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Identification
NameLenvatinib
Accession NumberDB09078
TypeSmall Molecule
GroupsApproved
DescriptionLenvatinib is a receptor tyrosine kinase (RTK) inhibitor that inhibits the kinase activities of vascular endothelial growth factor (VEGF) receptors VEGFR1 (FLT1), VEGFR2 (KDR), and VEGFR3 (FLT4). Lenvatinib also inhibits other RTKs that have been implicated in pathogenic angiogenesis, tumor growth, and cancer progression in addition to their normal cellular functions, including fibroblast growth factor (FGF) receptors FGFR1, 2, 3, and 4; the platelet derived growth factor receptor alpha (PDGFRα), KIT, and RET. These receptor tyrosine kinases (RTKs) located in the cell membrane play a central role in the activation of signal transduction pathways involved in the normal regulation of cellular processes, such as cell proliferation, migration, apoptosis and differentiation, and in pathogenic angiogenesis, lymphogenesis, tumour growth and cancer progression. In particular, VEGF has been identified as a crucial regulator of both physiologic and pathologic angiogenesis and increased expression of VEGF is associated with a poor prognosis in many types of cancers. Lenvatinib is indicated for the treatment of patients with locally recurrent or metastatic, progressive, radioactive iodine (RAI)-refractory differentiated thyroid cancer. Most patients with thyroid cancer have a very good prognosis with treatment (98% 5 year survival rate) involving surgery and hormone therapy. However, for patients with RAI-refractory thyroid cancer, treatment options are limited and the prognosis is poor, leading to a push for the development of more targeted therapies such as lenvatinib.
Structure
Thumb
Synonyms
4-{3-chloro-4-[(cyclopropylcarbamoyl)amino]phenoxy}-7-methoxyquinoline-6-carboxamide
Lenvatinib Mesylate
External Identifiers
  • E 7080
  • E-7080
  • E7080
  • ER-203492-00
  • UNII-EE083865G2
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
LenvimaKitEisai Inc.2015-02-13Not applicableUs
LenvimaCapsule24 mgOralEisai Limited2016-03-31Not applicableCanada
LenvimaCapsule10 mg/1OralEisai Inc.2015-02-13Not applicableUs
LenvimaCapsule4 mg/1OralEisai Inc.2016-05-13Not applicableUs
LenvimaCapsule20 mgOralEisai Limited2016-03-31Not applicableCanada
LenvimaKitEisai Inc.2015-02-13Not applicableUs
LenvimaKitEisai Inc.2016-05-13Not applicableUs
LenvimaCapsule14 mgOralEisai Limited2016-03-31Not applicableCanada
LenvimaCapsule10 mg/1OralEisai Inc.2015-02-13Not applicableUs
LenvimaCapsule10 mgOralEisai Limited2016-03-31Not applicableCanada
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
Lenvatinib Mesylate
ThumbNot applicableDBSALT001109
Categories
UNIIEE083865G2
CAS number417716-92-8
WeightAverage: 426.86
Monoisotopic: 426.1094828
Chemical FormulaC21H19ClN4O4
InChI KeyWOSKHXYHFSIKNG-UHFFFAOYSA-N
InChI
InChI=1S/C21H19ClN4O4/c1-29-19-10-17-13(9-14(19)20(23)27)18(6-7-24-17)30-12-4-5-16(15(22)8-12)26-21(28)25-11-2-3-11/h4-11H,2-3H2,1H3,(H2,23,27)(H2,25,26,28)
IUPAC Name
4-{3-chloro-4-[(cyclopropyl-C-hydroxycarbonimidoyl)amino]phenoxy}-7-methoxyquinoline-6-carboximidic acid
SMILES
COC1=C(C=C2C(OC3=CC(Cl)=C(NC(O)=NC4CC4)C=C3)=CC=NC2=C1)C(O)=N
Pharmacology
IndicationLenvatinib is indicated for the treatment of patients with locally recurrent or metastatic, progressive, radioactive iodine-refractory differentiated thyroid cancer.
Structured Indications
PharmacodynamicsBased on x-ray crystallography and kinetic interaction studies, lenvatinib binds to the adenosine 5'-triphosphate binding site of VEGFR2 and to a neighbouring region via a cyclopropane ring and thereby inhibits tyrosine kinase activity and associated signalling pathways.
Mechanism of actionLenvatinib is a receptor tyrosine kinase (RTK) inhibitor that inhibits the kinase activities of vascular endothelial growth factor (VEGF) receptors VEGFR1 (FLT1), VEGFR2 (KDR), and VEGFR3 (FLT4). Lenvatinib also inhibits other RTKs that have been implicated in pathogenic angiogenesis, tumor growth, and cancer progression in addition to their normal cellular functions, including fibroblast growth factor (FGF) receptors FGFR1, 2, 3, and 4; the platelet derived growth factor receptor alpha (PDGFRα), KIT, and RET.
TargetKindPharmacological actionActionsOrganismUniProt ID
Vascular endothelial growth factor receptor 1Proteinyes
Inhibitor
HumanP17948 details
Vascular endothelial growth factor receptor 2Proteinyes
Inhibitor
HumanP35968 details
Vascular endothelial growth factor receptor 3Proteinyes
Inhibitor
HumanP35916 details
Fibroblast growth factor receptor 1Proteinyes
Inhibitor
HumanP11362 details
Fibroblast growth factor receptor 2Proteinyes
Inhibitor
HumanP21802 details
Fibroblast growth factor receptor 3Proteinyes
Inhibitor
HumanP22607 details
Fibroblast growth factor receptor 4Proteinyes
Inhibitor
HumanP22455 details
Platelet derived growth factor receptor alphaProteinyes
Inhibitor
Humannot applicabledetails
RET Proteinyes
Inhibitor
Humannot applicabledetails
Mast/stem cell growth factor receptor KitProteinyes
Inhibitor
HumanP10721 details
Related Articles
AbsorptionTime to peak plasma concentration occurred from 1 to 4 hours post­dose. Administration with food did not affect the extent of absorption, but decreased the rate of absorption and delayed the median Tmax from 2 hours to 4 hours.
