pyridine N-oxideDetails
Sorafenib
Not Available
Pyridine N-oxide glucuronideDetails
Sorafenib
Sorafenib beta-D-GlucuronideDetails
Route of eliminationFollowing oral administration of a 100 mg dose of a solution formulation of sorafenib, 96% of the dose was recovered within 14 days, with 77% of the dose excreted in feces, and 19% of the dose excreted in urine as glucuronidated metabolites.
Half life25-48 hours
ClearanceNot Available
ToxicityThe highest dose of sorafenib studied clinically is 800 mg twice daily. The adverse reactions observed at this dose were primarily diarrhea and dermatologic events. No information is available on symptoms of acute overdose in animals because of the saturation of absorption in oral acute toxicity studies conducted in animals.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Sorafenib Metabolism PathwayDrug metabolismSMP00648
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
AbirateroneThe serum concentration of Sorafenib can be increased when it is combined with Abiraterone.Approved
AcebutololThe serum concentration of Acebutolol can be increased when it is combined with Sorafenib.Approved
AceclofenacThe metabolism of Aceclofenac can be decreased when combined with Sorafenib.Approved
AcenocoumarolThe metabolism of Acenocoumarol can be decreased when combined with Sorafenib.Approved
AcetaminophenAcetaminophen may increase the hepatotoxic activities of Sorafenib.Approved
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Sorafenib.Approved
Acetylsalicylic acidThe serum concentration of Acetylsalicylic acid can be increased when it is combined with Sorafenib.Approved, Vet Approved
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Sorafenib.Approved
AlbendazoleThe serum concentration of Sorafenib can be increased when it is combined with Albendazole.Approved, Vet Approved
AldosteroneThe serum concentration of Sorafenib can be decreased when it is combined with Aldosterone.Experimental
AlectinibThe serum concentration of Sorafenib can be increased when it is combined with Alectinib.Approved
AlfentanilThe serum concentration of Sorafenib can be increased when it is combined with Alfentanil.Approved, Illicit
AlitretinoinThe serum concentration of Alitretinoin can be increased when it is combined with Sorafenib.Approved, Investigational
AlosetronThe metabolism of Alosetron can be decreased when combined with Sorafenib.Approved, Withdrawn
AlprazolamThe metabolism of Alprazolam can be decreased when combined with Sorafenib.Approved, Illicit, Investigational
ALT-110The risk or severity of adverse effects can be increased when Sorafenib is combined with ALT-110.Investigational
AmantadineThe serum concentration of Sorafenib can be increased when it is combined with Amantadine.Approved
AmbrisentanThe serum concentration of Ambrisentan can be increased when it is combined with Sorafenib.Approved, Investigational
Aminohippuric acidThe serum concentration of Sorafenib can be increased when it is combined with Aminohippuric acid.Approved
AminophenazoneThe metabolism of Aminophenazone can be decreased when combined with Sorafenib.Approved, Withdrawn
AmiodaroneThe serum concentration of Sorafenib can be increased when it is combined with Amiodarone.Approved, Investigational
AmitriptylineThe serum concentration of Sorafenib can be increased when it is combined with Amitriptyline.Approved
AmlodipineThe serum concentration of Sorafenib can be increased when it is combined with Amlodipine.Approved
AmodiaquineThe serum concentration of Amodiaquine can be increased when it is combined with Sorafenib.Approved
AmprenavirThe serum concentration of Sorafenib can be decreased when it is combined with Amprenavir.Approved
AmsacrineThe serum concentration of Sorafenib can be increased when it is combined with Amsacrine.Approved
AnagrelideSorafenib may increase the QTc-prolonging activities of Anagrelide.Approved
AntipyrineThe metabolism of Antipyrine can be decreased when combined with Sorafenib.Approved
AnvirzelAnvirzel may decrease the cardiotoxic activities of Sorafenib.Investigational
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Sorafenib.Approved
AprepitantThe serum concentration of Sorafenib can be increased when it is combined with Aprepitant.Approved, Investigational
Arachidonic AcidThe metabolism of Arachidonic Acid can be decreased when combined with Sorafenib.Experimental
ArformoterolThe metabolism of Arformoterol can be decreased when combined with Sorafenib.Approved, Investigational
Arsenic trioxideSorafenib may increase the QTc-prolonging activities of Arsenic trioxide.Approved, Investigational
ArtemetherSorafenib may increase the QTc-prolonging activities of Artemether.Approved
AsenapineSorafenib may increase the QTc-prolonging activities of Asenapine.Approved
AstemizoleThe serum concentration of Sorafenib can be increased when it is combined with Astemizole.Approved, Withdrawn
AtazanavirThe serum concentration of Sorafenib can be increased when it is combined with Atazanavir.Approved, Investigational
AtenololThe serum concentration of Sorafenib can be increased when it is combined with Atenolol.Approved
AtomoxetineThe metabolism of Sorafenib can be decreased when combined with Atomoxetine.Approved
AtorvastatinThe serum concentration of Sorafenib can be increased when it is combined with Atorvastatin.Approved
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Sorafenib.Approved, Investigational
AzelastineThe serum concentration of Sorafenib can be increased when it is combined with Azelastine.Approved
AzithromycinSorafenib may increase the QTc-prolonging activities of Azithromycin.Approved
BanoxantroneThe metabolism of Banoxantrone can be decreased when combined with Sorafenib.Investigational
BcgThe therapeutic efficacy of Bcg can be decreased when used in combination with Sorafenib.Investigational
BedaquilineSorafenib may increase the QTc-prolonging activities of Bedaquiline.Approved
BenzocaineThe serum concentration of Sorafenib can be increased when it is combined with Benzocaine.Approved
BenzphetamineThe metabolism of Benzphetamine can be decreased when combined with Sorafenib.Approved, Illicit
Benzyl alcoholThe metabolism of Benzyl alcohol can be decreased when combined with Sorafenib.Approved
BepridilThe serum concentration of Sorafenib can be increased when it is combined with Bepridil.Approved, Withdrawn
BetamethasoneThe serum concentration of Betamethasone can be increased when it is combined with Sorafenib.Approved, Vet Approved
BevacizumabThe risk or severity of adverse effects can be increased when Bevacizumab is combined with Sorafenib.Approved, Investigational
BexaroteneThe serum concentration of Sorafenib can be decreased when it is combined with Bexarotene.Approved, Investigational
BiperidenThe serum concentration of Sorafenib can be increased when it is combined with Biperiden.Approved
BoceprevirThe serum concentration of Sorafenib can be increased when it is combined with Boceprevir.Approved
BortezomibThe metabolism of Sorafenib can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Bosentan can be increased when it is combined with Sorafenib.Approved, Investigational
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Sorafenib.Approved
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Sorafenib.Approved
BromocriptineThe serum concentration of Sorafenib can be increased when it is combined with Bromocriptine.Approved, Investigational
BrompheniramineThe metabolism of Brompheniramine can be decreased when combined with Sorafenib.Approved
BuprenorphineThe serum concentration of Sorafenib can be increased when it is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BupropionThe serum concentration of Bupropion can be increased when it is combined with Sorafenib.Approved
BuspironeThe serum concentration of Sorafenib can be increased when it is combined with Buspirone.Approved, Investigational
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Sorafenib.Approved
CabozantinibThe metabolism of Cabozantinib can be decreased when combined with Sorafenib.Approved
CaffeineThe serum concentration of Sorafenib can be increased when it is combined with Caffeine.Approved
CamptothecinThe serum concentration of Camptothecin can be increased when it is combined with Sorafenib.Experimental
CanagliflozinThe serum concentration of Canagliflozin can be increased when it is combined with Sorafenib.Approved
CandesartanThe serum concentration of Sorafenib can be increased when it is combined with Candesartan.Approved
CaptoprilThe serum concentration of Sorafenib can be increased when it is combined with Captopril.Approved
CarbamazepineThe serum concentration of Sorafenib can be decreased when it is combined with Carbamazepine.Approved, Investigational
CarbinoxamineThe metabolism of Carbinoxamine can be decreased when combined with Sorafenib.Approved
CarboplatinThe risk or severity of adverse effects can be increased when Sorafenib is combined with Carboplatin.Approved
CarfilzomibThe serum concentration of Carfilzomib can be increased when it is combined with Sorafenib.Approved
CarvedilolThe serum concentration of Carvedilol can be increased when it is combined with Sorafenib.Approved, Investigational
CaspofunginThe serum concentration of Sorafenib can be increased when it is combined with Caspofungin.Approved
CDX-110The risk or severity of adverse effects can be increased when Sorafenib is combined with CDX-110.Investigational
CelecoxibThe metabolism of Celecoxib can be decreased when combined with Sorafenib.Approved, Investigational
CeritinibThe serum concentration of Sorafenib can be increased when it is combined with Ceritinib.Approved
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Sorafenib.Withdrawn
ChloroquineSorafenib may increase the QTc-prolonging activities of Chloroquine.Approved, Vet Approved
ChlorpromazineSorafenib may increase the QTc-prolonging activities of Chlorpromazine.Approved, Vet Approved
ChlorpropamideThe serum concentration of Sorafenib can be increased when it is combined with Chlorpropamide.Approved
ChlorprothixeneThe serum concentration of Sorafenib can be increased when it is combined with Chlorprothixene.Approved, Withdrawn
CholesterolThe serum concentration of Sorafenib can be increased when it is combined with Cholesterol.Experimental
Cholic AcidThe serum concentration of Sorafenib can be decreased when it is combined with Cholic Acid.Approved
CilazaprilThe serum concentration of Sorafenib can be increased when it is combined with Cilazapril.Approved
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Sorafenib.Approved
CimetidineThe serum concentration of Sorafenib can be decreased when it is combined with Cimetidine.Approved
CinnarizineThe metabolism of Cinnarizine can be decreased when combined with Sorafenib.Approved
CiprofloxacinSorafenib may increase the QTc-prolonging activities of Ciprofloxacin.Approved, Investigational
CisaprideSorafenib may increase the QTc-prolonging activities of Cisapride.Approved, Investigational, Withdrawn
CisplatinThe serum concentration of Cisplatin can be increased when it is combined with Sorafenib.Approved
CitalopramSorafenib may increase the QTc-prolonging activities of Citalopram.Approved
ClarithromycinThe serum concentration of Sorafenib can be increased when it is combined with Clarithromycin.Approved
ClemastineThe metabolism of Sorafenib can be decreased when combined with Clemastine.Approved
ClobazamThe serum concentration of Clobazam can be increased when it is combined with Sorafenib.Approved, Illicit
ClofazimineThe serum concentration of Sorafenib can be increased when it is combined with Clofazimine.Approved, Investigational
clomethiazoleThe metabolism of clomethiazole can be decreased when combined with Sorafenib.Investigational
ClomifeneThe serum concentration of Clomifene can be increased when it is combined with Sorafenib.Approved, Investigational
ClomipramineThe serum concentration of Sorafenib can be increased when it is combined with Clomipramine.Approved, Vet Approved
ClonidineThe serum concentration of Clonidine can be increased when it is combined with Sorafenib.Approved
ClopidogrelThe metabolism of Sorafenib can be decreased when combined with Clopidogrel.Approved, Nutraceutical
ClotiazepamThe metabolism of Clotiazepam can be decreased when combined with Sorafenib.Approved, Illicit
ClotrimazoleThe metabolism of Sorafenib can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe risk or severity of adverse effects can be increased when Sorafenib is combined with Clozapine.Approved
