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Identification
NameVandetanib
Accession NumberDB05294
TypeSmall Molecule
GroupsApproved
DescriptionVandetanib is an oral once-daily kinase inhibitor of tumour angiogenesis and tumour cell proliferation with the potential for use in a broad range of tumour types. On April 6 2011, vandetanib was approved by the FDA to treat nonresectable, locally advanced, or metastatic medullary thyroid cancer in adult patients.
Structure
Thumb
Synonyms
4-BROMO-2-fluoro-N-[(4e)-6-methoxy-7-[(1-methylpiperidin-4-yl)methoxy]quinazolin-4(1H)-ylidene]aniline
4-quinazolinamine, N-(4-bromo-2-fluorophenyl)-6-methoxy-7-[(1-methyl-4-piperidinyl)methoxy]-
N-(4-Bromo-2-fluorophenyl)-6-methoxy-7-[(1-methyl-4-piperidinyl)methoxy]-4-quinazolinamine
N-(4-bromo-2-fluorophenyl)-6-methoxy-7-[(1-methylpiperidin-4-yl)methoxy]quinazolin-4-amine
Zactima
ZD 6474
ZD6474
External Identifiers
  • ZD-6474
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
CaprelsaFilm-coated tablet300 mgOral useAstra Zeneca Ab2012-02-17Not applicableEu
Caprelsatablet100 mgoralGenzyme Canada A Division Of Sanofi Aventis Canada Inc2012-02-23Not applicableCanada
Caprelsatablet100 mg/1oralAstra Zeneca Pharmaceuticals Lp2011-07-25Not applicableUs
Caprelsatablet300 mgoralGenzyme Canada A Division Of Sanofi Aventis Canada Inc2012-02-23Not applicableCanada
CaprelsaFilm-coated tablet100 mgOral useAstra Zeneca Ab2012-02-17Not applicableEu
Caprelsatablet300 mg/1oralAstra Zeneca Pharmaceuticals Lp2011-07-25Not applicableUs
Vandetanibtablet100 mg/1oralAstra Zeneca Pharmaceuticals Lp2011-04-21Not applicableUs
Vandetanibtablet300 mg/1oralAstra Zeneca Pharmaceuticals Lp2011-04-21Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
Zactima AstraZeneca
Zictifa AstraZeneca
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIYO460OQ37K
CAS number443913-73-3
WeightAverage: 475.354
Monoisotopic: 474.106666884
Chemical FormulaC22H24BrFN4O2
InChI KeyInChIKey=UHTHHESEBZOYNR-UHFFFAOYSA-N
InChI
InChI=1S/C22H24BrFN4O2/c1-28-7-5-14(6-8-28)12-30-21-11-19-16(10-20(21)29-2)22(26-13-25-19)27-18-4-3-15(23)9-17(18)24/h3-4,9-11,13-14H,5-8,12H2,1-2H3,(H,25,26,27)
IUPAC Name
N-(4-bromo-2-fluorophenyl)-6-methoxy-7-[(1-methylpiperidin-4-yl)methoxy]quinazolin-4-amine
SMILES
COC1=C(OCC2CCN(C)CC2)C=C2N=CN=C(NC3=C(F)C=C(Br)C=C3)C2=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as quinazolinamines. These are heterocyclic aromatic compounds containing a quianazoline moiety substituted by one or more amine groups.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassNaphthyridines
Sub ClassQuinazolines
Direct ParentQuinazolinamines
Alternative Parents
Substituents
  • Quinazolinamine
  • Anisole
  • Halobenzene
  • Fluorobenzene
  • Bromobenzene
  • Aminopyrimidine
  • Alkyl aryl ether
  • Imidolactam
  • Benzenoid
  • Pyrimidine
  • Piperidine
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl fluoride
  • Aryl bromide
  • Heteroaromatic compound
  • Tertiary aliphatic amine
  • Tertiary amine
  • Azacycle
  • Secondary amine
  • Ether
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organofluoride
  • Organobromide
  • Organohalogen compound
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationVandetanib is currently approved as an alternative to local therapies for both unresectable and disseminated disease. Because Vandetanib can prolong the Q-T interval, it is contraindicated for use in patients with serious cardiac complications such as congenital long QT syndrome and uncompensated heart failure.