Volume of distributionNot Available
Protein bindingIn vitro binding of lenvatinib to human plasma proteins ranged from 98% to 99%.
Metabolism

Lenvatinib is metabolized by CYP3A and aldehyde oxidase.

Route of eliminationFollowing administration of a radiolabeled dose, approximately 64% and 25% of the radiolabel were eliminated in the feces and urine, respectively.
Half lifeThe terminal elimination half­life of lenvatinib is approximately 28 hours.
ClearanceNot Available
ToxicityThe most common adverse events that occurred in lenvatinib recipients were hypertension (67.8 vs. 9.2 % in the placebo group), diarrhea (59.4 vs. 8.4 %), fatigue or asthenia (59.0 vs. 27.5 %), decreased appetite (50.2 vs. 11.5 %), decreased bodyweight (46.4 vs. 9.2 %), nausea (41.0 vs. 13.7 %), stomatitis (35.6 vs. 3.8 %), palmar-plantar erythrodysethesia syndrome (31.8 vs. 8.0 %) and proteinuria (31.0 vs. 1.5 %). Adverse events that occurred in clinical trials and for which there is a warning/precaution in US manufacturer’s pre- scribing information were hypertension, cardiac dysfunction (decreased left or right ventricular function, cardiac failure or pulmonary edema), arterial thromboembolic events, hepatotoxicity, proteinuria, renal failure and impairment, gastrointestinal perforation and fistula formation, QT interval prolongation, hypocalcaemia, reversible posterior leucoencephalopathy syndrome, haemorrhagic events, and impairment of thyroid stimulating hormone (TSH) suppression. Based on the mechanism of action of lenvatinib and results from animal reproduction studies, which showed embryotoxicity, foetotoxicity and teratogenicity at lenvatinib doses below the recommended dose in humans, females of reproductive potential should be advised to use effective contraception during treatment and for at least 2 weeks following completion of therapy.
Affected organismsNot Available
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
AcetaminophenThe serum concentration of Lenvatinib can be increased when it is combined with Acetaminophen.Approved
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Lenvatinib.Approved
AfatinibThe serum concentration of Lenvatinib can be increased when it is combined with Afatinib.Approved
AlbendazoleThe serum concentration of Lenvatinib can be increased when it is combined with Albendazole.Approved, Vet Approved
AldosteroneThe serum concentration of Lenvatinib can be decreased when it is combined with Aldosterone.Experimental
AlectinibThe serum concentration of Lenvatinib can be increased when it is combined with Alectinib.Approved
AlfentanilThe serum concentration of Lenvatinib can be increased when it is combined with Alfentanil.Approved, Illicit
AlfuzosinAlfuzosin may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
AmantadineAmantadine may increase the QTc-prolonging activities of Lenvatinib.Approved
Aminohippuric acidThe serum concentration of Lenvatinib can be increased when it is combined with Aminohippuric acid.Approved
AmiodaroneLenvatinib may increase the QTc-prolonging activities of Amiodarone.Approved, Investigational
AmitriptylineAmitriptyline may increase the QTc-prolonging activities of Lenvatinib.Approved
AmlodipineThe serum concentration of Lenvatinib can be increased when it is combined with Amlodipine.Approved
AmoxapineAmoxapine may increase the QTc-prolonging activities of Lenvatinib.Approved
AmprenavirThe serum concentration of Lenvatinib can be decreased when it is combined with Amprenavir.Approved
AmsacrineThe serum concentration of Lenvatinib can be increased when it is combined with Amsacrine.Approved
AnagrelideLenvatinib may increase the QTc-prolonging activities of Anagrelide.Approved
AnvirzelAnvirzel may decrease the cardiotoxic activities of Lenvatinib.Investigational
ApomorphineApomorphine may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
AprepitantThe serum concentration of Lenvatinib can be increased when it is combined with Aprepitant.Approved, Investigational
ArformoterolArformoterol may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
AripiprazoleAripiprazole may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
Arsenic trioxideLenvatinib may increase the QTc-prolonging activities of Arsenic trioxide.Approved, Investigational
ArtemetherLenvatinib may increase the QTc-prolonging activities of Artemether.Approved
AsenapineLenvatinib may increase the QTc-prolonging activities of Asenapine.Approved
AstemizoleThe serum concentration of Lenvatinib can be increased when it is combined with Astemizole.Approved, Withdrawn
AtazanavirThe metabolism of Lenvatinib can be decreased when combined with Atazanavir.Approved, Investigational
AtenololThe serum concentration of Lenvatinib can be increased when it is combined with Atenolol.Approved
AtomoxetineAtomoxetine may increase the QTc-prolonging activities of Lenvatinib.Approved
AtorvastatinThe serum concentration of Lenvatinib can be increased when it is combined with Atorvastatin.Approved
AzelastineThe serum concentration of Lenvatinib can be increased when it is combined with Azelastine.Approved
AzithromycinAzithromycin may increase the QTc-prolonging activities of Lenvatinib.Approved
BedaquilineBedaquiline may increase the QTc-prolonging activities of Lenvatinib.Approved
BenzocaineThe serum concentration of Lenvatinib can be increased when it is combined with Benzocaine.Approved
BepridilThe serum concentration of Lenvatinib can be increased when it is combined with Bepridil.Approved, Withdrawn
BevacizumabBevacizumab may increase the cardiotoxic activities of Lenvatinib.Approved, Investigational
BexaroteneThe serum concentration of Lenvatinib can be decreased when it is combined with Bexarotene.Approved, Investigational
BiperidenThe serum concentration of Lenvatinib can be increased when it is combined with Biperiden.Approved
BoceprevirThe metabolism of Lenvatinib can be decreased when combined with Boceprevir.Approved