CobicistatThe serum concentration of Sorafenib can be increased when it is combined with Cobicistat.Approved
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Sorafenib.Approved
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Sorafenib.Approved
ColforsinThe serum concentration of Sorafenib can be increased when it is combined with Colforsin.Experimental
ConivaptanThe serum concentration of Sorafenib 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 Sorafenib.Approved
CrizotinibSorafenib may increase the QTc-prolonging activities of Crizotinib.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Sorafenib.Approved, Investigational
CyclosporineThe metabolism of Sorafenib can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Sorafenib.Approved
DabrafenibThe serum concentration of Sorafenib can be decreased when it is combined with Dabrafenib.Approved
DacarbazineThe serum concentration of Dacarbazine can be decreased when it is combined with Sorafenib.Approved, Investigational
DaclatasvirThe serum concentration of Sorafenib can be increased when it is combined with Daclatasvir.Approved
DactinomycinThe serum concentration of Sorafenib can be increased when it is combined with Dactinomycin.Approved
DapagliflozinThe serum concentration of Dapagliflozin can be increased when it is combined with Sorafenib.Approved
DapsoneThe metabolism of Dapsone can be decreased when combined with Sorafenib.Approved, Investigational
DarunavirThe serum concentration of Sorafenib can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Sorafenib can be increased when it is combined with Dasatinib.Approved, Investigational
DaunorubicinThe serum concentration of Sorafenib can be decreased when it is combined with Daunorubicin.Approved
DebrisoquinThe serum concentration of Debrisoquin can be increased when it is combined with Sorafenib.Approved
DeferasiroxThe serum concentration of Sorafenib can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Sorafenib can be decreased when combined with Delavirdine.Approved
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Sorafenib.Approved
DesipramineThe serum concentration of Sorafenib can be increased when it is combined with Desipramine.Approved
DeslanosideDeslanoside may decrease the cardiotoxic activities of Sorafenib.Approved
DesloratadineThe serum concentration of Sorafenib can be increased when it is combined with Desloratadine.Approved, Investigational
DexamethasoneThe serum concentration of Sorafenib can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DextromethorphanThe serum concentration of Sorafenib can be increased when it is combined with Dextromethorphan.Approved
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Sorafenib.Approved, Illicit, Vet Approved
DiclofenacThe serum concentration of Sorafenib can be increased when it is combined with Diclofenac.Approved, Vet Approved
DicoumarolThe metabolism of Dicoumarol can be decreased when combined with Sorafenib.Approved
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be increased when it is combined with Sorafenib.Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Sorafenib.Approved
DigoxinDigoxin may decrease the cardiotoxic activities of Sorafenib.Approved
DihydroergotamineThe metabolism of Sorafenib can be decreased when combined with Dihydroergotamine.Approved
DihydrotestosteroneThe serum concentration of Dihydrotestosterone can be increased when it is combined with Sorafenib.Illicit
DiltiazemThe metabolism of Sorafenib can be decreased when combined with Diltiazem.Approved
DiphenhydramineThe metabolism of Diphenhydramine can be decreased when combined with Sorafenib.Approved
DipyridamoleThe serum concentration of Sorafenib can be increased when it is combined with Dipyridamole.Approved
DisopyramideSorafenib may increase the QTc-prolonging activities of Disopyramide.Approved
DocetaxelThe serum concentration of Docetaxel can be increased when it is combined with Sorafenib.Approved, Investigational
DofetilideSorafenib may increase the QTc-prolonging activities of Dofetilide.Approved
DolasetronSorafenib may increase the QTc-prolonging activities of Dolasetron.Approved
DomperidoneSorafenib may increase the QTc-prolonging activities of Domperidone.Approved, Investigational, Vet Approved
DonepezilThe metabolism of Donepezil can be decreased when combined with Sorafenib.Approved
DopamineThe metabolism of Dopamine can be decreased when combined with Sorafenib.Approved
DorzolamideThe metabolism of Dorzolamide can be decreased when combined with Sorafenib.Approved
DoxazosinThe serum concentration of Sorafenib can be increased when it is combined with Doxazosin.Approved
DoxepinThe serum concentration of Sorafenib can be increased when it is combined with Doxepin.Approved
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Sorafenib.Approved, Investigational
DoxorubicinThe serum concentration of Sorafenib can be decreased when it is combined with Doxorubicin.Approved, Investigational
DoxycyclineThe metabolism of Sorafenib can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronabinolThe serum concentration of Dronabinol can be increased when it is combined with Sorafenib.Approved, Illicit
DronedaroneSorafenib may increase the QTc-prolonging activities of Dronedarone.Approved
DroperidolSorafenib may increase the QTc-prolonging activities of Droperidol.Approved, Vet Approved
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Sorafenib.Approved
EfavirenzThe serum concentration of Sorafenib can be decreased when it is combined with Efavirenz.Approved, Investigational
ElbasvirThe serum concentration of Sorafenib can be increased when it is combined with Elbasvir.Approved
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Sorafenib.Approved, Investigational
EliglustatSorafenib may increase the QTc-prolonging activities of Eliglustat.Approved
EltrombopagThe serum concentration of Sorafenib can be increased when it is combined with Eltrombopag.Approved
EnalaprilThe serum concentration of Sorafenib can be increased when it is combined with Enalapril.Approved, Vet Approved
EnzalutamideThe serum concentration of Sorafenib can be decreased when it is combined with Enzalutamide.Approved
EpinastineThe serum concentration of Epinastine can be increased when it is combined with Sorafenib.Approved, Investigational
EpoprostenolThe metabolism of Epoprostenol can be decreased when combined with Sorafenib.Approved
ErgonovineThe serum concentration of Sorafenib can be increased when it is combined with Ergonovine.Approved
ErgotamineThe serum concentration of Sorafenib can be increased when it is combined with Ergotamine.Approved
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Sorafenib.Approved, Investigational
ErythromycinSorafenib may increase the QTc-prolonging activities of Erythromycin.Approved, Vet Approved
EscitalopramSorafenib may increase the QTc-prolonging activities of Escitalopram.Approved, Investigational
Eslicarbazepine acetateThe serum concentration of Sorafenib can be decreased when it is combined with Eslicarbazepine acetate.Approved
EstradiolThe serum concentration of Estradiol can be increased when it is combined with Sorafenib.Approved, Investigational, Vet Approved
EstramustineThe serum concentration of Sorafenib can be increased when it is combined with Estramustine.Approved
EstriolThe serum concentration of Sorafenib can be decreased when it is combined with Estriol.Approved, Vet Approved
EstroneThe serum concentration of Sorafenib can be decreased when it is combined with Estrone.Approved
EszopicloneThe metabolism of Eszopiclone can be decreased when combined with Sorafenib.Approved
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be increased when it is combined with Sorafenib.Approved
EthylmorphineThe metabolism of Ethylmorphine can be decreased when combined with Sorafenib.Approved, Illicit
EtodolacThe metabolism of Etodolac can be decreased when combined with Sorafenib.Approved, Investigational, Vet Approved
EtoposideThe serum concentration of Sorafenib can be increased when it is combined with Etoposide.Approved
EtoricoxibThe metabolism of Etoricoxib can be decreased when combined with Sorafenib.Approved, Investigational
EtravirineThe serum concentration of Sorafenib can be decreased when it is combined with Etravirine.Approved
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Sorafenib.Approved
EzetimibeThe serum concentration of Ezetimibe can be increased when it is combined with Sorafenib.Approved
FelodipineThe serum concentration of Sorafenib can be increased when it is combined with Felodipine.Approved, Investigational
FentanylThe serum concentration of Sorafenib can be increased when it is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Sorafenib.Approved
FexofenadineThe serum concentration of Sorafenib can be increased when it is combined with Fexofenadine.Approved
FidaxomicinThe serum concentration of Fidaxomicin can be increased when it is combined with Sorafenib.Approved
FingolimodSorafenib may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
FlecainideSorafenib may increase the QTc-prolonging activities of Flecainide.Approved, Withdrawn
FluconazoleThe metabolism of Sorafenib can be decreased when combined with Fluconazole.Approved
FlunarizineThe metabolism of Flunarizine can be decreased when combined with Sorafenib.Approved
FlunitrazepamThe metabolism of Flunitrazepam can be decreased when combined with Sorafenib.Approved, Illicit
FluorouracilThe serum concentration of Fluorouracil can be decreased when it is combined with Sorafenib.Approved
FluoxetineSorafenib may increase the QTc-prolonging activities of Fluoxetine.Approved, Vet Approved
FlupentixolSorafenib may increase the QTc-prolonging activities of Flupentixol.Approved, Withdrawn
FluphenazineThe serum concentration of Sorafenib can be increased when it is combined with Fluphenazine.Approved
FlurazepamThe serum concentration of Sorafenib can be increased when it is combined with Flurazepam.Approved, Illicit
FlurbiprofenThe metabolism of Flurbiprofen can be decreased when combined with Sorafenib.Approved, Investigational
Fluticasone furoateThe serum concentration of Fluticasone furoate can be increased when it is combined with Sorafenib.Approved
FluvastatinThe metabolism of Fluvastatin can be decreased when combined with Sorafenib.Approved
FluvoxamineThe metabolism of Sorafenib can be decreased when combined with Fluvoxamine.Approved, Investigational
FormoterolThe metabolism of Formoterol can be decreased when combined with Sorafenib.Approved, Investigational
FosamprenavirThe metabolism of Sorafenib can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Sorafenib can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe serum concentration of Sorafenib can be decreased when it is combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Sorafenib can be increased when it is combined with Fusidic Acid.Approved
G17DTThe risk or severity of adverse effects can be increased when Sorafenib is combined with G17DT.Investigational
Gadobenic acidSorafenib may increase the QTc-prolonging activities of Gadobenic acid.Approved
GavestinelThe metabolism of Gavestinel can be decreased when combined with Sorafenib.Investigational
GefitinibThe serum concentration of Gefitinib can be increased when it is combined with Sorafenib.Approved, Investigational
GemcitabineThe serum concentration of Gemcitabine can be increased when it is combined with Sorafenib.Approved
GemfibrozilThe metabolism of Sorafenib can be decreased when combined with Gemfibrozil.Approved
GemifloxacinSorafenib may increase the QTc-prolonging activities of Gemifloxacin.Approved, Investigational
GenisteinThe serum concentration of Sorafenib can be increased when it is combined with Genistein.Investigational
GI-5005The risk or severity of adverse effects can be increased when Sorafenib is combined with GI-5005.Investigational
GliclazideThe metabolism of Gliclazide can be decreased when combined with Sorafenib.Approved
GlimepirideThe metabolism of Glimepiride can be decreased when combined with Sorafenib.Approved
GlipizideThe metabolism of Glipizide can be decreased when combined with Sorafenib.Approved
GlyburideThe serum concentration of Sorafenib can be increased when it is combined with Glyburide.Approved
GlycerolThe serum concentration of Sorafenib can be increased when it is combined with Glycerol.Experimental
GoserelinSorafenib may increase the QTc-prolonging activities of Goserelin.Approved