PharmacodynamicsMean IC50 of approximately 2.1 μg/mL.
Mechanism of actionZD-6474 is a potent and selective inhibitor of VEGFR (vascular endothelial growth factor receptor), EGFR (epidermal growth factor receptor) and RET (REarranged during Transfection) tyrosine kinases. VEGFR- and EGFR-dependent signalling are both clinically validated pathways in cancer, including non-small-cell lung cancer (NSCLC). RET activity is important in some types of thyroid cancer, and early data with vandetanib in medullary thyroid cancer has led to orphan-drug designation by the regulatory authorities in the USA and EU.
Related Articles
AbsorptionSlow- peak plasma concentrations reached at a median 6 hours. On multiple dosing, Vandetanib accumulates about 8 fold with steady state reached after around 3 months.
Volume of distribution

Vd of about 7450 L.

Protein bindingProtein binding of about 90%.
Metabolism

Unchanged vandentanib and metabolites vandetanib N-oxide and N-desmethyl vandetanib were detected in plasma, urine and feces. N-desmethyl-vandetanib is primarily produced by CYP3A4, and vandetanib-N-oxide is primarily produced by flavin–containing monooxygenase enzymes FMO1 and FMO3.

SubstrateEnzymesProduct
Vandetanib
Not Available
N-desmethyl vandetanibDetails
Route of eliminationAbout 69% was recovered following 21 days after a single dose of vandentanib. 44% was found in feces and 25% in urine.
Half lifeMedian half life of 19 days.
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9961
Blood Brain Barrier+0.9596
Caco-2 permeable+0.611
P-glycoprotein substrateSubstrate0.7412
P-glycoprotein inhibitor IInhibitor0.7327
P-glycoprotein inhibitor IIInhibitor0.9501
Renal organic cation transporterInhibitor0.6556
CYP450 2C9 substrateNon-substrate0.8419
CYP450 2D6 substrateNon-substrate0.5827
CYP450 3A4 substrateSubstrate0.6006
CYP450 1A2 substrateInhibitor0.7333
CYP450 2C9 inhibitorNon-inhibitor0.7749
CYP450 2D6 inhibitorInhibitor0.5867
CYP450 2C19 inhibitorInhibitor0.5077
CYP450 3A4 inhibitorInhibitor0.5288
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.8009
Ames testAMES toxic0.5693
CarcinogenicityNon-carcinogens0.9322
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.5482 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.5
hERG inhibition (predictor II)Inhibitor0.8342
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Film-coated tabletOral use100 mg
Film-coated tabletOral use300 mg
Tabletoral100 mg
Tabletoral300 mg
Tabletoral100 mg/1
Tabletoral300 mg/1
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US7173038 No2001-08-142021-08-14Us
US8067427 No2008-08-082028-08-08Us
US8642608 No2002-02-062022-02-06Us
USRE42353 No1997-09-232017-09-23Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubility0.008 mg/mL at 25°C (77°F )FDA Label
Predicted Properties
PropertyValueSource
Water Solubility0.0102 mg/mLALOGPS
logP5.01ALOGPS
logP4.54ChemAxon
logS-4.7ALOGPS
pKa (Strongest Acidic)13.8ChemAxon
pKa (Strongest Basic)9.13ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area59.51 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity118.63 m3·mol-1ChemAxon
Polarizability47.1 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (103 KB)
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
References
Synthesis ReferenceNot Available
General References
  1. Bates D: ZD-6474. AstraZeneca. Curr Opin Investig Drugs. 2003 Dec;4(12):1468-72. [PubMed:14763134 ]
  2. Ton GN, Banaszynski ME, Kolesar JM: Vandetanib: a novel targeted therapy for the treatment of metastatic or locally advanced medullary thyroid cancer. Am J Health Syst Pharm. 2013 May 15;70(10):849-55. doi: 10.2146/ajhp120253. [PubMed:23640345 ]
  3. Andriamanana I, Gana I, Duretz B, Hulin A: Simultaneous analysis of anticancer agents bortezomib, imatinib, nilotinib, dasatinib, erlotinib, lapatinib, sorafenib, sunitinib and vandetanib in human plasma using LC/MS/MS. J Chromatogr B Analyt Technol Biomed Life Sci. 2013 May 1;926:83-91. doi: 10.1016/j.jchromb.2013.01.037. Epub 2013 Mar 16. [PubMed:23562906 ]
External Links
ATC CodesL01XE12
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (220 KB)
MSDSDownload (220 KB)
Interactions
Drug Interactions
Drug
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Vandetanib.
