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Identification
NameSunitinib
Accession NumberDB01268  (DB07417)
TypeSmall Molecule
GroupsApproved, Investigational
DescriptionSunitinib is an oral, small-molecule, multi-targeted receptor tyrosine kinase (RTK) inhibitor that was approved by the FDA for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST) on January 26, 2006. Sunitinib inhibits cellular signaling by targeting multiple RTKs. These include all platelet-derived growth factor receptors (PDGF-R) and vascular endothelial growth factor receptors (VEGF-R). Sunitinib also inhibits KIT (CD117), the RTK that drives the majority of GISTs. In addition, sunitinib inhibits other RTKs including RET, CSF-1R, and flt3.
Structure
Thumb
Synonyms
Sunitinibum
External Identifiers
  • SU-011248
  • SU-11248
  • SU011248
  • SU11248
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
SutentCapsule37.5 mgOralPfizer Canada IncNot applicableNot applicableCanada
SutentCapsule12.5 mg/1OralPfizer Laboratories Div Pfizer Inc2006-01-26Not applicableUs
SutentCapsule37.5 mgOralPfizer Limited2006-07-19Not applicableEu
SutentCapsule12.5 mgOralPfizer Limited2006-07-19Not applicableEu
SutentCapsule12.5 mgOralPfizer Canada Inc2006-06-22Not applicableCanada
SutentCapsule12.5 mgOralPfizer Limited2006-07-19Not applicableEu
SutentCapsule25 mg/1OralPfizer Laboratories Div Pfizer Inc2006-01-26Not applicableUs
SutentCapsule25 mgOralPfizer Limited2006-07-19Not applicableEu
SutentCapsule25 mgOralPfizer Canada Inc2006-06-22Not applicableCanada
SutentCapsule25 mgOralPfizer Limited2006-07-19Not applicableEu
SutentCapsule37.5 mg/1OralPfizer Laboratories Div Pfizer Inc2014-07-12Not applicableUs
SutentCapsule50 mgOralPfizer Limited2006-07-19Not applicableEu
SutentCapsule50 mgOralPfizer Canada Inc2006-06-22Not applicableCanada
SutentCapsule50 mgOralPfizer Limited2006-07-19Not applicableEu
SutentCapsule50 mg/1OralPfizer Laboratories Div Pfizer Inc2006-01-26Not applicableUs
SutentCapsule37.5 mgOralPfizer Limited2006-07-19Not 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
Sunitinib malate
341031-54-7
Thumb
  • InChI Key: LBWFXVZLPYTWQI-IPOVEDGCSA-N
  • Monoisotopic Mass: 532.233327635
  • Average Mass: 532.5612
DBSALT000166
Categories
UNIIV99T50803M
CAS number557795-19-4
WeightAverage: 398.4738
Monoisotopic: 398.211804333
Chemical FormulaC22H27FN4O2
InChI KeyWINHZLLDWRZWRT-ATVHPVEESA-N
InChI
InChI=1S/C22H27FN4O2/c1-5-27(6-2)10-9-24-22(29)20-13(3)19(25-14(20)4)12-17-16-11-15(23)7-8-18(16)26-21(17)28/h7-8,11-12,25H,5-6,9-10H2,1-4H3,(H,24,29)(H,26,28)/b17-12-
IUPAC Name
N-[2-(diethylamino)ethyl]-5-{[(3Z)-5-fluoro-2-oxo-2,3-dihydro-1H-indol-3-ylidene]methyl}-2,4-dimethyl-1H-pyrrole-3-carboxamide
SMILES
CCN(CC)CCNC(=O)C1=C(C)NC(\C=C2/C(=O)NC3=C2C=C(F)C=C3)=C1C
Pharmacology
IndicationFor the treatment of advanced renal cell carcinoma as well as the treatment of gastrointestinal stromal tumor after disease progression on or intolerance to imatinib mesylate.
Structured Indications
PharmacodynamicsSunitinib is an oral, small-molecule, multi-targeted receptor tyrosine kinase (RTK) inhibitor that was approved by the FDA on January 26, 2006.
Mechanism of actionSunitinib is a small molecule that inhibits multiple RTKs, some of which are implicated in tumor growth, pathologic angiogenesis, and metastatic progression of cancer. Sunitinib was evaluated for its inhibitory activity against a variety of kinases (>80 kinases) and was identified as an inhibitor of platelet-derived growth factor receptors (PDGFRa and PDGFRb), vascular endothelial growth factor receptors (VEGFR1, VEGFR2 and VEGFR3), stem cell factor receptor (KIT), Fms-like tyrosine kinase-3 (FLT3), colony stimulating factor receptor Type 1 (CSF-1R), and the glial cell-line derived neurotrophic factor receptor (RET). Sunitinib inhibition of the activity of these RTKs has been demonstrated in biochemical and cellular assays, and inhibition of function has been demonstrated in cell proliferation assays. The primary metabolite exhibits similar potency compared to sunitinib in biochemical and cellular assays.
TargetKindPharmacological actionActionsOrganismUniProt ID
Platelet-derived growth factor receptor betaProteinyes
inhibitor
HumanP09619 details
Vascular endothelial growth factor receptor 1Proteinyes
inhibitor
HumanP17948 details
Mast/stem cell growth factor receptor KitProteinyes
inhibitor
HumanP10721 details
Vascular endothelial growth factor receptor 2Proteinyes
inhibitor
HumanP35968 details
Vascular endothelial growth factor receptor 3Proteinyes
inhibitor
HumanP35916 details
Receptor-type tyrosine-protein kinase FLT3Proteinyes
inhibitor
HumanP36888 details
Macrophage colony-stimulating factor 1 receptorProteinyes
Inhibitor
HumanP07333 details
Platelet-derived growth factor receptor alphaProteinyes
inhibitor
HumanP16234 details
Related Articles
AbsorptionMaximum plasma concentrations (Cmax) of sunitinib are generally observed between 6 and 12 hours (Tmax) following oral administration. Food has no effect on the bioavailability of sunitinib. Sunitinib may be taken with or without food. The pharmacokinetics were similar in healthy volunteers and in the solid tumor patient populations tested, including patients with GIST and RCC.
Volume of distribution
  • 2230 L (apparent volume of distribution, Vd/F)
Protein bindingBinding of sunitinib and its primary metabolite to human plasma protein in vitro was 95% and 90%, respectively.
Metabolism

Sunitinib is metabolized primarily by the cytochrome P450 enzyme, CYP3A4, to produce its primary active metabolite, which is further metabolized by CYP3A4.

Route of eliminationSunitinib is metabolized primarily by the cytochrome P450 enzyme, CYP3A4, to produce its primary active metabolite, which is further metabolized by CYP3A4. Elimination is primarily via feces. In a human mass balance study of [14C]sunitinib, 61% of the dose was eliminated in feces, with renal elimination accounting for 16% of the administered dose.
Half lifeFollowing administration of a single oral dose in healthy volunteers, the terminal half-lives of sunitinib and its primary active metabolite are approximately 40 to 60 hours and 80 to 110 hours, respectively.