Gramicidin DThe serum concentration of Sorafenib can be increased when it is combined with Gramicidin D.Approved
GranisetronSorafenib may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
GrazoprevirThe serum concentration of Grazoprevir can be increased when it is combined with Sorafenib.Approved
GrepafloxacinThe serum concentration of Grepafloxacin can be increased when it is combined with Sorafenib.Withdrawn
GuanfacineThe metabolism of Guanfacine can be decreased when combined with Sorafenib.Approved, Investigational
HaloperidolSorafenib may increase the QTc-prolonging activities of Haloperidol.Approved
HalothaneThe metabolism of Halothane can be decreased when combined with Sorafenib.Approved, Vet Approved
HexobarbitalThe metabolism of Hexobarbital can be decreased when combined with Sorafenib.Approved
Histamine PhosphateThe metabolism of Histamine Phosphate can be decreased when combined with Sorafenib.Approved
HydrocortisoneThe serum concentration of Sorafenib can be increased when it is combined with Hydrocortisone.Approved, Vet Approved
HydromorphoneThe metabolism of Hydromorphone can be decreased when combined with Sorafenib.Approved, Illicit
IbuprofenThe serum concentration of Ibuprofen can be increased when it is combined with Sorafenib.Approved
IbutilideSorafenib may increase the QTc-prolonging activities of Ibutilide.Approved
IdarubicinThe metabolism of Idarubicin can be decreased when combined with Sorafenib.Approved
IdelalisibThe serum concentration of Sorafenib can be increased when it is combined with Idelalisib.Approved
IfosfamideThe metabolism of Ifosfamide can be decreased when combined with Sorafenib.Approved
IloperidoneSorafenib may increase the QTc-prolonging activities of Iloperidone.Approved
ImatinibThe metabolism of Sorafenib can be decreased when combined with Imatinib.Approved
ImipramineThe serum concentration of Sorafenib can be increased when it is combined with Imipramine.Approved
IndacaterolThe serum concentration of Indacaterol can be increased when it is combined with Sorafenib.Approved
IndinavirThe serum concentration of Sorafenib can be increased when it is combined with Indinavir.Approved
indisulamThe metabolism of indisulam can be decreased when combined with Sorafenib.Investigational
IndomethacinThe serum concentration of Sorafenib can be increased when it is combined with Indomethacin.Approved, Investigational
INGN 201The risk or severity of adverse effects can be increased when Sorafenib is combined with INGN 201.Investigational
INGN 225The risk or severity of adverse effects can be increased when Sorafenib is combined with INGN 225.Investigational
IrbesartanThe metabolism of Irbesartan can be decreased when combined with Sorafenib.Approved, Investigational
IrinotecanThe serum concentration of Irinotecan can be increased when it is combined with Sorafenib.Approved, Investigational
IsavuconazoniumThe metabolism of Sorafenib can be decreased when combined with Isavuconazonium.Approved, Investigational
IsofluraneThe metabolism of Isoflurane can be decreased when combined with Sorafenib.Approved, Vet Approved
IsradipineThe metabolism of Sorafenib can be decreased when combined with Isradipine.Approved
ItraconazoleThe serum concentration of Sorafenib can be increased when it is combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Sorafenib can be increased when it is combined with Ivacaftor.Approved
IvermectinThe serum concentration of Sorafenib can be increased when it is combined with Ivermectin.Approved, Vet Approved
IxazomibThe metabolism of Ixazomib can be decreased when combined with Sorafenib.Approved
KetamineThe serum concentration of Sorafenib can be increased when it is combined with Ketamine.Approved, Vet Approved
KetazolamThe serum concentration of Ketazolam can be increased when it is combined with Sorafenib.Approved
KetobemidoneThe metabolism of Ketobemidone can be decreased when combined with Sorafenib.Approved
KetoconazoleThe serum concentration of Sorafenib can be increased when it is combined with Ketoconazole.Approved, Investigational
KetoprofenThe metabolism of Ketoprofen can be decreased when combined with Sorafenib.Approved, Vet Approved
LamivudineThe serum concentration of Lamivudine can be increased when it is combined with Sorafenib.Approved, Investigational
LamotrigineThe serum concentration of Lamotrigine can be increased when it is combined with Sorafenib.Approved, Investigational
LansoprazoleThe serum concentration of Sorafenib can be increased when it is combined with Lansoprazole.Approved, Investigational
LapatinibThe serum concentration of Sorafenib can be increased when it is combined with Lapatinib.Approved, Investigational
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Sorafenib.Approved
LeflunomideThe risk or severity of adverse effects can be increased when Sorafenib is combined with Leflunomide.Approved, Investigational
LenalidomideThe serum concentration of Lenalidomide can be increased when it is combined with Sorafenib.Approved
LenvatinibSorafenib may increase the QTc-prolonging activities of Lenvatinib.Approved
LesinuradThe metabolism of Lesinurad can be decreased when combined with Sorafenib.Approved
LeuprolideSorafenib may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
LevetiracetamThe serum concentration of Levetiracetam can be increased when it is combined with Sorafenib.Approved, Investigational
LevofloxacinSorafenib may increase the QTc-prolonging activities of Levofloxacin.Approved, Investigational
LevomilnacipranThe serum concentration of Levomilnacipran can be increased when it is combined with Sorafenib.Approved
LevothyroxineThe serum concentration of Sorafenib can be decreased when it is combined with Levothyroxine.Approved
LicofeloneThe metabolism of Licofelone can be decreased when combined with Sorafenib.Investigational
LidocaineThe serum concentration of Sorafenib can be increased when it is combined with Lidocaine.Approved, Vet Approved
LinagliptinThe serum concentration of Linagliptin can be increased when it is combined with Sorafenib.Approved
LiothyronineThe serum concentration of Sorafenib can be decreased when it is combined with Liothyronine.Approved, Vet Approved
LiotrixThe serum concentration of Sorafenib can be decreased when it is combined with Liotrix.Approved
LisinoprilThe serum concentration of Sorafenib can be increased when it is combined with Lisinopril.Approved, Investigational
LomitapideThe serum concentration of Sorafenib can be increased when it is combined with Lomitapide.Approved
LoperamideThe serum concentration of Sorafenib can be increased when it is combined with Loperamide.Approved
LopinavirThe serum concentration of Sorafenib can be increased when it is combined with Lopinavir.Approved
LoratadineThe serum concentration of Sorafenib can be increased when it is combined with Loratadine.Approved
LorcaserinThe metabolism of Lorcaserin can be decreased when combined with Sorafenib.Approved
LornoxicamThe metabolism of Lornoxicam can be decreased when combined with Sorafenib.Approved
LosartanThe serum concentration of Sorafenib can be increased when it is combined with Losartan.Approved
LovastatinThe metabolism of Sorafenib can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Sorafenib can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Sorafenib can be decreased when it is combined with Lumacaftor.Approved
LumefantrineSorafenib may increase the QTc-prolonging activities of Lumefantrine.Approved
LumiracoxibThe metabolism of Lumiracoxib can be decreased when combined with Sorafenib.Approved, Investigational
MalathionThe metabolism of Malathion can be decreased when combined with Sorafenib.Approved, Investigational
MannitolThe serum concentration of Mannitol can be increased when it is combined with Sorafenib.Approved, Investigational
MaprotilineThe serum concentration of Sorafenib can be increased when it is combined with Maprotiline.Approved
MebendazoleThe serum concentration of Sorafenib can be increased when it is combined with Mebendazole.Approved, Vet Approved
Mefenamic acidThe metabolism of Mefenamic acid can be decreased when combined with Sorafenib.Approved
MefloquineThe serum concentration of Sorafenib can be increased when it is combined with Mefloquine.Approved
Megestrol acetateThe serum concentration of Sorafenib can be increased when it is combined with Megestrol acetate.Approved, Vet Approved
MelatoninThe metabolism of Melatonin can be decreased when combined with Sorafenib.Approved, Nutraceutical, Vet Approved
MeloxicamThe metabolism of Meloxicam can be decreased when combined with Sorafenib.Approved, Vet Approved
MephenytoinThe metabolism of Mephenytoin can be decreased when combined with Sorafenib.Investigational, Withdrawn
MeprobamateThe serum concentration of Sorafenib can be increased when it is combined with Meprobamate.Approved, Illicit
MestranolThe metabolism of Mestranol can be decreased when combined with Sorafenib.Approved
MetamizoleThe risk or severity of adverse effects can be increased when Metamizole is combined with Sorafenib.Withdrawn
MethadoneSorafenib may increase the QTc-prolonging activities of Methadone.Approved
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Sorafenib.Approved
MethoxyfluraneThe metabolism of Methoxyflurane can be decreased when combined with Sorafenib.Approved, Vet Approved
MethylphenobarbitalThe metabolism of Methylphenobarbital can be decreased when combined with Sorafenib.Approved
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Sorafenib.Approved, Vet Approved
MethyltestosteroneThe metabolism of Methyltestosterone can be decreased when combined with Sorafenib.Approved
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Sorafenib.Approved, Investigational
MetronidazoleThe metabolism of Metronidazole can be decreased when combined with Sorafenib.Approved
MexiletineThe metabolism of Mexiletine can be decreased when combined with Sorafenib.Approved
MianserinThe metabolism of Mianserin can be decreased when combined with Sorafenib.Approved
MibefradilThe serum concentration of Sorafenib can be increased when it is combined with Mibefradil.Withdrawn
MiconazoleThe serum concentration of Sorafenib can be increased when it is combined with Miconazole.Approved, Investigational, Vet Approved
MidazolamThe serum concentration of Sorafenib can be decreased when it is combined with Midazolam.Approved, Illicit
MifepristoneThe serum concentration of Sorafenib can be increased when it is combined with Mifepristone.Approved, Investigational
MirabegronThe serum concentration of Mirabegron can be increased when it is combined with Sorafenib.Approved
MirtazapineThe metabolism of Mirtazapine can be decreased when combined with Sorafenib.Approved
MitomycinThe serum concentration of Sorafenib can be increased when it is combined with Mitomycin.Approved
MitotaneThe serum concentration of Sorafenib can be decreased when it is combined with Mitotane.Approved
MitoxantroneThe serum concentration of Sorafenib can be decreased when it is combined with Mitoxantrone.Approved, Investigational
MoclobemideThe metabolism of Moclobemide can be decreased when combined with Sorafenib.Approved
ModafinilThe serum concentration of Sorafenib can be decreased when it is combined with Modafinil.Approved, Investigational
MontelukastThe metabolism of Montelukast can be decreased when combined with Sorafenib.Approved
MorphineThe serum concentration of Sorafenib can be increased when it is combined with Morphine.Approved, Investigational
MoxifloxacinSorafenib may increase the QTc-prolonging activities of Moxifloxacin.Approved, Investigational
Mycophenolate mofetilThe serum concentration of Mycophenolate mofetil can be increased when it is combined with Sorafenib.Approved, Investigational
NadololThe serum concentration of Nadolol can be increased when it is combined with Sorafenib.Approved
NafcillinThe serum concentration of Sorafenib can be decreased when it is combined with Nafcillin.Approved
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Sorafenib.Approved
NaloxoneThe serum concentration of Naloxone can be increased when it is combined with Sorafenib.Approved, Vet Approved
NaltrexoneThe serum concentration of Sorafenib can be increased when it is combined with Naltrexone.Approved, Investigational, Vet Approved
NaproxenThe metabolism of Naproxen can be decreased when combined with Sorafenib.Approved, Vet Approved