AlfuzosinAlfuzosin may increase the QTc-prolonging activities of Vandetanib.
AmantadineAmantadine may increase the QTc-prolonging activities of Vandetanib.
AmiodaroneAmiodarone may increase the QTc-prolonging activities of Vandetanib.
AmitriptylineAmitriptyline may increase the QTc-prolonging activities of Vandetanib.
AmoxapineAmoxapine may increase the QTc-prolonging activities of Vandetanib.
AnagrelideAnagrelide may increase the QTc-prolonging activities of Vandetanib.
ApomorphineApomorphine may increase the QTc-prolonging activities of Vandetanib.
AprepitantThe serum concentration of Vandetanib can be increased when it is combined with Aprepitant.
ArformoterolArformoterol may increase the QTc-prolonging activities of Vandetanib.
AripiprazoleAripiprazole may increase the QTc-prolonging activities of Vandetanib.
Arsenic trioxideArsenic trioxide may increase the QTc-prolonging activities of Vandetanib.
ArtemetherVandetanib may increase the QTc-prolonging activities of Artemether.
AsenapineVandetanib may increase the QTc-prolonging activities of Asenapine.
AtazanavirThe metabolism of Vandetanib can be decreased when combined with Atazanavir.
AtomoxetineThe metabolism of Vandetanib can be decreased when combined with Atomoxetine.
AzithromycinAzithromycin may increase the QTc-prolonging activities of Vandetanib.
BedaquilineBedaquiline may increase the QTc-prolonging activities of Vandetanib.
BevacizumabBevacizumab may increase the cardiotoxic activities of Vandetanib.
BexaroteneThe serum concentration of Vandetanib can be decreased when it is combined with Bexarotene.
BoceprevirThe metabolism of Vandetanib can be decreased when combined with Boceprevir.
BortezomibThe metabolism of Vandetanib can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Vandetanib can be decreased when it is combined with Bosentan.
BuserelinBuserelin may increase the QTc-prolonging activities of Vandetanib.
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Vandetanib.
CarbamazepineThe serum concentration of Vandetanib can be decreased when it is combined with Carbamazepine.
CeritinibCeritinib may increase the QTc-prolonging activities of Vandetanib.
ChloroquineChloroquine may increase the QTc-prolonging activities of Vandetanib.
ChlorpromazineChlorpromazine may increase the QTc-prolonging activities of Vandetanib.
CiprofloxacinCiprofloxacin may increase the QTc-prolonging activities of Vandetanib.
CisaprideCisapride may increase the QTc-prolonging activities of Vandetanib.
CitalopramCitalopram may increase the QTc-prolonging activities of Vandetanib.
ClarithromycinClarithromycin may increase the QTc-prolonging activities of Vandetanib.
ClemastineThe metabolism of Vandetanib can be decreased when combined with Clemastine.
ClomipramineClomipramine may increase the QTc-prolonging activities of Vandetanib.
ClotrimazoleThe metabolism of Vandetanib can be decreased when combined with Clotrimazole.
ClozapineClozapine may increase the QTc-prolonging activities of Vandetanib.
CobicistatThe metabolism of Vandetanib can be decreased when combined with Cobicistat.
ConivaptanThe serum concentration of Vandetanib can be increased when it is combined with Conivaptan.
CrizotinibCrizotinib may increase the QTc-prolonging activities of Vandetanib.
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Vandetanib.
CyclosporineThe metabolism of Vandetanib can be decreased when combined with Cyclosporine.
DabrafenibThe serum concentration of Vandetanib can be decreased when it is combined with Dabrafenib.
DarunavirThe metabolism of Vandetanib can be decreased when combined with Darunavir.