Clearance
  • 34 – 62 L/h [Total oral clearance]
ToxicityThe maximally tolerated dose for rat, mouse, and dog when given orally is greater than 500 mg/kg. The maximally tolerated dose of a non-human primate is greater 1200 mg/kg.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
2-HYDROXY-1,4-NAPHTHOQUINONEThe metabolism of Sunitinib can be decreased when combined with 2-HYDROXY-1,4-NAPHTHOQUINONE.Experimental
2-mercaptobenzothiazoleThe metabolism of Sunitinib can be decreased when combined with 2-mercaptobenzothiazole.Vet Approved
7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE may increase the hypoglycemic activities of Sunitinib.Experimental
AcarboseAcarbose may increase the hypoglycemic activities of Sunitinib.Approved, Investigational
AcebutololThe serum concentration of Acebutolol can be increased when it is combined with Sunitinib.Approved
AcetaminophenThe serum concentration of Acetaminophen can be increased when it is combined with Sunitinib.Approved
AcetohexamideAcetohexamide may increase the hypoglycemic activities of Sunitinib.Withdrawn
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Sunitinib.Approved
Acetylsalicylic acidThe serum concentration of Acetylsalicylic acid can be increased when it is combined with Sunitinib.Approved, Vet Approved
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Sunitinib.Approved
AicarAicar may increase the hypoglycemic activities of Sunitinib.Experimental
AldosteroneThe serum concentration of Aldosterone can be increased when it is combined with Sunitinib.Experimental
AlitretinoinThe serum concentration of Alitretinoin can be increased when it is combined with Sunitinib.Approved, Investigational
AlogliptinAlogliptin may increase the hypoglycemic activities of Sunitinib.Approved
ALT-110The risk or severity of adverse effects can be increased when Sunitinib is combined with ALT-110.Investigational
AmbrisentanThe serum concentration of Ambrisentan can be increased when it is combined with Sunitinib.Approved, Investigational
Aminosalicylic AcidAminosalicylic Acid may increase the hypoglycemic activities of Sunitinib.Approved
AmiodaroneThe metabolism of Sunitinib can be decreased when combined with Amiodarone.Approved, Investigational
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Sunitinib.Approved
AmorolfineThe metabolism of Sunitinib can be decreased when combined with Amorolfine.Approved
Amphotericin BThe metabolism of Sunitinib can be decreased when combined with Amphotericin B.Approved, Investigational
AN2690The metabolism of Sunitinib can be decreased when combined with AN2690.Investigational
AnagrelideSunitinib may increase the QTc-prolonging activities of Anagrelide.Approved
AnidulafunginThe metabolism of Sunitinib can be decreased when combined with Anidulafungin.Approved, Investigational
AnvirzelAnvirzel may decrease the cardiotoxic activities of Sunitinib.Investigational
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Sunitinib.Approved
AprepitantThe serum concentration of Sunitinib can be increased when it is combined with Aprepitant.Approved, Investigational
Arsenic trioxideSunitinib may increase the QTc-prolonging activities of Arsenic trioxide.Approved, Investigational
ArtemetherThe metabolism of Sunitinib can be decreased when combined with Artemether.Approved
AsenapineSunitinib may increase the QTc-prolonging activities of Asenapine.Approved
AtazanavirThe metabolism of Sunitinib can be decreased when combined with Atazanavir.Approved, Investigational
AtenololThe serum concentration of Atenolol can be increased when it is combined with Sunitinib.Approved
AtomoxetineThe metabolism of Sunitinib can be decreased when combined with Atomoxetine.Approved
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Sunitinib.Approved, Investigational
AzithromycinSunitinib may increase the QTc-prolonging activities of Azithromycin.Approved
Bafilomycin A1The metabolism of Sunitinib can be decreased when combined with Bafilomycin A1.Experimental
BalaglitazoneBalaglitazone may increase the hypoglycemic activities of Sunitinib.Investigational
BalsalazideBalsalazide may increase the hypoglycemic activities of Sunitinib.Approved, Investigational
BcgThe therapeutic efficacy of Bcg can be decreased when used in combination with Sunitinib.Investigational
BedaquilineSunitinib may increase the QTc-prolonging activities of Bedaquiline.Approved
BenmoxinBenmoxin may increase the hypoglycemic activities of Sunitinib.Withdrawn
Benzoic AcidThe metabolism of Sunitinib can be decreased when combined with Benzoic Acid.Approved
BetamethasoneThe serum concentration of Betamethasone can be increased when it is combined with Sunitinib.Approved, Vet Approved
BevacizumabThe risk or severity of adverse effects can be increased when Sunitinib is combined with Bevacizumab.Approved, Investigational
BexaroteneThe serum concentration of Sunitinib can be decreased when it is combined with Bexarotene.Approved, Investigational
BifonazoleThe metabolism of Sunitinib can be decreased when combined with Bifonazole.Approved
BoceprevirThe metabolism of Sunitinib can be decreased when combined with Boceprevir.Approved
BortezomibThe metabolism of Sunitinib can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Sunitinib can be decreased when it is combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Sunitinib.Approved
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Sunitinib.Approved
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Sunitinib.Approved, Investigational
BuforminBuformin may increase the hypoglycemic activities of Sunitinib.Withdrawn
ButenafineThe metabolism of Sunitinib can be decreased when combined with Butenafine.Approved
ButoconazoleThe metabolism of Sunitinib can be decreased when combined with Butoconazole.Approved
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Sunitinib.Approved
CaffeineThe serum concentration of Caffeine can be increased when it is combined with Sunitinib.Approved
CamptothecinThe serum concentration of Camptothecin can be increased when it is combined with Sunitinib.Experimental
CanagliflozinThe serum concentration of Canagliflozin can be increased when it is combined with Sunitinib.Approved
CandicidinThe metabolism of Sunitinib can be decreased when combined with Candicidin.Withdrawn
CarbamazepineThe serum concentration of Sunitinib can be decreased when it is combined with Carbamazepine.Approved, Investigational
CarfilzomibThe serum concentration of Carfilzomib can be increased when it is combined with Sunitinib.Approved
CaroxazoneCaroxazone may increase the hypoglycemic activities of Sunitinib.Withdrawn
CaspofunginThe metabolism of Sunitinib can be decreased when combined with Caspofungin.Approved
CastanospermineCastanospermine may increase the hypoglycemic activities of Sunitinib.Experimental
CDX-110The risk or severity of adverse effects can be increased when Sunitinib is combined with CDX-110.Investigational
CeritinibThe serum concentration of Sunitinib can be increased when it is combined with Ceritinib.Approved
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Sunitinib.Withdrawn
CeruleninThe metabolism of Sunitinib can be decreased when combined with Cerulenin.Approved
ChloroquineSunitinib may increase the QTc-prolonging activities of Chloroquine.Approved, Vet Approved
ChloroxineThe metabolism of Sunitinib can be decreased when combined with Chloroxine.Approved
ChlorpromazineSunitinib may increase the QTc-prolonging activities of Chlorpromazine.Approved, Vet Approved
ChlorpropamideChlorpropamide may increase the hypoglycemic activities of Sunitinib.Approved
CiclopiroxThe metabolism of Sunitinib can be decreased when combined with Ciclopirox.Approved, Investigational
CiglitazoneCiglitazone may increase the hypoglycemic activities of Sunitinib.Experimental
CimetidineThe serum concentration of Cimetidine can be increased when it is combined with Sunitinib.Approved
CinoxacinCinoxacin may increase the hypoglycemic activities of Sunitinib.Approved, Withdrawn
CiprofloxacinSunitinib may increase the QTc-prolonging activities of Ciprofloxacin.Approved, Investigational
CisaprideSunitinib may increase the QTc-prolonging activities of Cisapride.Approved, Investigational, Withdrawn
CisplatinThe serum concentration of Cisplatin can be increased when it is combined with Sunitinib.Approved
CitalopramSunitinib may increase the QTc-prolonging activities of Citalopram.Approved
ClarithromycinThe metabolism of Sunitinib can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Sunitinib can be decreased when combined with Clemastine.Approved
ClobazamThe serum concentration of Clobazam can be increased when it is combined with Sunitinib.Approved, Illicit
ClomifeneThe serum concentration of Clomifene can be increased when it is combined with Sunitinib.Approved, Investigational
ClonidineThe serum concentration of Clonidine can be increased when it is combined with Sunitinib.Approved
ClopidogrelThe serum concentration of Clopidogrel can be increased when it is combined with Sunitinib.Approved, Nutraceutical
ClotrimazoleThe metabolism of Sunitinib can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineSunitinib may increase the QTc-prolonging activities of Clozapine.Approved
CobicistatThe metabolism of Sunitinib can be decreased when combined with Cobicistat.Approved
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Sunitinib.Approved
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Sunitinib.Approved
ConivaptanThe serum concentration of Sunitinib 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 Sunitinib.Approved