NaringeninThe serum concentration of Sorafenib can be increased when it is combined with Naringenin.Experimental
NatalizumabThe risk or severity of adverse effects can be increased when Sorafenib is combined with Natalizumab.Approved, Investigational
NateglinideThe metabolism of Nateglinide can be decreased when combined with Sorafenib.Approved, Investigational
NefazodoneThe serum concentration of Sorafenib can be increased when it is combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Sorafenib can be increased when it is combined with Nelfinavir.Approved
NeomycinThe serum concentration of Sorafenib can be decreased when it is combined with Neomycin.Approved, Vet Approved
NeostigmineThe serum concentration of Sorafenib can be increased when it is combined with Neostigmine.Approved, Vet Approved
NetupitantThe serum concentration of Sorafenib can be increased when it is combined with Netupitant.Approved
NevirapineThe serum concentration of Sorafenib can be decreased when it is combined with Nevirapine.Approved
NicardipineThe serum concentration of Sorafenib can be increased when it is combined with Nicardipine.Approved
NiclosamideThe metabolism of Niclosamide can be decreased when combined with Sorafenib.Approved, Vet Approved
NicotineThe metabolism of Nicotine can be decreased when combined with Sorafenib.Approved
NifedipineThe serum concentration of Sorafenib can be decreased when it is combined with Nifedipine.Approved
NilotinibSorafenib may increase the QTc-prolonging activities of Nilotinib.Approved, Investigational
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Sorafenib.Approved
NisoldipineThe serum concentration of Sorafenib can be increased when it is combined with Nisoldipine.Approved
NitrazepamThe serum concentration of Sorafenib can be increased when it is combined with Nitrazepam.Approved
NitrendipineThe serum concentration of Sorafenib can be increased when it is combined with Nitrendipine.Approved
NizatidineThe serum concentration of Nizatidine can be increased when it is combined with Sorafenib.Approved
NorethisteroneThe serum concentration of Sorafenib can be decreased when it is combined with Norethisterone.Approved
NortriptylineThe metabolism of Nortriptyline can be decreased when combined with Sorafenib.Approved
OfloxacinSorafenib may increase the QTc-prolonging activities of Ofloxacin.Approved
OlanzapineThe serum concentration of Olanzapine can be increased when it is combined with Sorafenib.Approved, Investigational
OlaparibThe metabolism of Sorafenib can be decreased when combined with Olaparib.Approved
OlodaterolThe metabolism of Olodaterol can be decreased when combined with Sorafenib.Approved
OmbitasvirThe serum concentration of Ombitasvir can be increased when it is combined with Sorafenib.Approved
OmeprazoleThe serum concentration of Sorafenib can be increased when it is combined with Omeprazole.Approved, Investigational, Vet Approved
OndansetronSorafenib may increase the QTc-prolonging activities of Ondansetron.Approved
OsimertinibThe serum concentration of Sorafenib can be increased when it is combined with Osimertinib.Approved
OspemifeneThe metabolism of Ospemifene can be decreased when combined with Sorafenib.Approved
OuabainOuabain may decrease the cardiotoxic activities of Sorafenib.Approved
OxaprozinThe metabolism of Oxaprozin can be decreased when combined with Sorafenib.Approved
P-NitrophenolThe serum concentration of Sorafenib can be increased when it is combined with P-Nitrophenol.Experimental
PaclitaxelThe risk or severity of adverse effects can be increased when Sorafenib is combined with Paclitaxel.Approved, Vet Approved
PalbociclibThe serum concentration of Sorafenib can be increased when it is combined with Palbociclib.Approved
PaliperidoneSorafenib may increase the QTc-prolonging activities of Paliperidone.Approved
Palmitic AcidThe serum concentration of Sorafenib can be increased when it is combined with Palmitic Acid.Experimental
PanobinostatSorafenib may increase the QTc-prolonging activities of Panobinostat.Approved, Investigational
PantoprazoleThe serum concentration of Sorafenib can be increased when it is combined with Pantoprazole.Approved
ParamethadioneThe metabolism of Paramethadione can be decreased when combined with Sorafenib.Approved
ParecoxibThe metabolism of Parecoxib can be decreased when combined with Sorafenib.Approved
ParoxetineThe serum concentration of Sorafenib can be increased when it is combined with Paroxetine.Approved, Investigational
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Sorafenib.Approved
PentamidineSorafenib may increase the QTc-prolonging activities of Pentamidine.Approved
PentobarbitalThe serum concentration of Sorafenib can be decreased when it is combined with Pentobarbital.Approved, Vet Approved
PerflutrenSorafenib may increase the QTc-prolonging activities of Perflutren.Approved
PerhexilineThe metabolism of Perhexiline can be decreased when combined with Sorafenib.Approved
PerindoprilThe serum concentration of Sorafenib can be increased when it is combined with Perindopril.Approved
PermethrinThe metabolism of Permethrin can be decreased when combined with Sorafenib.Approved, Investigational
PerphenazineThe metabolism of Perphenazine can be decreased when combined with Sorafenib.Approved
PethidineThe metabolism of Pethidine can be decreased when combined with Sorafenib.Approved
PhenacetinThe metabolism of Phenacetin can be decreased when combined with Sorafenib.Withdrawn
PhenobarbitalThe serum concentration of Sorafenib can be decreased when it is combined with Phenobarbital.Approved
PhenprocoumonThe metabolism of Phenprocoumon can be decreased when combined with Sorafenib.Approved
PhenylbutazoneThe metabolism of Phenylbutazone can be decreased when combined with Sorafenib.Approved, Vet Approved
PhenytoinThe serum concentration of Sorafenib can be decreased when it is combined with Phenytoin.Approved, Vet Approved
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Sorafenib.Approved, Investigational
PimozideSorafenib may increase the QTc-prolonging activities of Pimozide.Approved
PioglitazoneThe metabolism of Pioglitazone can be decreased when combined with Sorafenib.Approved, Investigational
PiroxicamThe metabolism of Piroxicam can be decreased when combined with Sorafenib.Approved, Investigational
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Sorafenib.Approved
Platelet Activating FactorThe serum concentration of Sorafenib can be decreased when it is combined with Platelet Activating Factor.Experimental
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Sorafenib.Approved
PonatinibThe serum concentration of Ponatinib can be increased when it is combined with Sorafenib.Approved
PosaconazoleThe serum concentration of Sorafenib can be increased when it is combined with Posaconazole.Approved, Investigational, Vet Approved
PrasugrelThe metabolism of Prasugrel can be decreased when combined with Sorafenib.Approved
PravastatinThe serum concentration of Sorafenib can be increased when it is combined with Pravastatin.Approved
PrazosinThe serum concentration of Sorafenib can be increased when it is combined with Prazosin.Approved
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Sorafenib.Approved, Vet Approved
PrednisoneThe serum concentration of Sorafenib can be increased when it is combined with Prednisone.Approved, Vet Approved
PrimaquineSorafenib may increase the QTc-prolonging activities of Primaquine.Approved
PrimidoneThe serum concentration of Sorafenib can be decreased when it is combined with Primidone.Approved, Vet Approved
ProbenecidThe serum concentration of Sorafenib can be increased when it is combined with Probenecid.Approved
ProcainamideSorafenib may increase the QTc-prolonging activities of Procainamide.Approved
ProgesteroneThe serum concentration of Sorafenib can be decreased when it is combined with Progesterone.Approved, Vet Approved
ProguanilThe metabolism of Proguanil can be decreased when combined with Sorafenib.Approved
PromazineSorafenib may increase the QTc-prolonging activities of Promazine.Approved, Vet Approved
PromethazineThe serum concentration of Sorafenib can be increased when it is combined with Promethazine.Approved
PropacetamolSorafenib may increase the hepatotoxic activities of Propacetamol.Approved
PropafenoneSorafenib may increase the QTc-prolonging activities of Propafenone.Approved
PropofolThe metabolism of Propofol can be decreased when combined with Sorafenib.Approved, Investigational, Vet Approved
PropranololThe serum concentration of Sorafenib can be increased when it is combined with Propranolol.Approved, Investigational
ProtriptylineThe serum concentration of Sorafenib can be increased when it is combined with Protriptyline.Approved
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Sorafenib.Approved
QuazepamThe serum concentration of Sorafenib can be increased when it is combined with Quazepam.Approved, Illicit
QuercetinThe serum concentration of Sorafenib can be increased when it is combined with Quercetin.Experimental
QuetiapineSorafenib may increase the QTc-prolonging activities of Quetiapine.Approved
QuinacrineThe serum concentration of Sorafenib can be increased when it is combined with Quinacrine.Approved
QuinidineSorafenib may increase the QTc-prolonging activities of Quinidine.Approved
QuinineSorafenib may increase the QTc-prolonging activities of Quinine.Approved
RabeprazoleThe metabolism of Sorafenib can be decreased when combined with Rabeprazole.Approved, Investigational
Rabies vaccineThe risk or severity of adverse effects can be increased when Sorafenib is combined with Rabies vaccine.Approved
Rabies vaccineThe therapeutic efficacy of Rabies vaccine can be decreased when used in combination with Sorafenib.Approved
RanitidineThe serum concentration of Sorafenib can be increased when it is combined with Ranitidine.Approved
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Sorafenib.Approved, Investigational
ReboxetineThe serum concentration of Sorafenib can be increased when it is combined with Reboxetine.Approved, Investigational
RegorafenibThe serum concentration of Sorafenib can be increased when it is combined with Regorafenib.Approved
ReserpineThe serum concentration of Sorafenib can be decreased when it is combined with Reserpine.Approved
RifabutinThe serum concentration of Sorafenib can be decreased when it is combined with Rifabutin.Approved
RifampicinThe serum concentration of Sorafenib can be decreased when it is combined with Rifampicin.Approved
RifapentineThe serum concentration of Sorafenib can be decreased when it is combined with Rifapentine.Approved
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Sorafenib.Approved, Investigational
RilpivirineThe serum concentration of Sorafenib can be increased when it is combined with Rilpivirine.Approved
RisperidoneThe serum concentration of Risperidone can be increased when it is combined with Sorafenib.Approved, Investigational
RitonavirThe serum concentration of Sorafenib can be increased when it is combined with Ritonavir.Approved, Investigational
RivaroxabanThe serum concentration of Rivaroxaban can be increased when it is combined with Sorafenib.Approved
RofecoxibThe metabolism of Rofecoxib can be decreased when combined with Sorafenib.Investigational, Withdrawn
RoflumilastRoflumilast may increase the immunosuppressive activities of Sorafenib.Approved
RolapitantThe serum concentration of Sorafenib can be increased when it is combined with Rolapitant.Approved
RomidepsinThe serum concentration of Romidepsin can be increased when it is combined with Sorafenib.Approved, Investigational
RopivacaineThe metabolism of Ropivacaine can be decreased when combined with Sorafenib.Approved
RosiglitazoneThe metabolism of Rosiglitazone can be decreased when combined with Sorafenib.Approved, Investigational
RosuvastatinThe metabolism of Rosuvastatin can be decreased when combined with Sorafenib.Approved
Salicylic acidThe serum concentration of Salicylic acid can be increased when it is combined with Sorafenib.Approved, Vet Approved
SaquinavirThe serum concentration of Sorafenib can be increased when it is combined with Saquinavir.Approved, Investigational
ScopolamineThe serum concentration of Sorafenib can be increased when it is combined with Scopolamine.Approved
SecobarbitalThe metabolism of Sorafenib can be increased when combined with Secobarbital.Approved, Vet Approved
SelegilineThe serum concentration of Sorafenib can be increased when it is combined with Selegiline.Approved, Investigational, Vet Approved