BortezomibBortezomib may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
BosentanThe serum concentration of Lenvatinib can be decreased when it is combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Lenvatinib can be increased when it is combined with Bosutinib.Approved
BromocriptineThe serum concentration of Lenvatinib can be increased when it is combined with Bromocriptine.Approved, Investigational
BuprenorphineThe serum concentration of Lenvatinib can be increased when it is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BuserelinBuserelin may increase the QTc-prolonging activities of Lenvatinib.Approved
BuspironeThe serum concentration of Lenvatinib can be increased when it is combined with Buspirone.Approved, Investigational
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Lenvatinib.Approved
CaffeineThe serum concentration of Lenvatinib can be increased when it is combined with Caffeine.Approved
CanagliflozinThe serum concentration of Lenvatinib can be increased when it is combined with Canagliflozin.Approved
CandesartanThe serum concentration of Lenvatinib can be increased when it is combined with Candesartan.Approved
CaptoprilThe serum concentration of Lenvatinib can be increased when it is combined with Captopril.Approved
CarbamazepineThe metabolism of Lenvatinib can be increased when combined with Carbamazepine.Approved, Investigational
CarvedilolThe serum concentration of Lenvatinib can be increased when it is combined with Carvedilol.Approved, Investigational
CaspofunginThe serum concentration of Lenvatinib can be increased when it is combined with Caspofungin.Approved
CeritinibThe serum concentration of Lenvatinib can be increased when it is combined with Ceritinib.Approved
ChloroquineChloroquine may increase the QTc-prolonging activities of Lenvatinib.Approved, Vet Approved
ChlorpromazineChlorpromazine may increase the QTc-prolonging activities of Lenvatinib.Approved, Vet Approved
ChlorpropamideThe serum concentration of Lenvatinib can be increased when it is combined with Chlorpropamide.Approved
ChlorprothixeneThe serum concentration of Lenvatinib can be increased when it is combined with Chlorprothixene.Approved, Withdrawn
CholesterolThe serum concentration of Lenvatinib can be increased when it is combined with Cholesterol.Experimental
Cholic AcidThe serum concentration of Lenvatinib can be decreased when it is combined with Cholic Acid.Approved
CilazaprilThe serum concentration of Lenvatinib can be increased when it is combined with Cilazapril.Approved
CimetidineThe serum concentration of Lenvatinib can be decreased when it is combined with Cimetidine.Approved
CiprofloxacinCiprofloxacin may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
CisaprideLenvatinib may increase the QTc-prolonging activities of Cisapride.Approved, Investigational, Withdrawn
CitalopramLenvatinib may increase the QTc-prolonging activities of Citalopram.Approved
ClarithromycinClarithromycin may increase the QTc-prolonging activities of Lenvatinib.Approved
ClemastineThe metabolism of Lenvatinib can be decreased when combined with Clemastine.Approved
ClofazimineThe serum concentration of Lenvatinib can be increased when it is combined with Clofazimine.Approved, Investigational
ClomipramineClomipramine may increase the QTc-prolonging activities of Lenvatinib.Approved, Vet Approved
ClotrimazoleThe metabolism of Lenvatinib can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineClozapine may increase the QTc-prolonging activities of Lenvatinib.Approved
CobicistatThe metabolism of Lenvatinib can be decreased when combined with Cobicistat.Approved
ColchicineThe serum concentration of Lenvatinib can be increased when it is combined with Colchicine.Approved
ColforsinThe serum concentration of Lenvatinib can be increased when it is combined with Colforsin.Experimental
ConivaptanThe serum concentration of Lenvatinib can be increased when it is combined with Conivaptan.Approved, Investigational
CrizotinibCrizotinib may increase the QTc-prolonging activities of Lenvatinib.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Lenvatinib.Approved, Investigational
CyclosporineThe metabolism of Lenvatinib can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
DabrafenibThe serum concentration of Lenvatinib can be decreased when it is combined with Dabrafenib.Approved
DaclatasvirThe serum concentration of Lenvatinib can be increased when it is combined with Daclatasvir.Approved
DactinomycinThe serum concentration of Lenvatinib can be increased when it is combined with Dactinomycin.Approved
DarunavirThe metabolism of Lenvatinib can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Lenvatinib can be increased when it is combined with Dasatinib.Approved, Investigational
DaunorubicinThe serum concentration of Lenvatinib can be decreased when it is combined with Daunorubicin.Approved
DeferasiroxThe serum concentration of Lenvatinib can be decreased when it is combined with Deferasirox.Approved, Investigational
DegarelixDegarelix may increase the QTc-prolonging activities of Lenvatinib.Approved
DelavirdineThe metabolism of Lenvatinib can be decreased when combined with Delavirdine.Approved
DesfluraneDesflurane may increase the QTc-prolonging activities of Lenvatinib.Approved
DesipramineDesipramine may increase the QTc-prolonging activities of Lenvatinib.Approved
DeslanosideDeslanoside may decrease the cardiotoxic activities of Lenvatinib.Approved
DesloratadineThe serum concentration of Lenvatinib can be increased when it is combined with Desloratadine.Approved, Investigational
DexamethasoneThe serum concentration of Lenvatinib can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DextromethorphanThe serum concentration of Lenvatinib can be increased when it is combined with Dextromethorphan.Approved