DasatinibThe serum concentration of Vandetanib can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Vandetanib can be decreased when it is combined with Deferasirox.
DegarelixDegarelix may increase the QTc-prolonging activities of Vandetanib.
DelavirdineThe metabolism of Vandetanib can be decreased when combined with Delavirdine.
DesfluraneDesflurane may increase the QTc-prolonging activities of Vandetanib.
DesipramineDesipramine may increase the QTc-prolonging activities of Vandetanib.
DeslanosideDeslanoside may decrease the cardiotoxic activities of Vandetanib.
DexamethasoneThe serum concentration of Vandetanib can be decreased when it is combined with Dexamethasone.
DigitoxinDigitoxin may decrease the cardiotoxic activities of Vandetanib.
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Vandetanib.
DigoxinDigoxin may decrease the cardiotoxic activities of Vandetanib.
DihydroergotamineThe metabolism of Vandetanib can be decreased when combined with Dihydroergotamine.
DiltiazemThe metabolism of Vandetanib can be decreased when combined with Diltiazem.
DiphenhydramineDiphenhydramine may increase the QTc-prolonging activities of Vandetanib.
DisopyramideDisopyramide may increase the QTc-prolonging activities of Vandetanib.
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Vandetanib.
DofetilideDofetilide may increase the QTc-prolonging activities of Vandetanib.
DolasetronDolasetron may increase the QTc-prolonging activities of Vandetanib.
DomperidoneDomperidone may increase the QTc-prolonging activities of Vandetanib.
DoxepinDoxepin may increase the QTc-prolonging activities of Vandetanib.
DoxycyclineThe metabolism of Vandetanib can be decreased when combined with Doxycycline.
DronedaroneDronedarone may increase the QTc-prolonging activities of Vandetanib.
DroperidolDroperidol may increase the QTc-prolonging activities of Vandetanib.
EfavirenzThe serum concentration of Vandetanib can be decreased when it is combined with Efavirenz.
EliglustatVandetanib may increase the QTc-prolonging activities of Eliglustat.
EnzalutamideThe serum concentration of Vandetanib can be decreased when it is combined with Enzalutamide.
EribulinEribulin may increase the QTc-prolonging activities of Vandetanib.
ErythromycinErythromycin may increase the QTc-prolonging activities of Vandetanib.
EscitalopramEscitalopram may increase the QTc-prolonging activities of Vandetanib.
Eslicarbazepine acetateThe serum concentration of Vandetanib can be decreased when it is combined with Eslicarbazepine acetate.
EtravirineThe serum concentration of Vandetanib can be decreased when it is combined with Etravirine.
EzogabineEzogabine may increase the QTc-prolonging activities of Vandetanib.
FamotidineFamotidine may increase the QTc-prolonging activities of Vandetanib.
FelbamateFelbamate may increase the QTc-prolonging activities of Vandetanib.
FingolimodFingolimod may increase the QTc-prolonging activities of Vandetanib.
FlecainideFlecainide may increase the QTc-prolonging activities of Vandetanib.
FluconazoleThe metabolism of Vandetanib can be decreased when combined with Fluconazole.
FluoxetineFluoxetine may increase the QTc-prolonging activities of Vandetanib.
FlupentixolFlupentixol may increase the QTc-prolonging activities of Vandetanib.
FluvoxamineThe metabolism of Vandetanib can be decreased when combined with Fluvoxamine.
FormoterolFormoterol may increase the QTc-prolonging activities of Vandetanib.
FosamprenavirThe metabolism of Vandetanib can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Vandetanib can be increased when it is combined with Fosaprepitant.
FoscarnetFoscarnet may increase the QTc-prolonging activities of Vandetanib.
FosphenytoinThe serum concentration of Vandetanib can be decreased when it is combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Vandetanib can be increased when it is combined with Fusidic Acid.
Gadobenic acidGadobenic acid may increase the QTc-prolonging activities of Vandetanib.
GalantamineGalantamine may increase the QTc-prolonging activities of Vandetanib.
GemifloxacinGemifloxacin may increase the QTc-prolonging activities of Vandetanib.
GoserelinGoserelin may increase the QTc-prolonging activities of Vandetanib.