SelexipagThe serum concentration of Selexipag can be increased when it is combined with Sorafenib.Approved
SeratrodastThe metabolism of Seratrodast can be decreased when combined with Sorafenib.Approved, Investigational
SertralineThe serum concentration of Sorafenib can be increased when it is combined with Sertraline.Approved
SevofluraneThe metabolism of Sevoflurane can be decreased when combined with Sorafenib.Approved, Vet Approved
SildenafilThe metabolism of Sorafenib can be decreased when combined with Sildenafil.Approved, Investigational
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Sorafenib.Approved
SiltuximabThe serum concentration of Sorafenib can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Sorafenib can be increased when it is combined with Simeprevir.Approved
SimvastatinThe serum concentration of Sorafenib can be increased when it is combined with Simvastatin.Approved
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Sorafenib.Approved
SirolimusThe serum concentration of Sorafenib can be decreased when it is combined with Sirolimus.Approved, Investigational
SitagliptinThe serum concentration of Sitagliptin can be increased when it is combined with Sorafenib.Approved, Investigational
SitaxentanThe metabolism of Sitaxentan can be decreased when combined with Sorafenib.Approved, Investigational, Withdrawn
SofosbuvirThe serum concentration of Sofosbuvir can be increased when it is combined with Sorafenib.Approved
SotalolSorafenib may increase the QTc-prolonging activities of Sotalol.Approved
SparfloxacinThe serum concentration of Sparfloxacin can be increased when it is combined with Sorafenib.Approved
SphingosineThe serum concentration of Sphingosine can be increased when it is combined with Sorafenib.Experimental
SpironolactoneThe serum concentration of Sorafenib can be increased when it is combined with Spironolactone.Approved
SRP 299The risk or severity of adverse effects can be increased when Sorafenib is combined with SRP 299.Investigational
St. John's WortThe serum concentration of Sorafenib can be decreased when it is combined with St. John's Wort.Nutraceutical
StaurosporineThe serum concentration of Sorafenib can be increased when it is combined with Staurosporine.Experimental
StiripentolThe serum concentration of Sorafenib can be increased when it is combined with Stiripentol.Approved
StreptozocinThe serum concentration of Sorafenib can be decreased when it is combined with Streptozocin.Approved
SulfadiazineThe metabolism of Sulfadiazine can be decreased when combined with Sorafenib.Approved, Vet Approved
SulfamethoxazoleThe metabolism of Sulfamethoxazole can be decreased when combined with Sorafenib.Approved
SulfamoxoleThe metabolism of Sulfamoxole can be decreased when combined with Sorafenib.Approved
SulfinpyrazoneThe serum concentration of Sorafenib can be increased when it is combined with Sulfinpyrazone.Approved
SulfisoxazoleSorafenib may increase the QTc-prolonging activities of Sulfisoxazole.Approved, Vet Approved
SumatriptanThe serum concentration of Sorafenib can be increased when it is combined with Sumatriptan.Approved, Investigational
SunitinibThe serum concentration of Sorafenib can be increased when it is combined with Sunitinib.Approved, Investigational
SuprofenThe metabolism of Suprofen can be decreased when combined with Sorafenib.Approved, Withdrawn
TacrineThe serum concentration of Sorafenib can be increased when it is combined with Tacrine.Withdrawn
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Sorafenib.Approved, Investigational
TacrolimusThe serum concentration of Sorafenib can be decreased when it is combined with Tacrolimus.Approved, Investigational
TamoxifenThe serum concentration of Sorafenib can be decreased when it is combined with Tamoxifen.Approved
TapentadolThe metabolism of Tapentadol can be decreased when combined with Sorafenib.Approved
Taurocholic AcidThe serum concentration of Sorafenib can be increased when it is combined with Taurocholic Acid.Experimental
Technetium Tc-99m sestamibiThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Sorafenib.Approved
TelaprevirThe serum concentration of Sorafenib can be increased when it is combined with Telaprevir.Approved
TelavancinSorafenib may increase the QTc-prolonging activities of Telavancin.Approved
TelithromycinThe serum concentration of Sorafenib can be increased when it is combined with Telithromycin.Approved
TelmisartanThe serum concentration of Sorafenib can be increased when it is combined with Telmisartan.Approved, Investigational
TemazepamThe metabolism of Temazepam can be decreased when combined with Sorafenib.Approved
TemsirolimusThe serum concentration of Temsirolimus can be increased when it is combined with Sorafenib.Approved
TenoxicamThe metabolism of Tenoxicam can be decreased when combined with Sorafenib.Approved
TerazosinThe serum concentration of Sorafenib can be increased when it is combined with Terazosin.Approved
TerbinafineThe metabolism of Terbinafine can be decreased when combined with Sorafenib.Approved, Investigational, Vet Approved
TerfenadineThe serum concentration of Sorafenib can be increased when it is combined with Terfenadine.Withdrawn
TeriflunomideThe serum concentration of Sorafenib can be increased when it is combined with Teriflunomide.Approved
TesmilifeneThe serum concentration of Sorafenib can be decreased when it is combined with Tesmilifene.Investigational
TestosteroneThe serum concentration of Sorafenib can be increased when it is combined with Testosterone.Approved, Investigational
TetrabenazineSorafenib may increase the QTc-prolonging activities of Tetrabenazine.Approved
TG4010The risk or severity of adverse effects can be increased when Sorafenib is combined with TG4010.Investigational
ThalidomideThe metabolism of Thalidomide can be decreased when combined with Sorafenib.Approved, Investigational, Withdrawn
TheophyllineThe metabolism of Theophylline can be decreased when combined with Sorafenib.Approved
ThiamylalThe metabolism of Thiamylal can be decreased when combined with Sorafenib.Approved, Vet Approved
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Sorafenib.Approved
ThiotepaThe metabolism of Sorafenib can be decreased when combined with Thiotepa.Approved
TicagrelorThe serum concentration of Ticagrelor can be increased when it is combined with Sorafenib.Approved
TiclopidineThe metabolism of Sorafenib can be decreased when combined with Ticlopidine.Approved
TimololThe serum concentration of Timolol can be increased when it is combined with Sorafenib.Approved
TocilizumabThe serum concentration of Sorafenib can be decreased when it is combined with Tocilizumab.Approved
TofacitinibSorafenib may increase the immunosuppressive activities of Tofacitinib.Approved, Investigational
TolbutamideThe metabolism of Tolbutamide can be decreased when combined with Sorafenib.Approved
TolterodineThe metabolism of Tolterodine can be decreased when combined with Sorafenib.Approved, Investigational
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Sorafenib.Approved
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Sorafenib.Approved, Investigational
TorasemideThe metabolism of Torasemide can be decreased when combined with Sorafenib.Approved
ToremifeneSorafenib may increase the QTc-prolonging activities of Toremifene.Approved, Investigational
TrabectedinThe metabolism of Trabectedin can be decreased when combined with Sorafenib.Approved, Investigational
TramadolThe metabolism of Tramadol can be decreased when combined with Sorafenib.Approved, Investigational
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Sorafenib.Approved, Investigational
Trastuzumab emtansineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Sorafenib.Approved
TrazodoneThe serum concentration of Sorafenib can be decreased when it is combined with Trazodone.Approved, Investigational
TreprostinilThe metabolism of Treprostinil can be decreased when combined with Sorafenib.Approved, Investigational
TretinoinThe metabolism of Tretinoin can be decreased when combined with Sorafenib.Approved, Investigational, Nutraceutical
TrifluoperazineThe serum concentration of Sorafenib can be increased when it is combined with Trifluoperazine.Approved
TriflupromazineThe serum concentration of Sorafenib can be increased when it is combined with Triflupromazine.Approved, Vet Approved
TrimethadioneThe metabolism of Trimethadione can be decreased when combined with Sorafenib.Approved
TrimethoprimThe serum concentration of Sorafenib can be decreased when it is combined with Trimethoprim.Approved, Vet Approved
TrimipramineThe serum concentration of Sorafenib can be increased when it is combined with Trimipramine.Approved
TroglitazoneThe metabolism of Troglitazone can be decreased when combined with Sorafenib.Withdrawn
TroleandomycinThe serum concentration of Sorafenib can be increased when it is combined with Troleandomycin.Approved
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Sorafenib.Approved
UmeclidiniumThe serum concentration of Umeclidinium can be increased when it is combined with Sorafenib.Approved
ValdecoxibThe metabolism of Valdecoxib can be decreased when combined with Sorafenib.Investigational, Withdrawn
Valproic AcidThe metabolism of Valproic Acid can be decreased when combined with Sorafenib.Approved, Investigational
ValsartanThe metabolism of Valsartan can be decreased when combined with Sorafenib.Approved, Investigational
VandetanibSorafenib may increase the QTc-prolonging activities of Vandetanib.Approved
VecuroniumThe serum concentration of Vecuronium can be increased when it is combined with Sorafenib.Approved
VemurafenibSorafenib may increase the QTc-prolonging activities of Vemurafenib.Approved
VenetoclaxThe serum concentration of Venetoclax can be increased when it is combined with Sorafenib.Approved
VenlafaxineThe metabolism of Sorafenib can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Sorafenib can be decreased when combined with Verapamil.Approved
VicrivirocThe metabolism of Vicriviroc can be decreased when combined with Sorafenib.Investigational
VinblastineThe serum concentration of Sorafenib can be decreased when it is combined with Vinblastine.Approved
VincristineThe serum concentration of Vincristine can be increased when it is combined with Sorafenib.Approved, Investigational
VincristineThe serum concentration of Sorafenib can be decreased when it is combined with Vincristine.Approved, Investigational
VinorelbineThe serum concentration of Sorafenib can be increased when it is combined with Vinorelbine.Approved, Investigational
VismodegibThe serum concentration of Vismodegib can be increased when it is combined with Sorafenib.Approved
VoriconazoleThe serum concentration of Sorafenib can be increased when it is combined with Voriconazole.Approved, Investigational
VortioxetineThe metabolism of Vortioxetine can be decreased when combined with Sorafenib.Approved
WarfarinSorafenib may increase the anticoagulant activities of Warfarin.Approved
XimelagatranThe metabolism of Ximelagatran can be decreased when combined with Sorafenib.Approved, Investigational, Withdrawn
ZafirlukastThe metabolism of Zafirlukast can be decreased when combined with Sorafenib.Approved, Investigational
ZalcitabineThe metabolism of Zalcitabine can be decreased when combined with Sorafenib.Approved
ZaltoprofenThe metabolism of Zaltoprofen can be decreased when combined with Sorafenib.Approved
ZidovudineThe serum concentration of Zidovudine can be increased when it is combined with Sorafenib.Approved
ZileutonThe metabolism of Zileuton can be decreased when combined with Sorafenib.Approved, Investigational, Withdrawn
ZimelidineThe serum concentration of Sorafenib can be increased when it is combined with Zimelidine.Withdrawn
ZiprasidoneSorafenib may increase the QTc-prolonging activities of Ziprasidone.Approved
ZolpidemThe metabolism of Zolpidem can be decreased when combined with Sorafenib.Approved
ZopicloneThe metabolism of Zopiclone can be decreased when combined with Sorafenib.Approved
ZuclopenthixolSorafenib may increase the QTc-prolonging activities of Zuclopenthixol.Approved, Investigational
Food InteractionsNot Available
References
Synthesis Reference

Ales Gavenda, Alexandr Jegorov, Pierluigi Rossetto, Peter Lindsay MacDonald, Augusto Canavesi, “POLYMORPHS OF SORAFENIB TOSYLATE AND SORAFENIB HEMI-TOSYLATE, AND PROCESSES FOR PREPARATION THEREOF.” U.S. Patent US20090192200, issued July 30, 2009.