DiclofenacThe serum concentration of Lenvatinib can be increased when it is combined with Diclofenac.Approved, Vet Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Lenvatinib.Approved
DigoxinDigoxin may decrease the cardiotoxic activities of Lenvatinib.Approved
DihydroergotamineThe metabolism of Lenvatinib can be decreased when combined with Dihydroergotamine.Approved
DiltiazemThe metabolism of Lenvatinib can be decreased when combined with Diltiazem.Approved
DiphenhydramineDiphenhydramine may increase the QTc-prolonging activities of Lenvatinib.Approved
DipyridamoleThe serum concentration of Lenvatinib can be increased when it is combined with Dipyridamole.Approved
DisopyramideLenvatinib may increase the QTc-prolonging activities of Disopyramide.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Lenvatinib.Approved, Investigational
DofetilideLenvatinib may increase the QTc-prolonging activities of Dofetilide.Approved
DolasetronDolasetron may increase the QTc-prolonging activities of Lenvatinib.Approved
DomperidoneLenvatinib may increase the QTc-prolonging activities of Domperidone.Approved, Investigational, Vet Approved
DoxazosinThe serum concentration of Lenvatinib can be increased when it is combined with Doxazosin.Approved
DoxepinDoxepin may increase the QTc-prolonging activities of Lenvatinib.Approved
DoxorubicinThe serum concentration of Lenvatinib can be decreased when it is combined with Doxorubicin.Approved, Investigational
DoxycyclineThe metabolism of Lenvatinib can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronabinolThe serum concentration of Lenvatinib can be increased when it is combined with Dronabinol.Approved, Illicit
DronedaroneLenvatinib may increase the QTc-prolonging activities of Dronedarone.Approved
DroperidolDroperidol may increase the QTc-prolonging activities of Lenvatinib.Approved, Vet Approved
EfavirenzThe serum concentration of Lenvatinib can be decreased when it is combined with Efavirenz.Approved, Investigational
ElbasvirThe serum concentration of Lenvatinib can be increased when it is combined with Elbasvir.Approved
EliglustatLenvatinib may increase the QTc-prolonging activities of Eliglustat.Approved
EltrombopagThe serum concentration of Lenvatinib can be increased when it is combined with Eltrombopag.Approved
EnalaprilThe serum concentration of Lenvatinib can be increased when it is combined with Enalapril.Approved, Vet Approved
EnzalutamideThe serum concentration of Lenvatinib can be decreased when it is combined with Enzalutamide.Approved
ErgonovineThe serum concentration of Lenvatinib can be increased when it is combined with Ergonovine.Approved
ErgotamineThe serum concentration of Lenvatinib can be increased when it is combined with Ergotamine.Approved
EribulinEribulin may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
ErythromycinErythromycin may increase the QTc-prolonging activities of Lenvatinib.Approved, Vet Approved
EscitalopramLenvatinib may increase the QTc-prolonging activities of Escitalopram.Approved, Investigational
Eslicarbazepine acetateThe serum concentration of Lenvatinib can be decreased when it is combined with Eslicarbazepine acetate.Approved
EstramustineThe serum concentration of Lenvatinib can be increased when it is combined with Estramustine.Approved
EstriolThe serum concentration of Lenvatinib can be decreased when it is combined with Estriol.Approved, Vet Approved
EstroneThe serum concentration of Lenvatinib can be decreased when it is combined with Estrone.Approved
EtoposideThe serum concentration of Lenvatinib can be increased when it is combined with Etoposide.Approved
EtravirineThe serum concentration of Lenvatinib can be decreased when it is combined with Etravirine.Approved
EzogabineEzogabine may increase the QTc-prolonging activities of Lenvatinib.Approved
FamotidineFamotidine may increase the QTc-prolonging activities of Lenvatinib.Approved
FelbamateFelbamate may increase the QTc-prolonging activities of Lenvatinib.Approved
FelodipineThe serum concentration of Lenvatinib can be increased when it is combined with Felodipine.Approved, Investigational
FentanylThe serum concentration of Lenvatinib can be increased when it is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FexofenadineThe serum concentration of Lenvatinib can be increased when it is combined with Fexofenadine.Approved
FidaxomicinThe serum concentration of Lenvatinib can be increased when it is combined with Fidaxomicin.Approved
FingolimodFingolimod may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
FlecainideFlecainide may increase the QTc-prolonging activities of Lenvatinib.Approved, Withdrawn
FluconazoleFluconazole may increase the QTc-prolonging activities of Lenvatinib.Approved
FluoxetineLenvatinib may increase the QTc-prolonging activities of Fluoxetine.Approved, Vet Approved
FlupentixolLenvatinib may increase the QTc-prolonging activities of Flupentixol.Approved, Withdrawn
FluphenazineThe serum concentration of Lenvatinib can be increased when it is combined with Fluphenazine.Approved
FlurazepamThe serum concentration of Lenvatinib can be increased when it is combined with Flurazepam.Approved, Illicit
FluvoxamineThe metabolism of Lenvatinib can be decreased when combined with Fluvoxamine.Approved, Investigational
FormoterolFormoterol may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
FosamprenavirThe metabolism of Lenvatinib can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Lenvatinib can be increased when it is combined with Fosaprepitant.Approved
FoscarnetFoscarnet may increase the QTc-prolonging activities of Lenvatinib.Approved
FosphenytoinThe metabolism of Lenvatinib can be increased when combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Lenvatinib can be increased when it is combined with Fusidic Acid.Approved
Gadobenic acidGadobenic acid may increase the QTc-prolonging activities of Lenvatinib.Approved