CordycepinThe metabolism of Sunitinib can be decreased when combined with Cordycepin.Investigational
CrizotinibSunitinib may increase the QTc-prolonging activities of Crizotinib.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Sunitinib.Approved, Investigational
CyclosporineThe metabolism of Sunitinib 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 Sunitinib.Approved
DabrafenibThe serum concentration of Sunitinib can be decreased when it is combined with Dabrafenib.Approved
DactinomycinThe serum concentration of Dactinomycin can be increased when it is combined with Sunitinib.Approved
DapagliflozinThe serum concentration of Dapagliflozin can be increased when it is combined with Sunitinib.Approved
DapoxetineDapoxetine may increase the hypoglycemic activities of Sunitinib.Investigational
DarunavirThe metabolism of Sunitinib can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Sunitinib can be increased when it is combined with Dasatinib.Approved, Investigational
DaunorubicinThe serum concentration of Daunorubicin can be increased when it is combined with Sunitinib.Approved
DebrisoquinThe serum concentration of Debrisoquin can be increased when it is combined with Sunitinib.Approved
Decanoic AcidThe metabolism of Sunitinib can be decreased when combined with Decanoic Acid.Experimental
DeferasiroxThe serum concentration of Sunitinib can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Sunitinib can be decreased when combined with Delavirdine.Approved
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Sunitinib.Approved
DeoxyspergualinDeoxyspergualin may increase the hypoglycemic activities of Sunitinib.Investigational
dersalazinedersalazine may increase the hypoglycemic activities of Sunitinib.Investigational
DeslanosideDeslanoside may decrease the cardiotoxic activities of Sunitinib.Approved
DesvenlafaxineDesvenlafaxine may increase the hypoglycemic activities of Sunitinib.Approved
DexamethasoneThe serum concentration of Sunitinib can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Sunitinib.Approved, Illicit, Vet Approved
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be increased when it is combined with Sunitinib.Approved
DiflunisalDiflunisal may increase the hypoglycemic activities of Sunitinib.Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Sunitinib.Approved
DigoxinDigoxin may decrease the cardiotoxic activities of Sunitinib.Approved
DihydroergotamineThe metabolism of Sunitinib can be decreased when combined with Dihydroergotamine.Approved
DihydrotestosteroneThe serum concentration of Dihydrotestosterone can be increased when it is combined with Sunitinib.Illicit
DiltiazemThe metabolism of Sunitinib can be decreased when combined with Diltiazem.Approved
DipyridamoleThe serum concentration of Dipyridamole can be increased when it is combined with Sunitinib.Approved
DisopyramideSunitinib may increase the QTc-prolonging activities of Disopyramide.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Sunitinib.Approved, Investigational
DofetilideSunitinib may increase the QTc-prolonging activities of Dofetilide.Approved
DolasetronSunitinib may increase the QTc-prolonging activities of Dolasetron.Approved
DomperidoneSunitinib may increase the QTc-prolonging activities of Domperidone.Approved, Investigational, Vet Approved
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Sunitinib.Approved, Investigational
DoxycyclineThe metabolism of Sunitinib can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneSunitinib may increase the QTc-prolonging activities of Dronedarone.Approved
DroperidolSunitinib may increase the QTc-prolonging activities of Droperidol.Approved, Vet Approved
DulaglutideDulaglutide may increase the hypoglycemic activities of Sunitinib.Approved
DuloxetineDuloxetine may increase the hypoglycemic activities of Sunitinib.Approved
EconazoleThe metabolism of Sunitinib can be decreased when combined with Econazole.Approved
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Sunitinib.Approved
EfavirenzThe serum concentration of Sunitinib can be decreased when it is combined with Efavirenz.Approved, Investigational
EfinaconazoleThe metabolism of Sunitinib can be decreased when combined with Efinaconazole.Approved
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Sunitinib.Approved, Investigational
EliglustatSunitinib may increase the QTc-prolonging activities of Eliglustat.Approved
EmpagliflozinEmpagliflozin may increase the hypoglycemic activities of Sunitinib.Approved
EnoxacinEnoxacin may increase the hypoglycemic activities of Sunitinib.Approved
EnzalutamideThe serum concentration of Sunitinib can be decreased when it is combined with Enzalutamide.Approved
EpinastineThe serum concentration of Epinastine can be increased when it is combined with Sunitinib.Approved, Investigational
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Sunitinib.Approved, Investigational
ErythromycinSunitinib may increase the QTc-prolonging activities of Erythromycin.Approved, Vet Approved
EscitalopramSunitinib may increase the QTc-prolonging activities of Escitalopram.Approved, Investigational
Eslicarbazepine acetateThe serum concentration of Sunitinib can be decreased when it is combined with Eslicarbazepine acetate.Approved
EstradiolThe serum concentration of Estradiol can be increased when it is combined with Sunitinib.Approved, Investigational, Vet Approved
EstriolThe serum concentration of Estriol can be increased when it is combined with Sunitinib.Approved, Vet Approved
EstroneThe serum concentration of Estrone can be increased when it is combined with Sunitinib.Approved
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be increased when it is combined with Sunitinib.Approved
EtoperidoneEtoperidone may increase the hypoglycemic activities of Sunitinib.Approved
EtoposideThe serum concentration of Etoposide can be increased when it is combined with Sunitinib.Approved
EtravirineThe serum concentration of Sunitinib can be decreased when it is combined with Etravirine.Approved
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Sunitinib.Approved
ExenatideExenatide may increase the hypoglycemic activities of Sunitinib.Approved, Investigational
EzetimibeThe serum concentration of Ezetimibe can be increased when it is combined with Sunitinib.Approved
FesoterodineThe serum concentration of Fesoterodine can be increased when it is combined with Sunitinib.Approved
FexofenadineThe serum concentration of Fexofenadine can be increased when it is combined with Sunitinib.Approved
FidaxomicinThe serum concentration of Fidaxomicin can be increased when it is combined with Sunitinib.Approved
FingolimodSunitinib may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
FlecainideSunitinib may increase the QTc-prolonging activities of Flecainide.Approved, Withdrawn
FleroxacinFleroxacin may increase the hypoglycemic activities of Sunitinib.Approved
FluconazoleThe metabolism of Sunitinib can be decreased when combined with Fluconazole.Approved
FlucytosineThe metabolism of Sunitinib can be decreased when combined with Flucytosine.Approved
FlumequineFlumequine may increase the hypoglycemic activities of Sunitinib.Withdrawn
FluoxetineSunitinib may increase the QTc-prolonging activities of Fluoxetine.Approved, Vet Approved
FluoxymesteroneFluoxymesterone may increase the hypoglycemic activities of Sunitinib.Approved, Illicit
FlupentixolSunitinib may increase the QTc-prolonging activities of Flupentixol.Approved, Withdrawn
Fluticasone furoateThe serum concentration of Fluticasone furoate can be increased when it is combined with Sunitinib.Approved
FluvoxamineThe metabolism of Sunitinib can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Sunitinib can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Sunitinib can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe serum concentration of Sunitinib can be decreased when it is combined with Fosphenytoin.Approved
FurazolidoneFurazolidone may increase the hypoglycemic activities of Sunitinib.Approved, Vet Approved
Fusidic AcidThe serum concentration of Sunitinib can be increased when it is combined with Fusidic Acid.Approved
G17DTThe risk or severity of adverse effects can be increased when Sunitinib is combined with G17DT.Investigational
Gadobenic acidSunitinib may increase the QTc-prolonging activities of Gadobenic acid.Approved
GarenoxacinGarenoxacin may increase the hypoglycemic activities of Sunitinib.Investigational
GatifloxacinGatifloxacin may increase the hypoglycemic activities of Sunitinib.Approved, Investigational
GefitinibThe serum concentration of Gefitinib can be increased when it is combined with Sunitinib.Approved, Investigational
GemcitabineThe serum concentration of Gemcitabine can be increased when it is combined with Sunitinib.Approved
GemifloxacinSunitinib may increase the QTc-prolonging activities of Gemifloxacin.Approved, Investigational
GI-5005The risk or severity of adverse effects can be increased when Sunitinib is combined with GI-5005.Investigational
GlibornurideGlibornuride may increase the hypoglycemic activities of Sunitinib.Withdrawn
GliclazideGliclazide may increase the hypoglycemic activities of Sunitinib.Approved
GlimepirideGlimepiride may increase the hypoglycemic activities of Sunitinib.Approved
GlipizideGlipizide may increase the hypoglycemic activities of Sunitinib.Approved
GliquidoneGliquidone may increase the hypoglycemic activities of Sunitinib.Approved
GlyburideGlyburide may increase the hypoglycemic activities of Sunitinib.Approved