US20090192200
General ReferencesNot Available
External Links
ATC CodesL01XE05
AHFS Codes
  • 92:00.00
PDB EntriesNot Available
FDA labelDownload (310 KB)
MSDSNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9649
Blood Brain Barrier+0.851
Caco-2 permeable-0.5138
P-glycoprotein substrateNon-substrate0.5086
P-glycoprotein inhibitor INon-inhibitor0.7141
P-glycoprotein inhibitor IINon-inhibitor0.9359
Renal organic cation transporterNon-inhibitor0.8938
CYP450 2C9 substrateNon-substrate0.6569
CYP450 2D6 substrateNon-substrate0.8212
CYP450 3A4 substrateNon-substrate0.5341
CYP450 1A2 substrateInhibitor0.6168
CYP450 2C9 inhibitorNon-inhibitor0.6171
CYP450 2D6 inhibitorNon-inhibitor0.9145
CYP450 2C19 inhibitorInhibitor0.637
CYP450 3A4 inhibitorNon-inhibitor0.7339
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.6629
Ames testNon AMES toxic0.8143
CarcinogenicityNon-carcinogens0.8684
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.7885 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9488
hERG inhibition (predictor II)Non-inhibitor0.6415
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Bayer healthcare pharmaceuticals inc
Packagers
Dosage forms
FormRouteStrength
TabletOral200 mg
Tablet, film coatedOral200 mg/1
Tablet, film coatedOral200 mg
Prices
Unit descriptionCostUnit
Nexavar 200 mg tablet66.61USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2315715 No2010-06-222018-12-22Canada
CA2359510 No2007-02-132020-01-12Canada
US7235576 No2000-01-122020-01-12Us
US7351834 No2000-01-122020-01-12Us
US7897623 No2000-01-122020-01-12Us
US8124630 No2000-01-122020-01-12Us
US8618141 No2003-02-112023-02-11Us
US8841330 No2000-01-122020-01-12Us
US8877933 No2007-12-242027-12-24Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubilityInsolubleFDA label
logP3.8Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00171 mg/mLALOGPS
logP4.12ALOGPS
logP4.34ChemAxon
logS-5.4ALOGPS
pKa (Strongest Acidic)11.55ChemAxon
pKa (Strongest Basic)2.03ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area92.35 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity114.52 m3·mol-1ChemAxon
Polarizability41.11 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as diarylethers. These are organic compounds containing the dialkyl ether functional group, with the formula ROR', where R and R' are aryl groups.
KingdomOrganic compounds
Super ClassOrganooxygen compounds
ClassEthers
Sub ClassDiarylethers
Direct ParentDiarylethers
Alternative Parents
Substituents
  • Diaryl ether
  • N-phenylurea
  • Pyridine carboxylic acid or derivatives
  • Pyridinecarboxamide
  • Halobenzene
  • Chlorobenzene
  • Benzenoid
  • Pyridine
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl chloride
  • Heteroaromatic compound
  • Urea
  • Secondary carboxylic acid amide
  • Carboxamide group
  • Azacycle
  • Organoheterocyclic compound
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Organofluoride
  • Organochloride
  • Organohalogen compound
  • Carbonyl group
  • Alkyl halide
  • Alkyl fluoride
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic 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. Flaherty KT: Chemotherapy and targeted therapy combinations in advanced melanoma. Clin Cancer Res. 2006 Apr 1;12(7 Pt 2):2366s-2370s. [PubMed:16609060 ]
  2. Haluska FG, Ibrahim N: Therapeutic targets in melanoma: map kinase pathway. Curr Oncol Rep. 2006 Sep;8(5):400-5. [PubMed:16901402 ]
  3. Kim S, Yazici YD, Calzada G, Wang ZY, Younes MN, Jasser SA, El-Naggar AK, Myers JN: Sorafenib inhibits the angiogenesis and growth of orthotopic anaplastic thyroid carcinoma xenografts in nude mice. Mol Cancer Ther. 2007 Jun;6(6):1785-92. [PubMed:17575107 ]
  4. Eisen T, Ahmad T, Flaherty KT, Gore M, Kaye S, Marais R, Gibbens I, Hackett S, James M, Schuchter LM, Nathanson KL, Xia C, Simantov R, Schwartz B, Poulin-Costello M, O'Dwyer PJ, Ratain MJ: Sorafenib in advanced melanoma: a Phase II randomised discontinuation trial analysis. Br J Cancer. 2006 Sep 4;95(5):581-6. Epub 2006 Aug 1. [PubMed:16880785 ]
  5. Lu X, Tang X, Guo W, Ren T, Zhao H: Sorafenib induces growth inhibition and apoptosis of human chondrosarcoma cells by blocking the RAF/ERK/MEK pathway. J Surg Oncol. 2010 Dec 1;102(7):821-6. doi: 10.1002/jso.21661. [PubMed:20812347 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Protein serine/threonine kinase activity
Specific Function:
Serine/threonine-protein kinase that acts as a regulatory link between the membrane-associated Ras GTPases and the MAPK/ERK cascade, and this critical regulatory link functions as a switch determining cell fate decisions including proliferation, differentiation, apoptosis, survival and oncogenic transformation. RAF1 activation initiates a mitogen-activated protein kinase (MAPK) cascade that com...
Gene Name:
RAF1
Uniprot ID:
P04049
Molecular Weight:
73051.025 Da
References
  1. Adnane L, Trail PA, Taylor I, Wilhelm SM: Sorafenib (BAY 43-9006, Nexavar), a dual-action inhibitor that targets RAF/MEK/ERK pathway in tumor cells and tyrosine kinases VEGFR/PDGFR in tumor vasculature. Methods Enzymol. 2006;407:597-612. [PubMed:16757355 ]
  2. Gollob JA, Wilhelm S, Carter C, Kelley SL: Role of Raf kinase in cancer: therapeutic potential of targeting the Raf/MEK/ERK signal transduction pathway. Semin Oncol. 2006 Aug;33(4):392-406. [PubMed:16890795 ]
  3. Huether A, Hopfner M, Baradari V, Schuppan D, Scherubl H: Sorafenib alone or as combination therapy for growth control of cholangiocarcinoma. Biochem Pharmacol. 2007 May 1;73(9):1308-17. Epub 2007 Jan 5. [PubMed:17266941 ]
  4. Cascone T, Gridelli C, Ciardiello F: Combined targeted therapies in non-small cell lung cancer: a winner strategy? Curr Opin Oncol. 2007 Mar;19(2):98-102. [PubMed:17272980 ]
  5. Gridelli C, Maione P, Del Gaizo F, Colantuoni G, Guerriero C, Ferrara C, Nicolella D, Comunale D, De Vita A, Rossi A: Sorafenib and sunitinib in the treatment of advanced non-small cell lung cancer. Oncologist. 2007 Feb;12(2):191-200. [PubMed:17296815 ]
  6. Lu X, Tang X, Guo W, Ren T, Zhao H: Sorafenib induces growth inhibition and apoptosis of human chondrosarcoma cells by blocking the RAF/ERK/MEK pathway. J Surg Oncol. 2010 Dec 1;102(7):821-6. doi: 10.1002/jso.21661. [PubMed:20812347 ]
  7. Smalley KS, Xiao M, Villanueva J, Nguyen TK, Flaherty KT, Letrero R, Van Belle P, Elder DE, Wang Y, Nathanson KL, Herlyn M: CRAF inhibition induces apoptosis in melanoma cells with non-V600E BRAF mutations. Oncogene. 2009 Jan 8;28(1):85-94. doi: 10.1038/onc.2008.362. Epub 2008 Sep 15. [PubMed:18794803 ]
  8. Wilhelm SM, Adnane L, Newell P, Villanueva A, Llovet JM, Lynch M: Preclinical overview of sorafenib, a multikinase inhibitor that targets both Raf and VEGF and PDGF receptor tyrosine kinase signaling. Mol Cancer Ther. 2008 Oct;7(10):3129-40. doi: 10.1158/1535-7163.MCT-08-0013. [PubMed:18852116 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Vascular endothelial growth factor-activated receptor activity
Specific Function:
Tyrosine-protein kinase that acts as a cell-surface receptor for VEGFC and VEGFD, and plays an essential role in adult lymphangiogenesis and in the development of the vascular network and the cardiovascular system during embryonic development. Promotes proliferation, survival and migration of endothelial cells, and regulates angiogenic sprouting. Signaling by activated FLT4 leads to enhanced pr...
Gene Name:
FLT4
Uniprot ID:
P35916
Molecular Weight:
152755.94 Da
References
  1. Lathia C, Lettieri J, Cihon F, Gallentine M, Radtke M, Sundaresan P: Lack of effect of ketoconazole-mediated CYP3A inhibition on sorafenib clinical pharmacokinetics. Cancer Chemother Pharmacol. 2006 May;57(5):685-92. Epub 2005 Aug 25. [PubMed:16133532 ]
  2. Adnane L, Trail PA, Taylor I, Wilhelm SM: Sorafenib (BAY 43-9006, Nexavar), a dual-action inhibitor that targets RAF/MEK/ERK pathway in tumor cells and tyrosine kinases VEGFR/PDGFR in tumor vasculature. Methods Enzymol. 2006;407:597-612. [PubMed:16757355 ]
  3. Gridelli C, Maione P, Del Gaizo F, Colantuoni G, Guerriero C, Ferrara C, Nicolella D, Comunale D, De Vita A, Rossi A: Sorafenib and sunitinib in the treatment of advanced non-small cell lung cancer. Oncologist. 2007 Feb;12(2):191-200. [PubMed:17296815 ]
  4. Strumberg D: Preclinical and clinical development of the oral multikinase inhibitor sorafenib in cancer treatment. Drugs Today (Barc). 2005 Dec;41(12):773-84. [PubMed:16474853 ]
  5. Reddy GK, Bukowski RM: Sorafenib: recent update on activity as a single agent and in combination with interferon-alpha2 in patients with advanced-stage renal cell carcinoma. Clin Genitourin Cancer. 2006 Mar;4(4):246-8. [PubMed:16729906 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Vascular endothelial growth factor-activated receptor activity
Specific Function:
Tyrosine-protein kinase that acts as a cell-surface receptor for VEGFA, VEGFC and VEGFD. Plays an essential role in the regulation of angiogenesis, vascular development, vascular permeability, and embryonic hematopoiesis. Promotes proliferation, survival, migration and differentiation of endothelial cells. Promotes reorganization of the actin cytoskeleton. Isoforms lacking a transmembrane domai...