GalantamineGalantamine may increase the QTc-prolonging activities of Lenvatinib.Approved
GefitinibThe serum concentration of Lenvatinib can be increased when it is combined with Gefitinib.Approved, Investigational
GemifloxacinGemifloxacin may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
GenisteinThe serum concentration of Lenvatinib can be increased when it is combined with Genistein.Investigational
GlyburideThe serum concentration of Lenvatinib can be increased when it is combined with Glyburide.Approved
GlycerolThe serum concentration of Lenvatinib can be increased when it is combined with Glycerol.Experimental
GoserelinGoserelin may increase the QTc-prolonging activities of Lenvatinib.Approved
Gramicidin DThe serum concentration of Lenvatinib can be increased when it is combined with Gramicidin D.Approved
GranisetronGranisetron may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
GrepafloxacinThe serum concentration of Lenvatinib can be increased when it is combined with Grepafloxacin.Withdrawn
HaloperidolHaloperidol may increase the QTc-prolonging activities of Lenvatinib.Approved
HistrelinHistrelin may increase the QTc-prolonging activities of Lenvatinib.Approved
HydrocortisoneThe serum concentration of Lenvatinib can be increased when it is combined with Hydrocortisone.Approved, Vet Approved
HydroxyzineHydroxyzine may increase the QTc-prolonging activities of Lenvatinib.Approved
IbandronateIbandronate may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
IbutilideLenvatinib may increase the QTc-prolonging activities of Ibutilide.Approved
IdelalisibThe serum concentration of Lenvatinib can be increased when it is combined with Idelalisib.Approved
IloperidoneLenvatinib may increase the QTc-prolonging activities of Iloperidone.Approved
ImatinibThe metabolism of Lenvatinib can be decreased when combined with Imatinib.Approved
ImipramineImipramine may increase the QTc-prolonging activities of Lenvatinib.Approved
IndacaterolIndacaterol may increase the QTc-prolonging activities of Lenvatinib.Approved
IndapamideIndapamide may increase the QTc-prolonging activities of Lenvatinib.Approved
IndinavirThe metabolism of Lenvatinib can be decreased when combined with Indinavir.Approved
IndomethacinThe serum concentration of Lenvatinib can be increased when it is combined with Indomethacin.Approved, Investigational
IsavuconazoniumThe metabolism of Lenvatinib can be decreased when combined with Isavuconazonium.Approved, Investigational
IsofluraneIsoflurane may increase the QTc-prolonging activities of Lenvatinib.Approved, Vet Approved
IsradipineIsradipine may increase the QTc-prolonging activities of Lenvatinib.Approved
ItraconazoleThe metabolism of Lenvatinib can be decreased when combined with Itraconazole.Approved, Investigational
IvabradineIvabradine may increase the QTc-prolonging activities of Lenvatinib.Approved
IvacaftorThe serum concentration of Lenvatinib can be increased when it is combined with Ivacaftor.Approved
IvermectinThe serum concentration of Lenvatinib can be increased when it is combined with Ivermectin.Approved, Vet Approved
KetamineThe serum concentration of Lenvatinib can be increased when it is combined with Ketamine.Approved, Vet Approved
KetoconazoleThe metabolism of Lenvatinib can be decreased when combined with Ketoconazole.Approved, Investigational
LansoprazoleThe serum concentration of Lenvatinib can be increased when it is combined with Lansoprazole.Approved, Investigational
LapatinibLapatinib may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
LeuprolideLeuprolide may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
LevofloxacinLevofloxacin may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
LevothyroxineThe serum concentration of Lenvatinib can be decreased when it is combined with Levothyroxine.Approved
LidocaineThe serum concentration of Lenvatinib can be increased when it is combined with Lidocaine.Approved, Vet Approved
LiothyronineThe serum concentration of Lenvatinib can be decreased when it is combined with Liothyronine.Approved, Vet Approved
LiotrixThe serum concentration of Lenvatinib can be decreased when it is combined with Liotrix.Approved
LisinoprilThe serum concentration of Lenvatinib can be increased when it is combined with Lisinopril.Approved, Investigational
LithiumLithium may increase the QTc-prolonging activities of Lenvatinib.Approved
LomitapideThe serum concentration of Lenvatinib can be increased when it is combined with Lomitapide.Approved
LoperamideThe serum concentration of Lenvatinib can be increased when it is combined with Loperamide.Approved
LopinavirLenvatinib may increase the QTc-prolonging activities of Lopinavir.Approved
LoratadineThe serum concentration of Lenvatinib can be increased when it is combined with Loratadine.Approved
LosartanThe serum concentration of Lenvatinib can be increased when it is combined with Losartan.Approved
LovastatinThe metabolism of Lenvatinib can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Lenvatinib can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Lenvatinib can be decreased when it is combined with Lumacaftor.Approved
LumefantrineLenvatinib may increase the QTc-prolonging activities of Lumefantrine.Approved
MaprotilineMaprotiline may increase the QTc-prolonging activities of Lenvatinib.Approved
MebendazoleThe serum concentration of Lenvatinib can be increased when it is combined with Mebendazole.Approved, Vet Approved
MefloquineMefloquine may increase the QTc-prolonging activities of Lenvatinib.Approved
Megestrol acetateThe serum concentration of Lenvatinib can be increased when it is combined with Megestrol acetate.Approved, Vet Approved
MeprobamateThe serum concentration of Lenvatinib can be increased when it is combined with Meprobamate.Approved, Illicit
MethadoneMethadone may increase the QTc-prolonging activities of Lenvatinib.Approved