GlyphosateThe metabolism of Sunitinib can be decreased when combined with Glyphosate.Experimental
GoserelinSunitinib may increase the QTc-prolonging activities of Goserelin.Approved
GranisetronSunitinib may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
GrazoprevirThe serum concentration of Grazoprevir can be increased when it is combined with Sunitinib.Approved
GrepafloxacinThe serum concentration of Grepafloxacin can be increased when it is combined with Sunitinib.Withdrawn
GriseofulvinThe metabolism of Sunitinib can be decreased when combined with Griseofulvin.Approved, Vet Approved
GusperimusGusperimus may increase the hypoglycemic activities of Sunitinib.Investigational
HaloperidolSunitinib may increase the QTc-prolonging activities of Haloperidol.Approved
HaloproginThe metabolism of Sunitinib can be decreased when combined with Haloprogin.Approved, Withdrawn
HexetidineThe metabolism of Sunitinib can be decreased when combined with Hexetidine.Approved
HydracarbazineHydracarbazine may increase the hypoglycemic activities of Sunitinib.Approved
HydrocortisoneThe serum concentration of Hydrocortisone can be increased when it is combined with Sunitinib.Approved, Vet Approved
IbuprofenThe serum concentration of Ibuprofen can be increased when it is combined with Sunitinib.Approved
IbutilideSunitinib may increase the QTc-prolonging activities of Ibutilide.Approved
IdelalisibThe serum concentration of Sunitinib can be increased when it is combined with Idelalisib.Approved
IloperidoneSunitinib may increase the QTc-prolonging activities of Iloperidone.Approved
ImatinibThe metabolism of Sunitinib can be decreased when combined with Imatinib.Approved
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Sunitinib.Approved
IndacaterolThe serum concentration of Indacaterol can be increased when it is combined with Sunitinib.Approved
IndalpineIndalpine may increase the hypoglycemic activities of Sunitinib.Investigational, Withdrawn
IndinavirThe metabolism of Sunitinib can be decreased when combined with Indinavir.Approved
IndomethacinThe serum concentration of Indomethacin can be increased when it is combined with Sunitinib.Approved, Investigational
INGN 201The risk or severity of adverse effects can be increased when Sunitinib is combined with INGN 201.Investigational
INGN 225The risk or severity of adverse effects can be increased when Sunitinib is combined with INGN 225.Investigational
Insulin AspartSunitinib may increase the hypoglycemic activities of Insulin Aspart.Approved
Insulin DetemirSunitinib may increase the hypoglycemic activities of Insulin Detemir.Approved
Insulin GlargineInsulin Glargine may increase the hypoglycemic activities of Sunitinib.Approved
Insulin GlulisineSunitinib may increase the hypoglycemic activities of Insulin Glulisine.Approved
Insulin HumanInsulin Human may increase the hypoglycemic activities of Sunitinib.Approved, Investigational
Insulin LisproInsulin Lispro may increase the hypoglycemic activities of Sunitinib.Approved
Insulin PorkInsulin Pork may increase the hypoglycemic activities of Sunitinib.Approved
IproclozideIproclozide may increase the hypoglycemic activities of Sunitinib.Withdrawn
IproniazidIproniazid may increase the hypoglycemic activities of Sunitinib.Withdrawn
IrinotecanThe serum concentration of Irinotecan can be increased when it is combined with Sunitinib.Approved, Investigational
IsavuconazoniumThe metabolism of Sunitinib can be decreased when combined with Isavuconazonium.Approved, Investigational
IsocarboxazidIsocarboxazid may increase the hypoglycemic activities of Sunitinib.Approved
IsoconazoleThe metabolism of Sunitinib can be decreased when combined with Isoconazole.Approved
IsradipineThe metabolism of Sunitinib can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Sunitinib can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Sunitinib can be increased when it is combined with Ivacaftor.Approved
IvermectinThe serum concentration of Ivermectin can be increased when it is combined with Sunitinib.Approved, Vet Approved
KetazolamThe serum concentration of Ketazolam can be increased when it is combined with Sunitinib.Approved
KetoconazoleThe metabolism of Sunitinib can be decreased when combined with Ketoconazole.Approved, Investigational
LamivudineThe serum concentration of Lamivudine can be increased when it is combined with Sunitinib.Approved, Investigational
LamotrigineThe serum concentration of Lamotrigine can be increased when it is combined with Sunitinib.Approved, Investigational
LanreotideSunitinib may increase the hypoglycemic activities of Lanreotide.Approved
LansoprazoleThe serum concentration of Lansoprazole can be increased when it is combined with Sunitinib.Approved, Investigational
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Sunitinib.Approved
LeflunomideThe risk or severity of adverse effects can be increased when Sunitinib is combined with Leflunomide.Approved, Investigational
LenalidomideThe serum concentration of Lenalidomide can be increased when it is combined with Sunitinib.Approved
LenvatinibSunitinib may increase the QTc-prolonging activities of Lenvatinib.Approved
LeuprolideSunitinib may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
LevetiracetamThe serum concentration of Levetiracetam can be increased when it is combined with Sunitinib.Approved, Investigational
LevofloxacinSunitinib may increase the QTc-prolonging activities of Levofloxacin.Approved, Investigational
LevomilnacipranThe serum concentration of Levomilnacipran can be increased when it is combined with Sunitinib.Approved
LinagliptinThe serum concentration of Linagliptin can be increased when it is combined with Sunitinib.Approved
LiraglutideLiraglutide may increase the hypoglycemic activities of Sunitinib.Approved
LomefloxacinLomefloxacin may increase the hypoglycemic activities of Sunitinib.Approved
LoperamideThe serum concentration of Loperamide can be increased when it is combined with Sunitinib.Approved
LopinavirThe metabolism of Sunitinib can be decreased when combined with Lopinavir.Approved
LosartanThe serum concentration of Losartan can be increased when it is combined with Sunitinib.Approved
LovastatinThe metabolism of Sunitinib can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Sunitinib can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Sunitinib can be decreased when it is combined with Lumacaftor.Approved
LumefantrineSunitinib may increase the QTc-prolonging activities of Lumefantrine.Approved
MannitolThe serum concentration of Mannitol can be increased when it is combined with Sunitinib.Approved, Investigational
MebanazineMebanazine may increase the hypoglycemic activities of Sunitinib.Withdrawn
MecaserminSunitinib may increase the hypoglycemic activities of Mecasermin.Approved, Investigational
MesalazineMesalazine may increase the hypoglycemic activities of Sunitinib.Approved
MetforminMetformin may increase the hypoglycemic activities of Sunitinib.Approved
MethadoneSunitinib may increase the QTc-prolonging activities of Methadone.Approved
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Sunitinib.Approved
Methylene blueMethylene blue may increase the hypoglycemic activities of Sunitinib.Investigational
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Sunitinib.Approved, Vet Approved
MethyltestosteroneMethyltestosterone may increase the hypoglycemic activities of Sunitinib.Approved
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Sunitinib.Approved, Investigational
MevastatinThe metabolism of Sunitinib can be decreased when combined with Mevastatin.Experimental
MicafunginThe metabolism of Sunitinib can be decreased when combined with Micafungin.Approved, Investigational
MiconazoleThe metabolism of Sunitinib can be decreased when combined with Miconazole.Approved, Investigational, Vet Approved
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Sunitinib.Approved, Illicit
MifepristoneMifepristone may increase the QTc-prolonging activities of Sunitinib.Approved, Investigational
MiglitolMiglitol may increase the hypoglycemic activities of Sunitinib.Approved
MiglustatMiglustat may increase the hypoglycemic activities of Sunitinib.Approved
MilnacipranMilnacipran may increase the hypoglycemic activities of Sunitinib.Approved
MiltefosineThe metabolism of Sunitinib can be decreased when combined with Miltefosine.Approved
MinaprineMinaprine may increase the hypoglycemic activities of Sunitinib.Approved
MirabegronThe serum concentration of Mirabegron can be increased when it is combined with Sunitinib.Approved
MitiglinideMitiglinide may increase the hypoglycemic activities of Sunitinib.Approved, Investigational
MitotaneThe serum concentration of Sunitinib can be decreased when it is combined with Mitotane.Approved
MitoxantroneThe serum concentration of Mitoxantrone can be increased when it is combined with Sunitinib.Approved, Investigational
MoclobemideMoclobemide may increase the hypoglycemic activities of Sunitinib.Approved
ModafinilThe serum concentration of Sunitinib can be decreased when it is combined with Modafinil.Approved, Investigational
MonensinThe metabolism of Sunitinib can be decreased when combined with Monensin.Vet Approved
MorphineThe serum concentration of Morphine can be increased when it is combined with Sunitinib.Approved, Investigational
MoxifloxacinSunitinib 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 Sunitinib.Approved, Investigational
MyxothiazolThe metabolism of Sunitinib can be decreased when combined with Myxothiazol.Experimental