Gene Name:
KDR
Uniprot ID:
P35968
Molecular Weight:
151525.555 Da
References
  1. Schoffski P, Dumez H, Clement P, Hoeben A, Prenen H, Wolter P, Joniau S, Roskams T, Van Poppel H: Emerging role of tyrosine kinase inhibitors in the treatment of advanced renal cell cancer: a review. Ann Oncol. 2006 Aug;17(8):1185-96. Epub 2006 Jan 17. [PubMed:16418310 ]
  2. Veronese ML, Mosenkis A, Flaherty KT, Gallagher M, Stevenson JP, Townsend RR, O'Dwyer PJ: Mechanisms of hypertension associated with BAY 43-9006. J Clin Oncol. 2006 Mar 20;24(9):1363-9. Epub 2006 Jan 30. [PubMed:16446323 ]
  3. Rini BI: Sorafenib. Expert Opin Pharmacother. 2006 Mar;7(4):453-61. [PubMed:16503817 ]
  4. Adnane L, Trail PA, Taylor I, Wilhelm SM: Sorafenib (BAY 43-9006, Nexavar), a dual-action inhibitor that targets RAF/MEK/ERK pathway in tumor cells and tyrosine kinases VEGFR/PDGFR in tumor vasculature. Methods Enzymol. 2006;407:597-612. [PubMed:16757355 ]
  5. Lacouture ME, Desai A, Soltani K, Petronic-Rosic V, Laumann AE, Ratain MJ, Stadler WM: Inflammation of actinic keratoses subsequent to therapy with sorafenib, a multitargeted tyrosine-kinase inhibitor. Clin Exp Dermatol. 2006 Nov;31(6):783-5. Epub 2006 Jul 4. [PubMed:16824050 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Vascular endothelial growth factor-activated receptor activity
Specific Function:
Tyrosine-protein kinase that acts as cell-surface receptor for the cytokine FLT3LG and regulates differentiation, proliferation and survival of hematopoietic progenitor cells and of dendritic cells. Promotes phosphorylation of SHC1 and AKT1, and activation of the downstream effector MTOR. Promotes activation of RAS signaling and phosphorylation of downstream kinases, including MAPK1/ERK2 and/or...
Gene Name:
FLT3
Uniprot ID:
P36888
Molecular Weight:
112902.51 Da
References
  1. Auclair D, Miller D, Yatsula V, Pickett W, Carter C, Chang Y, Zhang X, Wilkie D, Burd A, Shi H, Rocks S, Gedrich R, Abriola L, Vasavada H, Lynch M, Dumas J, Trail PA, Wilhelm SM: Antitumor activity of sorafenib in FLT3-driven leukemic cells. Leukemia. 2007 Mar;21(3):439-45. Epub 2007 Jan 4. [PubMed:17205056 ]
  2. Lierman E, Lahortiga I, Van Miegroet H, Mentens N, Marynen P, Cools J: The ability of sorafenib to inhibit oncogenic PDGFRbeta and FLT3 mutants and overcome resistance to other small molecule inhibitors. Haematologica. 2007 Jan;92(1):27-34. [PubMed:17229632 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Vascular endothelial growth factor binding
Specific Function:
Tyrosine-protein kinase that acts as cell-surface receptor for homodimeric PDGFB and PDGFD and for heterodimers formed by PDGFA and PDGFB, and plays an essential role in the regulation of embryonic development, cell proliferation, survival, differentiation, chemotaxis and migration. Plays an essential role in blood vessel development by promoting proliferation, migration and recruitment of peri...
Gene Name:
PDGFRB
Uniprot ID:
P09619
Molecular Weight:
123966.895 Da
References
  1. Gollob JA: Sorafenib: scientific rationales for single-agent and combination therapy in clear-cell renal cell carcinoma. Clin Genitourin Cancer. 2005 Dec;4(3):167-74. [PubMed:16425993 ]
  2. Guida T, Anaganti S, Provitera L, Gedrich R, Sullivan E, Wilhelm SM, Santoro M, Carlomagno F: Sorafenib inhibits imatinib-resistant KIT and platelet-derived growth factor receptor beta gatekeeper mutants. Clin Cancer Res. 2007 Jun 1;13(11):3363-9. [PubMed:17545544 ]
  3. Unnithan J, Rini BI: The role of targeted therapy in metastatic renal cell carcinoma. ScientificWorldJournal. 2007 Mar 2;7:800-7. [PubMed:17619763 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Transmembrane receptor protein tyrosine kinase activity
Specific Function:
Tyrosine-protein kinase that acts as cell-surface receptor for the cytokine KITLG/SCF and plays an essential role in the regulation of cell survival and proliferation, hematopoiesis, stem cell maintenance, gametogenesis, mast cell development, migration and function, and in melanogenesis. In response to KITLG/SCF binding, KIT can activate several signaling pathways. Phosphorylates PIK3R1, PLCG1...
Gene Name:
KIT
Uniprot ID:
P10721
Molecular Weight:
109863.655 Da
References
  1. Guida T, Anaganti S, Provitera L, Gedrich R, Sullivan E, Wilhelm SM, Santoro M, Carlomagno F: Sorafenib inhibits imatinib-resistant KIT and platelet-derived growth factor receptor beta gatekeeper mutants. Clin Cancer Res. 2007 Jun 1;13(11):3363-9. [PubMed:17545544 ]
  2. Koch CA, Gimm O, Vortmeyer AO, Al-Ali HK, Lamesch P, Ott R, Kluge R, Bierbach U, Tannapfel A: Does the expression of c-kit (CD117) in neuroendocrine tumors represent a target for therapy? Ann N Y Acad Sci. 2006 Aug;1073:517-26. [PubMed:17102120 ]
  3. Lierman E, Lahortiga I, Van Miegroet H, Mentens N, Marynen P, Cools J: The ability of sorafenib to inhibit oncogenic PDGFRbeta and FLT3 mutants and overcome resistance to other small molecule inhibitors. Haematologica. 2007 Jan;92(1):27-34. [PubMed:17229632 ]
  4. Cascone T, Gridelli C, Ciardiello F: Combined targeted therapies in non-small cell lung cancer: a winner strategy? Curr Opin Oncol. 2007 Mar;19(2):98-102. [PubMed:17272980 ]
  5. Liu L, Cao Y, Chen C, Zhang X, McNabola A, Wilkie D, Wilhelm S, Lynch M, Carter C: Sorafenib blocks the RAF/MEK/ERK pathway, inhibits tumor angiogenesis, and induces tumor cell apoptosis in hepatocellular carcinoma model PLC/PRF/5. Cancer Res. 2006 Dec 15;66(24):11851-8. [PubMed:17178882 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Protein tyrosine kinase activity
Specific Function:
Tyrosine-protein kinase that acts as cell-surface receptor for fibroblast growth factors and plays an essential role in the regulation of embryonic development, cell proliferation, differentiation and migration. Required for normal mesoderm patterning and correct axial organization during embryonic development, normal skeletogenesis and normal development of the gonadotropin-releasing hormone (...
Gene Name:
FGFR1
Uniprot ID:
P11362
Molecular Weight:
91866.935 Da
References
  1. Wilhelm SM, Carter C, Tang L, Wilkie D, McNabola A, Rong H, Chen C, Zhang X, Vincent P, McHugh M, Cao Y, Shujath J, Gawlak S, Eveleigh D, Rowley B, Liu L, Adnane L, Lynch M, Auclair D, Taylor I, Gedrich R, Voznesensky A, Riedl B, Post LE, Bollag G, Trail PA: BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis. Cancer Res. 2004 Oct 1;64(19):7099-109. [PubMed:15466206 ]
  2. Carlomagno F, Anaganti S, Guida T, Salvatore G, Troncone G, Wilhelm SM, Santoro M: BAY 43-9006 inhibition of oncogenic RET mutants. J Natl Cancer Inst. 2006 Mar 1;98(5):326-34. [PubMed:16507829 ]
  3. Wilhelm S, Carter C, Lynch M, Lowinger T, Dumas J, Smith RA, Schwartz B, Simantov R, Kelley S: Discovery and development of sorafenib: a multikinase inhibitor for treating cancer. Nat Rev Drug Discov. 2006 Oct;5(10):835-44. [PubMed:17016424 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Transmembrane receptor protein tyrosine kinase activity
Specific Function:
Receptor tyrosine-protein kinase involved in numerous cellular mechanisms including cell proliferation, neuronal navigation, cell migration, and cell differentiation upon binding with glial cell derived neurotrophic factor family ligands. Phosphorylates PTK2/FAK1. Regulates both cell death/survival balance and positional information. Required for the molecular mechanisms orchestration during in...
Gene Name:
RET
Uniprot ID:
P07949
Molecular Weight:
124317.465 Da
References
  1. Wilhelm SM, Carter C, Tang L, Wilkie D, McNabola A, Rong H, Chen C, Zhang X, Vincent P, McHugh M, Cao Y, Shujath J, Gawlak S, Eveleigh D, Rowley B, Liu L, Adnane L, Lynch M, Auclair D, Taylor I, Gedrich R, Voznesensky A, Riedl B, Post LE, Bollag G, Trail PA: BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis. Cancer Res. 2004 Oct 1;64(19):7099-109. [PubMed:15466206 ]
  2. Carlomagno F, Anaganti S, Guida T, Salvatore G, Troncone G, Wilhelm SM, Santoro M: BAY 43-9006 inhibition of oncogenic RET mutants. J Natl Cancer Inst. 2006 Mar 1;98(5):326-34. [PubMed:16507829 ]
  3. Wilhelm S, Carter C, Lynch M, Lowinger T, Dumas J, Smith RA, Schwartz B, Simantov R, Kelley S: Discovery and development of sorafenib: a multikinase inhibitor for treating cancer. Nat Rev Drug Discov. 2006 Oct;5(10):835-44. [PubMed:17016424 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Vegf-b-activated receptor activity
Specific Function:
Tyrosine-protein kinase that acts as a cell-surface receptor for VEGFA, VEGFB and PGF, and plays an essential role in the development of embryonic vasculature, the regulation of angiogenesis, cell survival, cell migration, macrophage function, chemotaxis, and cancer cell invasion. May play an essential role as a negative regulator of embryonic angiogenesis by inhibiting excessive proliferation ...