GranisetronGranisetron may increase the QTc-prolonging activities of Vandetanib.
HaloperidolHaloperidol may increase the QTc-prolonging activities of Vandetanib.
HistrelinHistrelin may increase the QTc-prolonging activities of Vandetanib.
HydroxyzineHydroxyzine may increase the QTc-prolonging activities of Vandetanib.
IbandronateIbandronate may increase the QTc-prolonging activities of Vandetanib.
IbutilideIbutilide may increase the QTc-prolonging activities of Vandetanib.
IdelalisibThe serum concentration of Vandetanib can be increased when it is combined with Idelalisib.
IloperidoneIloperidone may increase the QTc-prolonging activities of Vandetanib.
ImatinibThe metabolism of Vandetanib can be decreased when combined with Imatinib.
ImipramineImipramine may increase the QTc-prolonging activities of Vandetanib.
IndacaterolIndacaterol may increase the QTc-prolonging activities of Vandetanib.
IndapamideIndapamide may increase the QTc-prolonging activities of Vandetanib.
IndinavirThe metabolism of Vandetanib can be decreased when combined with Indinavir.
IsavuconazoniumThe metabolism of Vandetanib can be decreased when combined with Isavuconazonium.
IsofluraneIsoflurane may increase the QTc-prolonging activities of Vandetanib.
IsradipineThe metabolism of Vandetanib can be decreased when combined with Isradipine.
ItraconazoleThe metabolism of Vandetanib can be decreased when combined with Itraconazole.
IvabradineIvabradine may increase the QTc-prolonging activities of Vandetanib.
IvacaftorThe serum concentration of Vandetanib can be increased when it is combined with Ivacaftor.
KetoconazoleThe metabolism of Vandetanib can be decreased when combined with Ketoconazole.
LapatinibLapatinib may increase the QTc-prolonging activities of Vandetanib.
LenvatinibLenvatinib may increase the QTc-prolonging activities of Vandetanib.
LeuprolideLeuprolide may increase the QTc-prolonging activities of Vandetanib.
LevofloxacinLevofloxacin may increase the QTc-prolonging activities of Vandetanib.
LithiumLithium may increase the QTc-prolonging activities of Vandetanib.
LopinavirLopinavir may increase the QTc-prolonging activities of Vandetanib.
LovastatinThe metabolism of Vandetanib can be decreased when combined with Lovastatin.
LuliconazoleThe serum concentration of Vandetanib can be increased when it is combined with Luliconazole.
LumefantrineVandetanib may increase the QTc-prolonging activities of Lumefantrine.
MaprotilineMaprotiline may increase the QTc-prolonging activities of Vandetanib.
MefloquineMefloquine may increase the QTc-prolonging activities of Vandetanib.
MetforminThe serum concentration of Metformin can be increased when it is combined with Vandetanib.
MethadoneMethadone may increase the QTc-prolonging activities of Vandetanib.
MethotrimeprazineMethotrimeprazine may increase the QTc-prolonging activities of Vandetanib.
MetoclopramideMetoclopramide may increase the QTc-prolonging activities of Vandetanib.
MetronidazoleMetronidazole may increase the QTc-prolonging activities of Vandetanib.
MifepristoneMifepristone may increase the QTc-prolonging activities of Vandetanib.
MirabegronMirabegron may increase the QTc-prolonging activities of Vandetanib.
MirtazapineMirtazapine may increase the QTc-prolonging activities of Vandetanib.
MitotaneThe serum concentration of Vandetanib can be decreased when it is combined with Mitotane.
ModafinilThe serum concentration of Vandetanib can be decreased when it is combined with Modafinil.
MoexiprilMoexipril may increase the QTc-prolonging activities of Vandetanib.
MoxifloxacinMoxifloxacin may increase the QTc-prolonging activities of Vandetanib.
NafcillinThe serum concentration of Vandetanib can be decreased when it is combined with Nafcillin.
NefazodoneThe metabolism of Vandetanib can be decreased when combined with Nefazodone.
NelfinavirThe metabolism of Vandetanib can be decreased when combined with Nelfinavir.
NetupitantThe serum concentration of Vandetanib can be increased when it is combined with Netupitant.