MethotrimeprazineMethotrimeprazine may increase the QTc-prolonging activities of Lenvatinib.Approved
MetoclopramideMetoclopramide may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
MetoprololThe serum concentration of Lenvatinib can be increased when it is combined with Metoprolol.Approved, Investigational
MetronidazoleMetronidazole may increase the QTc-prolonging activities of Lenvatinib.Approved
MibefradilThe serum concentration of Lenvatinib can be increased when it is combined with Mibefradil.Withdrawn
MiconazoleThe serum concentration of Lenvatinib can be increased when it is combined with Miconazole.Approved, Investigational, Vet Approved
MidazolamThe serum concentration of Lenvatinib can be decreased when it is combined with Midazolam.Approved, Illicit
MifepristoneMifepristone may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
MirabegronMirabegron may increase the QTc-prolonging activities of Lenvatinib.Approved
MirtazapineMirtazapine may increase the QTc-prolonging activities of Lenvatinib.Approved
MitomycinThe serum concentration of Lenvatinib can be increased when it is combined with Mitomycin.Approved
MitotaneThe serum concentration of Lenvatinib can be decreased when it is combined with Mitotane.Approved
MitoxantroneThe serum concentration of Lenvatinib can be decreased when it is combined with Mitoxantrone.Approved, Investigational
ModafinilThe serum concentration of Lenvatinib can be decreased when it is combined with Modafinil.Approved, Investigational
MoexiprilMoexipril may increase the QTc-prolonging activities of Lenvatinib.Approved
MorphineThe serum concentration of Lenvatinib can be increased when it is combined with Morphine.Approved, Investigational
MoxifloxacinMoxifloxacin may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
NafcillinThe serum concentration of Lenvatinib can be decreased when it is combined with Nafcillin.Approved
NaltrexoneThe serum concentration of Lenvatinib can be increased when it is combined with Naltrexone.Approved, Investigational, Vet Approved
NaringeninThe serum concentration of Lenvatinib can be increased when it is combined with Naringenin.Experimental
NefazodoneThe metabolism of Lenvatinib can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Lenvatinib can be decreased when combined with Nelfinavir.Approved
NeostigmineThe serum concentration of Lenvatinib can be increased when it is combined with Neostigmine.Approved, Vet Approved
NetupitantThe serum concentration of Lenvatinib can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Lenvatinib can be increased when combined with Nevirapine.Approved
NicardipineNicardipine may increase the QTc-prolonging activities of Lenvatinib.Approved
NifedipineThe serum concentration of Lenvatinib can be decreased when it is combined with Nifedipine.Approved
NilotinibLenvatinib may increase the QTc-prolonging activities of Nilotinib.Approved, Investigational
NisoldipineThe serum concentration of Lenvatinib can be increased when it is combined with Nisoldipine.Approved
NitrazepamThe serum concentration of Lenvatinib can be increased when it is combined with Nitrazepam.Approved
NitrendipineThe serum concentration of Lenvatinib can be increased when it is combined with Nitrendipine.Approved
NorethisteroneThe serum concentration of Lenvatinib can be decreased when it is combined with Norethisterone.Approved
NorfloxacinNorfloxacin may increase the QTc-prolonging activities of Lenvatinib.Approved
NortriptylineNortriptyline may increase the QTc-prolonging activities of Lenvatinib.Approved
OctreotideOctreotide may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
OfloxacinOfloxacin may increase the QTc-prolonging activities of Lenvatinib.Approved
OlanzapineOlanzapine may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
OlaparibThe metabolism of Lenvatinib can be decreased when combined with Olaparib.Approved
OlodaterolOlodaterol may increase the QTc-prolonging activities of Lenvatinib.Approved
OmeprazoleThe serum concentration of Lenvatinib can be increased when it is combined with Omeprazole.Approved, Investigational, Vet Approved
OndansetronOndansetron may increase the QTc-prolonging activities of Lenvatinib.Approved
OsimertinibThe serum concentration of Lenvatinib can be increased when it is combined with Osimertinib.Approved
OuabainOuabain may decrease the cardiotoxic activities of Lenvatinib.Approved
OxytocinOxytocin may increase the QTc-prolonging activities of Lenvatinib.Approved, Vet Approved
P-NitrophenolThe serum concentration of Lenvatinib can be increased when it is combined with P-Nitrophenol.Experimental
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Lenvatinib.Approved, Vet Approved
PalbociclibThe serum concentration of Lenvatinib can be increased when it is combined with Palbociclib.Approved
PaliperidoneLenvatinib may increase the QTc-prolonging activities of Paliperidone.Approved
Palmitic AcidThe serum concentration of Lenvatinib can be increased when it is combined with Palmitic Acid.Experimental
PanobinostatPanobinostat may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
PantoprazoleThe serum concentration of Lenvatinib can be increased when it is combined with Pantoprazole.Approved
ParoxetineParoxetine may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
PasireotidePasireotide may increase the QTc-prolonging activities of Lenvatinib.Approved
PazopanibPazopanib may increase the QTc-prolonging activities of Lenvatinib.Approved
PentamidinePentamidine may increase the QTc-prolonging activities of Lenvatinib.Approved
PentobarbitalThe metabolism of Lenvatinib can be increased when combined with Pentobarbital.Approved, Vet Approved
PerflutrenPerflutren may increase the QTc-prolonging activities of Lenvatinib.Approved
PerindoprilThe serum concentration of Lenvatinib can be increased when it is combined with Perindopril.Approved
PhenobarbitalThe metabolism of Lenvatinib can be increased when combined with Phenobarbital.Approved