NadololThe serum concentration of Nadolol can be increased when it is combined with Sunitinib.Approved
NafcillinThe serum concentration of Sunitinib can be decreased when it is combined with Nafcillin.Approved
NaftifineThe metabolism of Sunitinib can be decreased when combined with Naftifine.Approved
Nalidixic AcidNalidixic Acid may increase the hypoglycemic activities of Sunitinib.Approved
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Sunitinib.Approved
NaloxoneThe serum concentration of Naloxone can be increased when it is combined with Sunitinib.Approved, Vet Approved
NatalizumabThe risk or severity of adverse effects can be increased when Sunitinib is combined with Natalizumab.Approved, Investigational
NatamycinThe metabolism of Sunitinib can be decreased when combined with Natamycin.Approved
NateglinideNateglinide may increase the hypoglycemic activities of Sunitinib.Approved, Investigational
NCX 4016NCX 4016 may increase the hypoglycemic activities of Sunitinib.Investigational
NefazodoneThe metabolism of Sunitinib can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Sunitinib can be decreased when combined with Nelfinavir.Approved
NemonoxacinNemonoxacin may increase the hypoglycemic activities of Sunitinib.Investigational
NetupitantThe serum concentration of Sunitinib can be increased when it is combined with Netupitant.Approved
NevirapineThe serum concentration of Sunitinib can be decreased when it is combined with Nevirapine.Approved
NialamideNialamide may increase the hypoglycemic activities of Sunitinib.Withdrawn
NicardipineThe serum concentration of Nicardipine can be increased when it is combined with Sunitinib.Approved
NifedipineThe serum concentration of Nifedipine can be increased when it is combined with Sunitinib.Approved
NilotinibSunitinib may increase the QTc-prolonging activities of Nilotinib.Approved, Investigational
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Sunitinib.Approved
NitroaspirinNitroaspirin may increase the hypoglycemic activities of Sunitinib.Investigational
NitroxolineThe metabolism of Sunitinib can be decreased when combined with Nitroxoline.Approved
NizatidineThe serum concentration of Nizatidine can be increased when it is combined with Sunitinib.Approved
NorfloxacinNorfloxacin may increase the hypoglycemic activities of Sunitinib.Approved
NystatinThe metabolism of Sunitinib can be decreased when combined with Nystatin.Approved, Vet Approved
OctamoxinOctamoxin may increase the hypoglycemic activities of Sunitinib.Withdrawn
OctreotideOctreotide may increase the hypoglycemic activities of Sunitinib.Approved, Investigational
OfloxacinSunitinib may increase the QTc-prolonging activities of Ofloxacin.Approved
OlanzapineThe serum concentration of Olanzapine can be increased when it is combined with Sunitinib.Approved, Investigational
OlaparibThe metabolism of Sunitinib can be decreased when combined with Olaparib.Approved
OlsalazineOlsalazine may increase the hypoglycemic activities of Sunitinib.Approved
OmbitasvirThe serum concentration of Ombitasvir can be increased when it is combined with Sunitinib.Approved
OndansetronSunitinib may increase the QTc-prolonging activities of Ondansetron.Approved
OsimertinibThe serum concentration of Sunitinib can be increased when it is combined with Osimertinib.Approved
OuabainOuabain may decrease the cardiotoxic activities of Sunitinib.Approved
OxandroloneOxandrolone may increase the hypoglycemic activities of Sunitinib.Approved, Investigational
OxiconazoleThe metabolism of Sunitinib can be decreased when combined with Oxiconazole.Approved
OxymetholoneOxymetholone may increase the hypoglycemic activities of Sunitinib.Approved, Illicit
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Sunitinib.Approved, Vet Approved
pafuramidineThe metabolism of Sunitinib can be decreased when combined with pafuramidine.Investigational
PalbociclibThe serum concentration of Sunitinib can be increased when it is combined with Palbociclib.Approved
PaliperidoneSunitinib may increase the QTc-prolonging activities of Paliperidone.Approved
PanobinostatSunitinib may increase the QTc-prolonging activities of Panobinostat.Approved, Investigational
PargylinePargyline may increase the hypoglycemic activities of Sunitinib.Approved
ParoxetineParoxetine may increase the hypoglycemic activities of Sunitinib.Approved, Investigational
PasireotideSunitinib may increase the hypoglycemic activities of Pasireotide.Approved
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Sunitinib.Approved
PazufloxacinPazufloxacin may increase the hypoglycemic activities of Sunitinib.Investigational
PefloxacinPefloxacin may increase the hypoglycemic activities of Sunitinib.Approved
PegvisomantPegvisomant may increase the hypoglycemic activities of Sunitinib.Approved
PentamidineThe metabolism of Sunitinib can be decreased when combined with Pentamidine.Approved
PentobarbitalThe serum concentration of Sunitinib can be decreased when it is combined with Pentobarbital.Approved, Vet Approved
PerflutrenSunitinib may increase the QTc-prolonging activities of Perflutren.Approved
PhenelzinePhenelzine may increase the hypoglycemic activities of Sunitinib.Approved
PhenforminPhenformin may increase the hypoglycemic activities of Sunitinib.Approved, Withdrawn
PheniprazinePheniprazine may increase the hypoglycemic activities of Sunitinib.Withdrawn
PhenobarbitalThe serum concentration of Sunitinib can be decreased when it is combined with Phenobarbital.Approved
PhenoxypropazinePhenoxypropazine may increase the hypoglycemic activities of Sunitinib.Withdrawn
PhenytoinThe serum concentration of Sunitinib 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 Sunitinib.Approved, Investigational
PimozideSunitinib may increase the QTc-prolonging activities of Pimozide.Approved
PioglitazonePioglitazone may increase the hypoglycemic activities of Sunitinib.Approved, Investigational
PirlindolePirlindole may increase the hypoglycemic activities of Sunitinib.Approved
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Sunitinib.Approved
PivhydrazinePivhydrazine may increase the hypoglycemic activities of Sunitinib.Withdrawn
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Sunitinib.Approved
PonatinibThe serum concentration of Ponatinib can be increased when it is combined with Sunitinib.Approved
PosaconazoleThe metabolism of Sunitinib can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PramlintidePramlintide may increase the hypoglycemic activities of Sunitinib.Approved, Investigational
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Sunitinib.Approved
PrazosinThe serum concentration of Prazosin can be increased when it is combined with Sunitinib.Approved
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Sunitinib.Approved, Vet Approved
PrednisoneThe serum concentration of Prednisone can be increased when it is combined with Sunitinib.Approved, Vet Approved
PrimaquineSunitinib may increase the QTc-prolonging activities of Primaquine.Approved
PrimidoneThe serum concentration of Sunitinib can be decreased when it is combined with Primidone.Approved, Vet Approved
ProcainamideSunitinib may increase the QTc-prolonging activities of Procainamide.Approved
ProgesteroneThe serum concentration of Progesterone can be increased when it is combined with Sunitinib.Approved, Vet Approved
PromazineSunitinib may increase the QTc-prolonging activities of Promazine.Approved, Vet Approved
PropafenoneSunitinib may increase the QTc-prolonging activities of Propafenone.Approved
PropranololThe serum concentration of Propranolol can be increased when it is combined with Sunitinib.Approved, Investigational
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Sunitinib.Approved
PrulifloxacinPrulifloxacin may increase the hypoglycemic activities of Sunitinib.Investigational
QuetiapineSunitinib may increase the QTc-prolonging activities of Quetiapine.Approved
QuinidineSunitinib may increase the QTc-prolonging activities of Quinidine.Approved
QuinineSunitinib may increase the QTc-prolonging activities of Quinine.Approved
Rabies vaccineThe risk or severity of adverse effects can be increased when Sunitinib is combined with Rabies vaccine.Approved
Rabies vaccineThe therapeutic efficacy of Rabies vaccine can be decreased when used in combination with Sunitinib.Approved
RadicicolThe metabolism of Sunitinib can be decreased when combined with Radicicol.Experimental
RanitidineThe serum concentration of Ranitidine can be increased when it is combined with Sunitinib.Approved
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Sunitinib.Approved, Investigational
RasagilineRasagiline may increase the hypoglycemic activities of Sunitinib.Approved
RepaglinideRepaglinide may increase the hypoglycemic activities of Sunitinib.Approved, Investigational
ReserpineThe serum concentration of Reserpine can be increased when it is combined with Sunitinib.Approved
RifabutinThe serum concentration of Sunitinib can be decreased when it is combined with Rifabutin.Approved
RifampicinThe serum concentration of Sunitinib can be decreased when it is combined with Rifampicin.Approved
RifapentineThe serum concentration of Sunitinib can be decreased when it is combined with Rifapentine.Approved
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Sunitinib.Approved, Investigational
RisperidoneThe serum concentration of Risperidone can be increased when it is combined with Sunitinib.Approved, Investigational
RitonavirThe metabolism of Sunitinib can be decreased when combined with Ritonavir.Approved, Investigational