NevirapineThe serum concentration of Vandetanib can be decreased when it is combined with Nevirapine.
NicardipineNicardipine may increase the QTc-prolonging activities of Vandetanib.
NilotinibNilotinib may increase the QTc-prolonging activities of Vandetanib.
NorfloxacinNorfloxacin may increase the QTc-prolonging activities of Vandetanib.
NortriptylineNortriptyline may increase the QTc-prolonging activities of Vandetanib.
OctreotideOctreotide may increase the QTc-prolonging activities of Vandetanib.
OfloxacinOfloxacin may increase the QTc-prolonging activities of Vandetanib.
OlanzapineOlanzapine may increase the QTc-prolonging activities of Vandetanib.
OlaparibThe metabolism of Vandetanib can be decreased when combined with Olaparib.
OlodaterolOlodaterol may increase the QTc-prolonging activities of Vandetanib.
OndansetronOndansetron may increase the QTc-prolonging activities of Vandetanib.
OsimertinibThe serum concentration of Vandetanib can be increased when it is combined with Osimertinib.
OuabainOuabain may decrease the cardiotoxic activities of Vandetanib.
OxytocinOxytocin may increase the QTc-prolonging activities of Vandetanib.
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Vandetanib.
PalbociclibThe serum concentration of Vandetanib can be increased when it is combined with Palbociclib.
PaliperidonePaliperidone may increase the QTc-prolonging activities of Vandetanib.
PanobinostatPanobinostat may increase the QTc-prolonging activities of Vandetanib.
ParoxetineParoxetine may increase the QTc-prolonging activities of Vandetanib.
PasireotidePasireotide may increase the QTc-prolonging activities of Vandetanib.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Vandetanib.
PazopanibPazopanib may increase the QTc-prolonging activities of Vandetanib.
PentamidinePentamidine may increase the QTc-prolonging activities of Vandetanib.
PentobarbitalThe serum concentration of Vandetanib can be decreased when it is combined with Pentobarbital.
PerflutrenPerflutren may increase the QTc-prolonging activities of Vandetanib.
PhenobarbitalThe serum concentration of Vandetanib can be decreased when it is combined with Phenobarbital.
PhenytoinThe serum concentration of Vandetanib can be decreased when it is combined with Phenytoin.
PimozidePimozide may increase the QTc-prolonging activities of Vandetanib.
PosaconazoleThe metabolism of Vandetanib can be decreased when combined with Posaconazole.
PrimaquinePrimaquine may increase the QTc-prolonging activities of Vandetanib.
PrimidoneThe serum concentration of Vandetanib can be decreased when it is combined with Primidone.
ProcainamideProcainamide may increase the QTc-prolonging activities of Vandetanib.
PromazinePromazine may increase the QTc-prolonging activities of Vandetanib.
PromethazinePromethazine may increase the QTc-prolonging activities of Vandetanib.
PropafenonePropafenone may increase the QTc-prolonging activities of Vandetanib.
PropofolPropofol may increase the QTc-prolonging activities of Vandetanib.
ProtriptylineProtriptyline may increase the QTc-prolonging activities of Vandetanib.
QuetiapineQuetiapine may increase the QTc-prolonging activities of Vandetanib.
QuinidineQuinidine may increase the QTc-prolonging activities of Vandetanib.
QuinineQuinine may increase the QTc-prolonging activities of Vandetanib.
RanolazineThe metabolism of Vandetanib can be decreased when combined with Ranolazine.
RifabutinThe serum concentration of Vandetanib can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Vandetanib can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Vandetanib can be decreased when it is combined with Rifapentine.
RilpivirineRilpivirine may increase the QTc-prolonging activities of Vandetanib.
RisperidoneRisperidone may increase the QTc-prolonging activities of Vandetanib.
RitonavirThe metabolism of Vandetanib can be decreased when combined with Ritonavir.
SalbutamolSalbutamol may increase the QTc-prolonging activities of Vandetanib.
SalmeterolSalmeterol may increase the QTc-prolonging activities of Vandetanib.
SaquinavirSaquinavir may increase the QTc-prolonging activities of Vandetanib.