Gene Name:
FLT1
Uniprot ID:
P17948
Molecular Weight:
150767.185 Da
References
  1. Wilhelm SM, Carter C, Tang L, Wilkie D, McNabola A, Rong H, Chen C, Zhang X, Vincent P, McHugh M, Cao Y, Shujath J, Gawlak S, Eveleigh D, Rowley B, Liu L, Adnane L, Lynch M, Auclair D, Taylor I, Gedrich R, Voznesensky A, Riedl B, Post LE, Bollag G, Trail PA: BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis. Cancer Res. 2004 Oct 1;64(19):7099-109. [PubMed:15466206 ]
  2. Carlomagno F, Anaganti S, Guida T, Salvatore G, Troncone G, Wilhelm SM, Santoro M: BAY 43-9006 inhibition of oncogenic RET mutants. J Natl Cancer Inst. 2006 Mar 1;98(5):326-34. [PubMed:16507829 ]
  3. Wilhelm S, Carter C, Lynch M, Lowinger T, Dumas J, Smith RA, Schwartz B, Simantov R, Kelley S: Discovery and development of sorafenib: a multikinase inhibitor for treating cancer. Nat Rev Drug Discov. 2006 Oct;5(10):835-44. [PubMed:17016424 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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. Gomo C, Coriat R, Faivre L, Mir O, Ropert S, Billemont B, Dauphin A, Tod M, Goldwasser F, Blanchet B: Pharmacokinetic interaction involving sorafenib and the calcium-channel blocker felodipine in a patient with hepatocellular carcinoma. Invest New Drugs. 2011 Dec;29(6):1511-4. doi: 10.1007/s10637-010-9514-3. Epub 2010 Aug 13. [PubMed:20706860 ]
  2. van Erp NP, Gelderblom H, Guchelaar HJ: Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev. 2009 Dec;35(8):692-706. doi: 10.1016/j.ctrv.2009.08.004. Epub 2009 Sep 5. [PubMed:19733976 ]
  3. Flaherty KT, Lathia C, Frye RF, Schuchter L, Redlinger M, Rosen M, O'Dwyer PJ: Interaction of sorafenib and cytochrome P450 isoenzymes in patients with advanced melanoma: a phase I/II pharmacokinetic interaction study. Cancer Chemother Pharmacol. 2011 Nov;68(5):1111-8. doi: 10.1007/s00280-011-1585-0. Epub 2011 Feb 25. [PubMed:21350850 ]
  4. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A7
Uniprot ID:
P24462
Molecular Weight:
57525.03 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Flaherty KT, Lathia C, Frye RF, Schuchter L, Redlinger M, Rosen M, O'Dwyer PJ: Interaction of sorafenib and cytochrome P450 isoenzymes in patients with advanced melanoma: a phase I/II pharmacokinetic interaction study. Cancer Chemother Pharmacol. 2011 Nov;68(5):1111-8. doi: 10.1007/s00280-011-1585-0. Epub 2011 Feb 25. [PubMed:21350850 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Acts as a 1,4-cineole 2-exo-monooxygenase.
Gene Name:
CYP2B6
Uniprot ID:
P20813
Molecular Weight:
56277.81 Da
References
  1. Flaherty KT, Lathia C, Frye RF, Schuchter L, Redlinger M, Rosen M, O'Dwyer PJ: Interaction of sorafenib and cytochrome P450 isoenzymes in patients with advanced melanoma: a phase I/II pharmacokinetic interaction study. Cancer Chemother Pharmacol. 2011 Nov;68(5):1111-8. doi: 10.1007/s00280-011-1585-0. Epub 2011 Feb 25. [PubMed:21350850 ]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Molecular Weight:
55824.275 Da
References
  1. Flaherty KT, Lathia C, Frye RF, Schuchter L, Redlinger M, Rosen M, O'Dwyer PJ: Interaction of sorafenib and cytochrome P450 isoenzymes in patients with advanced melanoma: a phase I/II pharmacokinetic interaction study. Cancer Chemother Pharmacol. 2011 Nov;68(5):1111-8. doi: 10.1007/s00280-011-1585-0. Epub 2011 Feb 25. [PubMed:21350850 ]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
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. Flaherty KT, Lathia C, Frye RF, Schuchter L, Redlinger M, Rosen M, O'Dwyer PJ: Interaction of sorafenib and cytochrome P450 isoenzymes in patients with advanced melanoma: a phase I/II pharmacokinetic interaction study. Cancer Chemother Pharmacol. 2011 Nov;68(5):1111-8. doi: 10.1007/s00280-011-1585-0. Epub 2011 Feb 25. [PubMed:21350850 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Flaherty KT, Lathia C, Frye RF, Schuchter L, Redlinger M, Rosen M, O'Dwyer PJ: Interaction of sorafenib and cytochrome P450 isoenzymes in patients with advanced melanoma: a phase I/II pharmacokinetic interaction study. Cancer Chemother Pharmacol. 2011 Nov;68(5):1111-8. doi: 10.1007/s00280-011-1585-0. Epub 2011 Feb 25. [PubMed:21350850 ]
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. Flaherty KT, Lathia C, Frye RF, Schuchter L, Redlinger M, Rosen M, O'Dwyer PJ: Interaction of sorafenib and cytochrome P450 isoenzymes in patients with advanced melanoma: a phase I/II pharmacokinetic interaction study. Cancer Chemother Pharmacol. 2011 Nov;68(5):1111-8. doi: 10.1007/s00280-011-1585-0. Epub 2011 Feb 25. [PubMed:21350850 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Retinoic acid binding
Specific Function:
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform has specificity for phenols. Isoform 2 lacks transferase activity but acts as a negative regulator of isoform 1.
Gene Name:
UGT1A9
Uniprot ID:
O60656
Molecular Weight:
59940.495 Da
References
  1. Gomo C, Coriat R, Faivre L, Mir O, Ropert S, Billemont B, Dauphin A, Tod M, Goldwasser F, Blanchet B: Pharmacokinetic interaction involving sorafenib and the calcium-channel blocker felodipine in a patient with hepatocellular carcinoma. Invest New Drugs. 2011 Dec;29(6):1511-4. doi: 10.1007/s10637-010-9514-3. Epub 2010 Aug 13. [PubMed:20706860 ]
  2. van Erp NP, Gelderblom H, Guchelaar HJ: Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev. 2009 Dec;35(8):692-706. doi: 10.1016/j.ctrv.2009.08.004. Epub 2009 Sep 5. [PubMed:19733976 ]
  3. Keating GM, Santoro A: Sorafenib: a review of its use in advanced hepatocellular carcinoma. Drugs. 2009;69(2):223-40. doi: 10.2165/00003495-200969020-00006. [PubMed:19228077 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid binding
Specific Function:
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the IX-alpha-C8 and IX-alpha-C12 monoconjugates and diconjugate. Is also able to catalyze the glucuronidation of 17beta-estradiol, 17alpha-ethinylestradiol, 1-hydroxypyrene, 4-methylumbelliferone, 1-naph...
Gene Name:
UGT1A1
Uniprot ID:
P22309
Molecular Weight:
59590.91 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Atpase activity, coupled to transmembrane movement of substances
Specific Function:
May be an organic anion pump relevant to cellular detoxification.
Gene Name:
ABCC4
Uniprot ID:
O15439
Molecular Weight:
149525.33 Da
References
  1. Hu S, Chen Z, Franke R, Orwick S, Zhao M, Rudek MA, Sparreboom A, Baker SD: Interaction of the multikinase inhibitors sorafenib and sunitinib with solute carriers and ATP-binding cassette transporters. Clin Cancer Res. 2009 Oct 1;15(19):6062-9. doi: 10.1158/1078-0432.CCR-09-0048. Epub 2009 Sep 22. [PubMed:19773380 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Hu S, Chen Z, Franke R, Orwick S, Zhao M, Rudek MA, Sparreboom A, Baker SD: Interaction of the multikinase inhibitors sorafenib and sunitinib with solute carriers and ATP-binding cassette transporters. Clin Cancer Res. 2009 Oct 1;15(19):6062-9. doi: 10.1158/1078-0432.CCR-09-0048. Epub 2009 Sep 22. [PubMed:19773380 ]
  2. Lagas JS, van Waterschoot RA, Sparidans RW, Wagenaar E, Beijnen JH, Schinkel AH: Breast cancer resistance protein and P-glycoprotein limit sorafenib brain accumulation. Mol Cancer Ther. 2010 Feb;9(2):319-26. doi: 10.1158/1535-7163.MCT-09-0663. Epub 2010 Jan 26. [PubMed:20103600 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Organic anion transmembrane transporter activity
Specific Function:
Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
Gene Name:
ABCC2
Uniprot ID:
Q92887
Molecular Weight:
174205.64 Da
References
  1. Hu S, Chen Z, Franke R, Orwick S, Zhao M, Rudek MA, Sparreboom A, Baker SD: Interaction of the multikinase inhibitors sorafenib and sunitinib with solute carriers and ATP-binding cassette transporters. Clin Cancer Res. 2009 Oct 1;15(19):6062-9. doi: 10.1158/1078-0432.CCR-09-0048. Epub 2009 Sep 22. [PubMed:19773380 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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. Hu S, Chen Z, Franke R, Orwick S, Zhao M, Rudek MA, Sparreboom A, Baker SD: Interaction of the multikinase inhibitors sorafenib and sunitinib with solute carriers and ATP-binding cassette transporters. Clin Cancer Res. 2009 Oct 1;15(19):6062-9. doi: 10.1158/1078-0432.CCR-09-0048. Epub 2009 Sep 22. [PubMed:19773380 ]
  2. Lagas JS, van Waterschoot RA, Sparidans RW, Wagenaar E, Beijnen JH, Schinkel AH: Breast cancer resistance protein and P-glycoprotein limit sorafenib brain accumulation. Mol Cancer Ther. 2010 Feb;9(2):319-26. doi: 10.1158/1535-7163.MCT-09-0663. Epub 2010 Jan 26. [PubMed:20103600 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Transmembrane transporter activity
Specific Function:
Can activate specifically hydrolysis of GTP bound to RAC1 and CDC42, but not RALA. Mediates ATP-dependent transport of S-(2,4-dinitrophenyl)-glutathione (DNP-SG) and doxorubicin (DOX) and is the major ATP-dependent transporter of glutathione conjugates of electrophiles (GS-E) and DOX in erythrocytes. Can catalyze transport of glutathione conjugates and xenobiotics, and may contribute to the mul...
Gene Name:
RALBP1
Uniprot ID:
Q15311
Molecular Weight:
76062.86 Da
References
  1. Singhal SS, Sehrawat A, Sahu M, Singhal P, Vatsyayan R, Rao Lelsani PC, Yadav S, Awasthi S: Rlip76 transports sunitinib and sorafenib and mediates drug resistance in kidney cancer. Int J Cancer. 2010 Mar 15;126(6):1327-38. doi: 10.1002/ijc.24767. [PubMed:19626587 ]
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Drug created on June 13, 2005 07:24 / Updated on December 09, 2016 02:38