RivaroxabanThe serum concentration of Rivaroxaban can be increased when it is combined with Sunitinib.Approved
RoflumilastRoflumilast may increase the immunosuppressive activities of Sunitinib.Approved
RomidepsinThe serum concentration of Romidepsin can be increased when it is combined with Sunitinib.Approved, Investigational
RosiglitazoneRosiglitazone may increase the hypoglycemic activities of Sunitinib.Approved, Investigational
RosoxacinRosoxacin may increase the hypoglycemic activities of Sunitinib.Approved
SafrazineSafrazine may increase the hypoglycemic activities of Sunitinib.Withdrawn
Salicylhydroxamic AcidThe metabolism of Sunitinib can be decreased when combined with Salicylhydroxamic Acid.Experimental
Salicylic acidThe metabolism of Sunitinib can be decreased when combined with Salicylic acid.Approved, Vet Approved
SaquinavirThe metabolism of Sunitinib can be decreased when combined with Saquinavir.Approved, Investigational
SaxagliptinSaxagliptin may increase the hypoglycemic activities of Sunitinib.Approved
SelegilineSelegiline may increase the hypoglycemic activities of Sunitinib.Approved, Investigational, Vet Approved
SelexipagThe serum concentration of Selexipag can be increased when it is combined with Sunitinib.Approved
SertaconazoleThe metabolism of Sunitinib can be decreased when combined with Sertaconazole.Approved
SertralineSertraline may increase the hypoglycemic activities of Sunitinib.Approved
SildenafilThe metabolism of Sunitinib can be decreased when combined with Sildenafil.Approved, Investigational
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Sunitinib.Approved
SiltuximabThe serum concentration of Sunitinib can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Sunitinib can be increased when it is combined with Simeprevir.Approved
SinefunginThe metabolism of Sunitinib can be decreased when combined with Sinefungin.Experimental
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Sunitinib.Approved
SirolimusThe metabolism of Sunitinib can be decreased when combined with Sirolimus.Approved, Investigational
SitagliptinThe serum concentration of Sitagliptin can be increased when it is combined with Sunitinib.Approved, Investigational
SofosbuvirThe serum concentration of Sofosbuvir can be increased when it is combined with Sunitinib.Approved
SorafenibThe serum concentration of Sorafenib can be increased when it is combined with Sunitinib.Approved, Investigational
SotalolSunitinib may increase the QTc-prolonging activities of Sotalol.Approved
SparfloxacinThe serum concentration of Sparfloxacin can be increased when it is combined with Sunitinib.Approved
SphingosineThe serum concentration of Sphingosine can be increased when it is combined with Sunitinib.Experimental
SRP 299The risk or severity of adverse effects can be increased when Sunitinib is combined with SRP 299.Investigational
St. John's WortThe serum concentration of Sunitinib can be decreased when it is combined with St. John's Wort.Nutraceutical
StanozololStanozolol may increase the hypoglycemic activities of Sunitinib.Approved, Vet Approved
StiripentolThe serum concentration of Sunitinib can be increased when it is combined with Stiripentol.Approved
SulconazoleThe metabolism of Sunitinib can be decreased when combined with Sulconazole.Approved
SulfadiazineSulfadiazine may increase the hypoglycemic activities of Sunitinib.Approved, Vet Approved
SulfamethoxazoleSulfamethoxazole may increase the hypoglycemic activities of Sunitinib.Approved
SulfisoxazoleSunitinib may increase the QTc-prolonging activities of Sulfisoxazole.Approved, Vet Approved
SulodexideSulodexide may increase the hypoglycemic activities of Sunitinib.Approved, Investigational
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Sunitinib.Approved, Investigational
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Sunitinib.Approved, Investigational
TamoxifenThe serum concentration of Tamoxifen can be increased when it is combined with Sunitinib.Approved
Taurocholic AcidThe serum concentration of Taurocholic Acid can be increased when it is combined with Sunitinib.Experimental
TavaboroleThe metabolism of Sunitinib can be decreased when combined with Tavaborole.Approved
Technetium Tc-99m sestamibiThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Sunitinib.Approved
TelaprevirThe metabolism of Sunitinib can be decreased when combined with Telaprevir.Approved
TelavancinSunitinib may increase the QTc-prolonging activities of Telavancin.Approved
TelithromycinThe metabolism of Sunitinib can be decreased when combined with Telithromycin.Approved
TemafloxacinTemafloxacin may increase the hypoglycemic activities of Sunitinib.Withdrawn
TemsirolimusThe risk or severity of adverse effects can be increased when Temsirolimus is combined with Sunitinib.Approved
TerbinafineThe metabolism of Sunitinib can be decreased when combined with Terbinafine.Approved, Investigational, Vet Approved
TerconazoleThe metabolism of Sunitinib can be decreased when combined with Terconazole.Approved
TestosteroneTestosterone may increase the hypoglycemic activities of Sunitinib.Approved, Investigational
TetrabenazineSunitinib may increase the QTc-prolonging activities of Tetrabenazine.Approved
TG4010The risk or severity of adverse effects can be increased when Sunitinib is combined with TG4010.Investigational
ThiazolidinedioneThiazolidinedione may increase the hypoglycemic activities of Sunitinib.Investigational
ThioridazineSunitinib may increase the QTc-prolonging activities of Thioridazine.Approved
ThymolThe metabolism of Sunitinib can be decreased when combined with Thymol.Approved
TicagrelorThe serum concentration of Ticagrelor can be increased when it is combined with Sunitinib.Approved
TiclopidineThe metabolism of Sunitinib can be decreased when combined with Ticlopidine.Approved
TimololThe serum concentration of Timolol can be increased when it is combined with Sunitinib.Approved
TioconazoleThe metabolism of Sunitinib can be decreased when combined with Tioconazole.Approved
TocilizumabThe serum concentration of Sunitinib can be decreased when it is combined with Tocilizumab.Approved
TofacitinibSunitinib may increase the immunosuppressive activities of Tofacitinib.Approved, Investigational
TolazamideTolazamide may increase the hypoglycemic activities of Sunitinib.Approved
TolbutamideTolbutamide may increase the hypoglycemic activities of Sunitinib.Approved
TolnaftateThe metabolism of Sunitinib can be decreased when combined with Tolnaftate.Approved, Vet Approved
ToloxatoneToloxatone may increase the hypoglycemic activities of Sunitinib.Approved
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Sunitinib.Approved
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Sunitinib.Approved, Investigational
ToremifeneSunitinib may increase the QTc-prolonging activities of Toremifene.Approved, Investigational
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypoglycemic activities of Sunitinib.Experimental
TranylcypromineTranylcypromine may increase the hypoglycemic activities of Sunitinib.Approved
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Sunitinib.Approved, Investigational
Trastuzumab emtansineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Sunitinib.Approved
TrimetrexateThe metabolism of Sunitinib can be decreased when combined with Trimetrexate.Approved, Investigational
TroglitazoneTroglitazone may increase the hypoglycemic activities of Sunitinib.Withdrawn
TrovafloxacinTrovafloxacin may increase the hypoglycemic activities of Sunitinib.Approved, Withdrawn
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Sunitinib.Approved
UmeclidiniumThe serum concentration of Umeclidinium can be increased when it is combined with Sunitinib.Approved
VandetanibSunitinib may increase the QTc-prolonging activities of Vandetanib.Approved
VecuroniumThe serum concentration of Vecuronium can be increased when it is combined with Sunitinib.Approved
VemurafenibSunitinib may increase the QTc-prolonging activities of Vemurafenib.Approved
VenetoclaxThe serum concentration of Venetoclax can be increased when it is combined with Sunitinib.Approved
VenlafaxineThe metabolism of Sunitinib can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Sunitinib can be decreased when combined with Verapamil.Approved
VildagliptinVildagliptin may increase the hypoglycemic activities of Sunitinib.Approved, Investigational
VinblastineThe serum concentration of Vinblastine can be increased when it is combined with Sunitinib.Approved
VincristineThe serum concentration of Vincristine can be increased when it is combined with Sunitinib.Approved, Investigational
VismodegibThe serum concentration of Vismodegib can be increased when it is combined with Sunitinib.Approved
VogliboseVoglibose may increase the hypoglycemic activities of Sunitinib.Approved, Investigational
VoriconazoleThe metabolism of Sunitinib can be decreased when combined with Voriconazole.Approved, Investigational
ZidovudineThe serum concentration of Zidovudine can be increased when it is combined with Sunitinib.Approved
ZimelidineZimelidine may increase the hypoglycemic activities of Sunitinib.Withdrawn
ZiprasidoneSunitinib may increase the QTc-prolonging activities of Ziprasidone.Approved
ZuclopenthixolSunitinib may increase the QTc-prolonging activities of Zuclopenthixol.Approved, Investigational
Food InteractionsNot Available
References
Synthesis Reference

Ettore BIGATTI, Augusto CANAVESI, Peter Lindsay MACDONALD, Francesca Scarpitta, “PROCESSES FOR PREPARING SUNITINIB AND SALTS THEREOF.” U.S. Patent US20090247767, issued October 01, 2009.