SertralineSertraline may increase the QTc-prolonging activities of Vandetanib.
SevofluraneSevoflurane may increase the QTc-prolonging activities of Vandetanib.
SildenafilThe metabolism of Vandetanib can be decreased when combined with Sildenafil.
SiltuximabThe serum concentration of Vandetanib can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Vandetanib can be increased when it is combined with Simeprevir.
SolifenacinSolifenacin may increase the QTc-prolonging activities of Vandetanib.
SorafenibSorafenib may increase the QTc-prolonging activities of Vandetanib.
SotalolSotalol may increase the QTc-prolonging activities of Vandetanib.
St. John's WortThe serum concentration of Vandetanib can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Vandetanib can be increased when it is combined with Stiripentol.
SulfamethoxazoleSulfamethoxazole may increase the QTc-prolonging activities of Vandetanib.
SulfisoxazoleSulfisoxazole may increase the QTc-prolonging activities of Vandetanib.
SunitinibSunitinib may increase the QTc-prolonging activities of Vandetanib.
TamoxifenTamoxifen may increase the QTc-prolonging activities of Vandetanib.
TelaprevirThe metabolism of Vandetanib can be decreased when combined with Telaprevir.
TelavancinTelavancin may increase the QTc-prolonging activities of Vandetanib.
TelithromycinTelithromycin may increase the QTc-prolonging activities of Vandetanib.
TerbutalineTerbutaline may increase the QTc-prolonging activities of Vandetanib.
TetrabenazineTetrabenazine may increase the QTc-prolonging activities of Vandetanib.
ThioridazineThioridazine may increase the QTc-prolonging activities of Vandetanib.
ThiothixeneThiothixene may increase the QTc-prolonging activities of Vandetanib.
TiclopidineThe metabolism of Vandetanib can be decreased when combined with Ticlopidine.
TizanidineTizanidine may increase the QTc-prolonging activities of Vandetanib.
TocilizumabThe serum concentration of Vandetanib can be decreased when it is combined with Tocilizumab.
TolterodineTolterodine may increase the QTc-prolonging activities of Vandetanib.
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Vandetanib.
ToremifeneToremifene may increase the QTc-prolonging activities of Vandetanib.
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Vandetanib.
TrazodoneTrazodone may increase the QTc-prolonging activities of Vandetanib.
TreprostinilTreprostinil may increase the QTc-prolonging activities of Vandetanib.
TrimethoprimTrimethoprim may increase the QTc-prolonging activities of Vandetanib.
TrimipramineTrimipramine may increase the QTc-prolonging activities of Vandetanib.
TriptorelinTriptorelin may increase the QTc-prolonging activities of Vandetanib.
VardenafilVardenafil may increase the QTc-prolonging activities of Vandetanib.
VemurafenibVandetanib may increase the QTc-prolonging activities of Vemurafenib.
VenlafaxineThe metabolism of Vandetanib can be decreased when combined with Venlafaxine.
VerapamilThe metabolism of Vandetanib can be decreased when combined with Verapamil.
VilanterolVilanterol may increase the QTc-prolonging activities of Vandetanib.
VoriconazoleThe metabolism of Vandetanib can be decreased when combined with Voriconazole.
VorinostatVorinostat may increase the QTc-prolonging activities of Vandetanib.
ZiprasidoneZiprasidone may increase the QTc-prolonging activities of Vandetanib.
ZuclopenthixolZuclopenthixol may increase the QTc-prolonging activities of Vandetanib.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Vascular endothelial growth factor receptor binding
Specific Function:
Growth factor active in angiogenesis, vasculogenesis and endothelial cell growth. Induces endothelial cell proliferation, promotes cell migration, inhibits apoptosis and induces permeabilization of blood vessels. Binds to the FLT1/VEGFR1 and KDR/VEGFR2 receptors, heparan sulfate and heparin. NRP1/Neuropilin-1 binds isoforms VEGF-165 and VEGF-145. Isoform VEGF165B binds to KDR but does not activ...