PhenytoinThe metabolism of Lenvatinib can be increased when combined with Phenytoin.Approved, Vet Approved
PimozideLenvatinib may increase the QTc-prolonging activities of Pimozide.Approved
Platelet Activating FactorThe serum concentration of Lenvatinib can be decreased when it is combined with Platelet Activating Factor.Experimental
PonatinibThe serum concentration of Lenvatinib can be increased when it is combined with Ponatinib.Approved
PosaconazoleThe metabolism of Lenvatinib can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PravastatinThe serum concentration of Lenvatinib can be increased when it is combined with Pravastatin.Approved
PrazosinThe serum concentration of Lenvatinib can be increased when it is combined with Prazosin.Approved
PrednisoneThe serum concentration of Lenvatinib can be increased when it is combined with Prednisone.Approved, Vet Approved
PrimaquinePrimaquine may increase the QTc-prolonging activities of Lenvatinib.Approved
PrimidoneThe metabolism of Lenvatinib can be increased when combined with Primidone.Approved, Vet Approved
ProbenecidThe serum concentration of Lenvatinib can be increased when it is combined with Probenecid.Approved
ProcainamideLenvatinib may increase the QTc-prolonging activities of Procainamide.Approved
ProgesteroneThe serum concentration of Lenvatinib can be decreased when it is combined with Progesterone.Approved, Vet Approved
PromazinePromazine may increase the QTc-prolonging activities of Lenvatinib.Approved, Vet Approved
PromethazinePromethazine may increase the QTc-prolonging activities of Lenvatinib.Approved
PropafenonePropafenone may increase the QTc-prolonging activities of Lenvatinib.Approved
PropofolPropofol may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational, Vet Approved
PropranololThe serum concentration of Lenvatinib can be increased when it is combined with Propranolol.Approved, Investigational
ProtriptylineProtriptyline may increase the QTc-prolonging activities of Lenvatinib.Approved
QuercetinThe serum concentration of Lenvatinib can be increased when it is combined with Quercetin.Experimental
QuetiapineLenvatinib may increase the QTc-prolonging activities of Quetiapine.Approved
QuinacrineThe serum concentration of Lenvatinib can be increased when it is combined with Quinacrine.Approved
QuinidineLenvatinib may increase the QTc-prolonging activities of Quinidine.Approved
QuinineLenvatinib may increase the QTc-prolonging activities of Quinine.Approved
RanitidineThe serum concentration of Lenvatinib can be increased when it is combined with Ranitidine.Approved
RanolazineThe serum concentration of Lenvatinib can be increased when it is combined with Ranolazine.Approved, Investigational
ReboxetineThe serum concentration of Lenvatinib can be increased when it is combined with Reboxetine.Approved, Investigational
RegorafenibThe serum concentration of Lenvatinib can be increased when it is combined with Regorafenib.Approved
ReserpineThe serum concentration of Lenvatinib can be decreased when it is combined with Reserpine.Approved
RifabutinThe metabolism of Lenvatinib can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Lenvatinib can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Lenvatinib can be increased when combined with Rifapentine.Approved
RilpivirineRilpivirine may increase the QTc-prolonging activities of Lenvatinib.Approved
RisperidoneRisperidone may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
RitonavirThe metabolism of Lenvatinib can be decreased when combined with Ritonavir.Approved, Investigational
RolapitantThe serum concentration of Lenvatinib can be increased when it is combined with Rolapitant.Approved
SalbutamolSalbutamol may increase the QTc-prolonging activities of Lenvatinib.Approved, Vet Approved
SalmeterolSalmeterol may increase the QTc-prolonging activities of Lenvatinib.Approved
SaquinavirSaquinavir may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
ScopolamineThe serum concentration of Lenvatinib can be increased when it is combined with Scopolamine.Approved
SelegilineThe serum concentration of Lenvatinib can be increased when it is combined with Selegiline.Approved, Investigational, Vet Approved
SertralineSertraline may increase the QTc-prolonging activities of Lenvatinib.Approved
SevofluraneSevoflurane may increase the QTc-prolonging activities of Lenvatinib.Approved, Vet Approved
SildenafilThe metabolism of Lenvatinib can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Lenvatinib can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Lenvatinib can be increased when it is combined with Simeprevir.Approved
SimvastatinThe serum concentration of Lenvatinib can be increased when it is combined with Simvastatin.Approved
SirolimusThe serum concentration of Lenvatinib can be decreased when it is combined with Sirolimus.Approved, Investigational
SolifenacinSolifenacin may increase the QTc-prolonging activities of Lenvatinib.Approved
SorafenibSorafenib may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
SotalolLenvatinib may increase the QTc-prolonging activities of Sotalol.Approved
SpironolactoneThe serum concentration of Lenvatinib can be increased when it is combined with Spironolactone.Approved
St. John's WortThe serum concentration of Lenvatinib can be decreased when it is combined with St. John's Wort.Nutraceutical
StaurosporineThe serum concentration of Lenvatinib can be increased when it is combined with Staurosporine.Experimental
StiripentolThe serum concentration of Lenvatinib can be increased when it is combined with Stiripentol.Approved
StreptozocinThe serum concentration of Lenvatinib can be decreased when it is combined with Streptozocin.Approved
SulfamethoxazoleSulfamethoxazole may increase the QTc-prolonging activities of Lenvatinib.Approved