US20090247767
General References
  1. Motzer RJ, Hutson TE, Tomczak P, Michaelson MD, Bukowski RM, Rixe O, Oudard S, Negrier S, Szczylik C, Kim ST, Chen I, Bycott PW, Baum CM, Figlin RA: Sunitinib versus interferon alfa in metastatic renal-cell carcinoma. N Engl J Med. 2007 Jan 11;356(2):115-24. [PubMed:17215529 ]
  2. Demetri GD, van Oosterom AT, Garrett CR, Blackstein ME, Shah MH, Verweij J, McArthur G, Judson IR, Heinrich MC, Morgan JA, Desai J, Fletcher CD, George S, Bello CL, Huang X, Baum CM, Casali PG: Efficacy and safety of sunitinib in patients with advanced gastrointestinal stromal tumour after failure of imatinib: a randomised controlled trial. Lancet. 2006 Oct 14;368(9544):1329-38. [PubMed:17046465 ]
External Links
ATC CodesL01XE04
AHFS Codes
  • 92:00.00
PDB EntriesNot Available
FDA labelDownload (159 KB)
MSDSDownload (98.3 KB)
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9938
Blood Brain Barrier+0.7993
Caco-2 permeable-0.5948
P-glycoprotein substrateSubstrate0.8648
P-glycoprotein inhibitor IInhibitor0.6809
P-glycoprotein inhibitor IINon-inhibitor0.5466
Renal organic cation transporterNon-inhibitor0.7385
CYP450 2C9 substrateNon-substrate0.8727
CYP450 2D6 substrateNon-substrate0.7716
CYP450 3A4 substrateSubstrate0.641
CYP450 1A2 substrateNon-inhibitor0.5626
CYP450 2C9 inhibitorNon-inhibitor0.6437
CYP450 2D6 inhibitorNon-inhibitor0.6846
CYP450 2C19 inhibitorNon-inhibitor0.6261
CYP450 3A4 inhibitorNon-inhibitor0.5991
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.7032
Ames testNon AMES toxic0.5699
CarcinogenicityNon-carcinogens0.784
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.6794 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8597
hERG inhibition (predictor II)Inhibitor0.8398
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
CapsuleOral12.5 mg/1
CapsuleOral12.5 mg
CapsuleOral25 mg
CapsuleOral25 mg/1
CapsuleOral37.5 mg
CapsuleOral37.5 mg/1
CapsuleOral50 mg/1
CapsuleOral50 mg
Prices
Unit descriptionCostUnit
Sutent 50 mg capsule333.39USD capsule
Sutent 25 mg capsule187.28USD capsule
Sutent 12.5 mg capsule93.64USD capsule
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Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2395461 No2010-05-252020-12-22Canada
CA2399358 No2006-03-212021-02-15Canada
US6573293 No2001-02-152021-02-15Us
US7125905 No2001-02-152021-02-15Us
US7211600 No2000-12-222020-12-22Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubility>25 mg/mL over pH of 1.2 to 6.8FDA label
logP5.2 FDA label
pKa8.95 FDA label
Predicted Properties
PropertyValueSource
Water Solubility0.0308 mg/mLALOGPS
logP3.24ALOGPS
logP2.93ChemAxon
logS-4.1ALOGPS
pKa (Strongest Acidic)11.46ChemAxon
pKa (Strongest Basic)9.04ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area77.23 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity116.27 m3·mol-1ChemAxon
Polarizability44.32 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 indolines. These are compounds containing an indole moiety, which consists of pyrrolidine ring fused to benzene to form 2,3-dihydroindole.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassIndoles and derivatives
Sub ClassIndolines
Direct ParentIndolines
Alternative Parents
Substituents
  • Dihydroindole
  • Pyrrole-3-carboxylic acid or derivatives
  • Pyrrole-3-carboxamide
  • Fluorobenzene
  • Benzenoid
  • Substituted pyrrole
  • Aryl halide
  • Aryl fluoride
  • Heteroaromatic compound
  • Vinylogous amide
  • Pyrrole
  • Tertiary aliphatic amine
  • Tertiary amine
  • Secondary carboxylic acid amide
  • Lactam
  • Carboxamide group
  • Azacycle
  • Carboxylic acid derivative
  • Carboxylic acid amide
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organofluoride
  • Organohalogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
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. Mendel DB, Laird AD, Xin X, Louie SG, Christensen JG, Li G, Schreck RE, Abrams TJ, Ngai TJ, Lee LB, Murray LJ, Carver J, Chan E, Moss KG, Haznedar JO, Sukbuntherng J, Blake RA, Sun L, Tang C, Miller T, Shirazian S, McMahon G, Cherrington JM: In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship. Clin Cancer Res. 2003 Jan;9(1):327-37. [PubMed:12538485 ]
  2. Abrams TJ, Lee LB, Murray LJ, Pryer NK, Cherrington JM: SU11248 inhibits KIT and platelet-derived growth factor receptor beta in preclinical models of human small cell lung cancer. Mol Cancer Ther. 2003 May;2(5):471-8. [PubMed:12748309 ]
  3. Baratte S, Sarati S, Frigerio E, James CA, Ye C, Zhang Q: Quantitation of SU1 1248, an oral multi-target tyrosine kinase inhibitor, and its metabolite in monkey tissues by liquid chromatograph with tandem mass spectrometry following semi-automated liquid-liquid extraction. J Chromatogr A. 2004 Jan 23;1024(1-2):87-94. [PubMed:14753710 ]
  4. Pietras K, Hanahan D: A multitargeted, metronomic, and maximum-tolerated dose "chemo-switch" regimen is antiangiogenic, producing objective responses and survival benefit in a mouse model of cancer. J Clin Oncol. 2005 Feb 10;23(5):939-52. Epub 2004 Nov 22. [PubMed:15557593 ]
  5. 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 ]
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. O'Farrell AM, Foran JM, Fiedler W, Serve H, Paquette RL, Cooper MA, Yuen HA, Louie SG, Kim H, Nicholas S, Heinrich MC, Berdel WE, Bello C, Jacobs M, Scigalla P, Manning WC, Kelsey S, Cherrington JM: An innovative phase I clinical study demonstrates inhibition of FLT3 phosphorylation by SU11248 in acute myeloid leukemia patients. Clin Cancer Res. 2003 Nov 15;9(15):5465-76. [PubMed:14654525 ]
  2. Roskoski R Jr: Sunitinib: a VEGF and PDGF receptor protein kinase and angiogenesis inhibitor. Biochem Biophys Res Commun. 2007 May 4;356(2):323-8. Epub 2007 Mar 7. [PubMed:17367763 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
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. Abrams TJ, Lee LB, Murray LJ, Pryer NK, Cherrington JM: SU11248 inhibits KIT and platelet-derived growth factor receptor beta in preclinical models of human small cell lung cancer. Mol Cancer Ther. 2003 May;2(5):471-8. [PubMed:12748309 ]
  2. Schueneman AJ, Himmelfarb E, Geng L, Tan J, Donnelly E, Mendel D, McMahon G, Hallahan DE: SU11248 maintenance therapy prevents tumor regrowth after fractionated irradiation of murine tumor models. Cancer Res. 2003 Jul 15;63(14):4009-16. [PubMed:12873999 ]
  3. Joensuu H: Second line therapies for the treatment of gastrointestinal stromal tumor. Curr Opin Oncol. 2007 Jul;19(4):353-8. [PubMed:17545799 ]
  4. Baratte S, Sarati S, Frigerio E, James CA, Ye C, Zhang Q: Quantitation of SU1 1248, an oral multi-target tyrosine kinase inhibitor, and its metabolite in monkey tissues by liquid chromatograph with tandem mass spectrometry following semi-automated liquid-liquid extraction. J Chromatogr A. 2004 Jan 23;1024(1-2):87-94. [PubMed:14753710 ]
  5. Roskoski R Jr: Sunitinib: a VEGF and PDGF receptor protein kinase and angiogenesis inhibitor. Biochem Biophys Res Commun. 2007 May 4;356(2):323-8. Epub 2007 Mar 7. [PubMed:17367763 ]
  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:
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. Mendel DB, Laird AD, Xin X, Louie SG, Christensen JG, Li G, Schreck RE, Abrams TJ, Ngai TJ, Lee LB, Murray LJ, Carver J, Chan E, Moss KG, Haznedar JO, Sukbuntherng J, Blake RA, Sun L, Tang C, Miller T, Shirazian S, McMahon G, Cherrington JM: In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship. Clin Cancer Res. 2003 Jan;9(1):327-37. [PubMed:12538485 ]
  2. Schueneman AJ, Himmelfarb E, Geng L, Tan J, Donnelly E, Mendel D, McMahon G, Hallahan DE: SU11248 maintenance therapy prevents tumor regrowth after fractionated irradiation of murine tumor models. Cancer Res. 2003 Jul 15;63(14):4009-16. [PubMed:12873999 ]
  3. Baratte S, Sarati S, Frigerio E, James CA, Ye C, Zhang Q: Quantitation of SU1 1248, an oral multi-target tyrosine kinase inhibitor, and its metabolite in monkey tissues by liquid chromatograph with tandem mass spectrometry following semi-automated liquid-liquid extraction. J Chromatogr A. 2004 Jan 23;1024(1-2):87-94. [PubMed:14753710 ]
  4. 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 ]
  5. Amino N, Ideyama Y, Yamano M, Kuromitsu S, Tajinda K, Samizu K, Hisamichi H, Matsuhisa A, Shirasuna K, Kudoh M, Shibasaki M: YM-359445, an orally bioavailable vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor, has highly potent antitumor activity against established tumors. Clin Cancer Res. 2006 Mar 1;12(5):1630-8. [PubMed:16533791 ]
  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:
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. Roskoski R Jr: Sunitinib: a VEGF and PDGF receptor protein kinase and angiogenesis inhibitor. Biochem Biophys Res Commun. 2007 May 4;356(2):323-8. Epub 2007 Mar 7. [PubMed:17367763 ]
  2. Deprimo SE, Bello CL, Smeraglia J, Baum CM, Spinella D, Rini BI, Michaelson MD, Motzer RJ: Circulating protein biomarkers of pharmacodynamic activity of sunitinib in patients with metastatic renal cell carcinoma: modulation of VEGF and VEGF-related proteins. J Transl Med. 2007 Jul 2;5:32. [PubMed:17605814 ]
  3. Katoh Y, Katoh M: Comparative integromics on VEGF family members. Int J Oncol. 2006 Jun;28(6):1585-9. [PubMed:16685460 ]
  4. 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 ]
  5. Ahmed SI, Thomas AL, Steward WP: Vascular endothelial growth factor (VEGF) inhibition by small molecules. J Chemother. 2004 Nov;16 Suppl 4:59-63. [PubMed:15688612 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
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. O'Farrell AM, Abrams TJ, Yuen HA, Ngai TJ, Louie SG, Yee KW, Wong LM, Hong W, Lee LB, Town A, Smolich BD, Manning WC, Murray LJ, Heinrich MC, Cherrington JM: SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo. Blood. 2003 May 1;101(9):3597-605. Epub 2003 Jan 16. [PubMed:12531805 ]
  2. O'Farrell AM, Foran JM, Fiedler W, Serve H, Paquette RL, Cooper MA, Yuen HA, Louie SG, Kim H, Nicholas S, Heinrich MC, Berdel WE, Bello C, Jacobs M, Scigalla P, Manning WC, Kelsey S, Cherrington JM: An innovative phase I clinical study demonstrates inhibition of FLT3 phosphorylation by SU11248 in acute myeloid leukemia patients. Clin Cancer Res. 2003 Nov 15;9(15):5465-76. [PubMed:14654525 ]
  3. Baratte S, Sarati S, Frigerio E, James CA, Ye C, Zhang Q: Quantitation of SU1 1248, an oral multi-target tyrosine kinase inhibitor, and its metabolite in monkey tissues by liquid chromatograph with tandem mass spectrometry following semi-automated liquid-liquid extraction. J Chromatogr A. 2004 Jan 23;1024(1-2):87-94. [PubMed:14753710 ]
  4. Schmidt-Arras D, Schwable J, Bohmer FD, Serve H: Flt3 receptor tyrosine kinase as a drug target in leukemia. Curr Pharm Des. 2004;10(16):1867-83. [PubMed:15180525 ]
  5. Yee KW, Schittenhelm M, O'Farrell AM, Town AR, McGreevey L, Bainbridge T, Cherrington JM, Heinrich MC: Synergistic effect of SU11248 with cytarabine or daunorubicin on FLT3 ITD-positive leukemic cells. Blood. 2004 Dec 15;104(13):4202-9. Epub 2004 Aug 10. [PubMed:15304385 ]
  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 homodimerization activity
Specific Function:
Tyrosine-protein kinase that acts as cell-surface receptor for CSF1 and IL34 and plays an essential role in the regulation of survival, proliferation and differentiation of hematopoietic precursor cells, especially mononuclear phagocytes, such as macrophages and monocytes. Promotes the release of proinflammatory chemokines in response to IL34 and CSF1, and thereby plays an important role in inn...
Gene Name:
CSF1R
Uniprot ID:
P07333
Molecular Weight:
107982.955 Da
References
  1. Guo J, Marcotte PA, McCall JO, Dai Y, Pease LJ, Michaelides MR, Davidsen SK, Glaser KB: Inhibition of phosphorylation of the colony-stimulating factor-1 receptor (c-Fms) tyrosine kinase in transfected cells by ABT-869 and other tyrosine kinase inhibitors. Mol Cancer Ther. 2006 Apr;5(4):1007-13. [PubMed:16648572 ]
  2. Roskoski R Jr: Sunitinib: a VEGF and PDGF receptor protein kinase and angiogenesis inhibitor. Biochem Biophys Res Commun. 2007 May 4;356(2):323-8. Epub 2007 Mar 7. [PubMed:17367763 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Vascular endothelial growth factor-activated receptor activity
Specific Function:
Tyrosine-protein kinase that acts as a cell-surface receptor for PDGFA, PDGFB and PDGFC and plays an essential role in the regulation of embryonic development, cell proliferation, survival and chemotaxis. Depending on the context, promotes or inhibits cell proliferation and cell migration. Plays an important role in the differentiation of bone marrow-derived mesenchymal stem cells. Required for...
Gene Name:
PDGFRA
Uniprot ID:
P16234
Molecular Weight:
122668.46 Da
References
  1. Prenen H, Cools J, Mentens N, Folens C, Sciot R, Schoffski P, Van Oosterom A, Marynen P, Debiec-Rychter M: Efficacy of the kinase inhibitor SU11248 against gastrointestinal stromal tumor mutants refractory to imatinib mesylate. Clin Cancer Res. 2006 Apr 15;12(8):2622-7. [PubMed:16638875 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. 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]

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
inhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. 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. Shukla S, Robey RW, Bates SE, Ambudkar SV: Sunitinib (Sutent, SU11248), a small-molecule receptor tyrosine kinase inhibitor, blocks function of the ATP-binding cassette (ABC) transporters P-glycoprotein (ABCB1) and ABCG2. Drug Metab Dispos. 2009 Feb;37(2):359-65. doi: 10.1124/dmd.108.024612. Epub 2008 Oct 29. [PubMed:18971320 ]
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
inhibitor
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. Dai CL, Liang YJ, Wang YS, Tiwari AK, Yan YY, Wang F, Chen ZS, Tong XZ, Fu LW: Sensitization of ABCG2-overexpressing cells to conventional chemotherapeutic agent by sunitinib was associated with inhibiting the function of ABCG2. Cancer Lett. 2009 Jun 28;279(1):74-83. doi: 10.1016/j.canlet.2009.01.027. Epub 2009 Feb 18. [PubMed:19232821 ]
  3. Shukla S, Robey RW, Bates SE, Ambudkar SV: Sunitinib (Sutent, SU11248), a small-molecule receptor tyrosine kinase inhibitor, blocks function of the ATP-binding cassette (ABC) transporters P-glycoprotein (ABCB1) and ABCG2. Drug Metab Dispos. 2009 Feb;37(2):359-65. doi: 10.1124/dmd.108.024612. Epub 2008 Oct 29. [PubMed:18971320 ]
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Drug created on May 16, 2007 14:11 / Updated on December 07, 2016 02:37