Gene Name:
VEGFA
Uniprot ID:
P15692
Molecular Weight:
27042.205 Da
References
  1. Link [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Ubiquitin protein ligase binding
Specific Function:
Receptor tyrosine kinase binding ligands of the EGF family and activating several signaling cascades to convert extracellular cues into appropriate cellular responses. Known ligands include EGF, TGFA/TGF-alpha, amphiregulin, epigen/EPGN, BTC/betacellulin, epiregulin/EREG and HBEGF/heparin-binding EGF. Ligand binding triggers receptor homo- and/or heterodimerization and autophosphorylation on ke...
Gene Name:
EGFR
Uniprot ID:
P00533
Molecular Weight:
134276.185 Da
References
  1. Link [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Receptor binding
Specific Function:
Non-receptor tyrosine-protein kinase implicated in the regulation of a variety of signaling pathways that control the differentiation and maintenance of normal epithelia, as well as tumor growth. Function seems to be context dependent and differ depending on cell type, as well as its intracellular localization. A number of potential nuclear and cytoplasmic substrates have been identified. These...
Gene Name:
PTK6
Uniprot ID:
Q13882
Molecular Weight:
51833.72 Da
References
  1. Link [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Transmembrane receptor protein tyrosine kinase activity
Specific Function:
Tyrosine-protein kinase that acts as cell-surface receptor for ANGPT1, ANGPT2 and ANGPT4 and regulates angiogenesis, endothelial cell survival, proliferation, migration, adhesion and cell spreading, reorganization of the actin cytoskeleton, but also maintenance of vascular quiescence. Has anti-inflammatory effects by preventing the leakage of proinflammatory plasma proteins and leukocytes from ...
Gene Name:
TEK
Uniprot ID:
Q02763
Molecular Weight:
125829.005 Da
References
  1. Link [Link]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Nadp binding
Specific Function:
This protein is involved in the oxidative metabolism of a variety of xenobiotics such as drugs and pesticides. Form I catalyzes the N-oxygenation of secondary and tertiary amines.
Gene Name:
FMO1
Uniprot ID:
Q01740
Molecular Weight:
60310.285 Da
References
  1. Link [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Trimethylamine monooxygenase activity
Specific Function:
Involved in the oxidative metabolism of a variety of xenobiotics such as drugs and pesticides. It N-oxygenates primary aliphatic alkylamines as well as secondary and tertiary amines. Plays an important role in the metabolism of trimethylamine (TMA), via the production of TMA N-oxide (TMAO). Is also able to perform S-oxidation when acting on sulfide compounds (PubMed:9224773).
Gene Name:
FMO3
Uniprot ID:
P31513
Molecular Weight:
60032.975 Da
References
  1. Link [Link]
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. Link [Link]

Carriers

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

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Transporter activity
Specific Function:
Mediates export of organic anions and drugs from the cytoplasm. Mediates ATP-dependent transport of glutathione and glutathione conjugates, leukotriene C4, estradiol-17-beta-o-glucuronide, methotrexate, antiviral drugs and other xenobiotics. Confers resistance to anticancer drugs. Hydrolyzes ATP with low efficiency.
Gene Name:
ABCC1
Uniprot ID:
P33527
Molecular Weight:
171589.5 Da
References
  1. Zheng LS, Wang F, Li YH, Zhang X, Chen LM, Liang YJ, Dai CL, Yan YY, Tao LY, Mi YJ, Yang AK, To KK, Fu LW: Vandetanib (Zactima, ZD6474) antagonizes ABCC1- and ABCG2-mediated multidrug resistance by inhibition of their transport function. PLoS One. 2009;4(4):e5172. doi: 10.1371/journal.pone.0005172. Epub 2009 Apr 23. [PubMed:19390592 ]
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. Zheng LS, Wang F, Li YH, Zhang X, Chen LM, Liang YJ, Dai CL, Yan YY, Tao LY, Mi YJ, Yang AK, To KK, Fu LW: Vandetanib (Zactima, ZD6474) antagonizes ABCC1- and ABCG2-mediated multidrug resistance by inhibition of their transport function. PLoS One. 2009;4(4):e5172. doi: 10.1371/journal.pone.0005172. Epub 2009 Apr 23. [PubMed:19390592 ]
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Drug created on November 18, 2007 11:23 / Updated on September 26, 2016 02:14