SulfinpyrazoneThe serum concentration of Lenvatinib can be increased when it is combined with Sulfinpyrazone.Approved
SulfisoxazoleSulfisoxazole may increase the QTc-prolonging activities of Lenvatinib.Approved, Vet Approved
SumatriptanThe serum concentration of Lenvatinib can be increased when it is combined with Sumatriptan.Approved, Investigational
SunitinibSunitinib may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
TacrineThe serum concentration of Lenvatinib can be increased when it is combined with Tacrine.Withdrawn
TacrolimusThe serum concentration of Lenvatinib can be decreased when it is combined with Tacrolimus.Approved, Investigational
TamoxifenTamoxifen may increase the QTc-prolonging activities of Lenvatinib.Approved
Taurocholic AcidThe serum concentration of Lenvatinib can be increased when it is combined with Taurocholic Acid.Experimental
TelaprevirThe metabolism of Lenvatinib can be decreased when combined with Telaprevir.Approved
TelavancinTelavancin may increase the QTc-prolonging activities of Lenvatinib.Approved
TelithromycinTelithromycin may increase the QTc-prolonging activities of Lenvatinib.Approved
TelmisartanThe serum concentration of Lenvatinib can be increased when it is combined with Telmisartan.Approved, Investigational
TemsirolimusThe serum concentration of Lenvatinib can be increased when it is combined with Temsirolimus.Approved
TerazosinThe serum concentration of Lenvatinib can be increased when it is combined with Terazosin.Approved
TerbutalineTerbutaline may increase the QTc-prolonging activities of Lenvatinib.Approved
TerfenadineThe serum concentration of Lenvatinib can be increased when it is combined with Terfenadine.Withdrawn
TeriflunomideThe serum concentration of Lenvatinib can be increased when it is combined with Teriflunomide.Approved
TesmilifeneThe serum concentration of Lenvatinib can be decreased when it is combined with Tesmilifene.Investigational
TestosteroneThe serum concentration of Lenvatinib can be increased when it is combined with Testosterone.Approved, Investigational
TetrabenazineLenvatinib may increase the QTc-prolonging activities of Tetrabenazine.Approved
ThioridazineLenvatinib may increase the QTc-prolonging activities of Thioridazine.Approved
ThiothixeneThiothixene may increase the QTc-prolonging activities of Lenvatinib.Approved
TicagrelorThe serum concentration of Lenvatinib can be increased when it is combined with Ticagrelor.Approved
TiclopidineThe metabolism of Lenvatinib can be decreased when combined with Ticlopidine.Approved
TizanidineTizanidine may increase the QTc-prolonging activities of Lenvatinib.Approved
TocilizumabThe serum concentration of Lenvatinib can be decreased when it is combined with Tocilizumab.Approved
TolterodineTolterodine may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
TolvaptanThe serum concentration of Lenvatinib can be increased when it is combined with Tolvaptan.Approved
ToremifeneLenvatinib may increase the QTc-prolonging activities of Toremifene.Approved, Investigational
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Lenvatinib.Approved, Investigational
TrazodoneTrazodone may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
TreprostinilTreprostinil may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
TrifluoperazineThe serum concentration of Lenvatinib can be increased when it is combined with Trifluoperazine.Approved
TriflupromazineThe serum concentration of Lenvatinib can be increased when it is combined with Triflupromazine.Approved, Vet Approved
TrimethoprimTrimethoprim may increase the QTc-prolonging activities of Lenvatinib.Approved, Vet Approved
TrimipramineTrimipramine may increase the QTc-prolonging activities of Lenvatinib.Approved
TriptorelinTriptorelin may increase the QTc-prolonging activities of Lenvatinib.Approved, Vet Approved
TroleandomycinThe serum concentration of Lenvatinib can be increased when it is combined with Troleandomycin.Approved
VandetanibLenvatinib may increase the QTc-prolonging activities of Vandetanib.Approved
VardenafilVardenafil may increase the QTc-prolonging activities of Lenvatinib.Approved
VemurafenibLenvatinib may increase the QTc-prolonging activities of Vemurafenib.Approved
VenlafaxineVenlafaxine may increase the QTc-prolonging activities of Lenvatinib.Approved
VerapamilThe metabolism of Lenvatinib can be decreased when combined with Verapamil.Approved
VilanterolVilanterol may increase the QTc-prolonging activities of Lenvatinib.Approved
VinblastineThe serum concentration of Lenvatinib can be decreased when it is combined with Vinblastine.Approved
VincristineThe serum concentration of Lenvatinib can be decreased when it is combined with Vincristine.Approved, Investigational
VinorelbineThe serum concentration of Lenvatinib can be increased when it is combined with Vinorelbine.Approved, Investigational
VoriconazoleThe metabolism of Lenvatinib can be decreased when combined with Voriconazole.Approved, Investigational
VorinostatVorinostat may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
ZimelidineThe serum concentration of Lenvatinib can be increased when it is combined with Zimelidine.Withdrawn
ZiprasidoneLenvatinib may increase the QTc-prolonging activities of Ziprasidone.Approved
ZuclopenthixolLenvatinib may increase the QTc-prolonging activities of Zuclopenthixol.Approved, Investigational
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General References
  1. Matsui J, Yamamoto Y, Funahashi Y, Tsuruoka A, Watanabe T, Wakabayashi T, Uenaka T, Asada M: E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition. Int J Cancer. 2008 Feb 1;122(3):664-71. [PubMed:17943726 ]
  2. Glen H, Mason S, Patel H, Macleod K, Brunton VG: E7080, a multi-targeted tyrosine kinase inhibitor suppresses tumor cell migration and invasion. BMC Cancer. 2011 Jul 22;11:309. doi: 10.1186/1471-2407-11-309. [PubMed:21781317 ]
  3. Scott LJ: Lenvatinib: first global approval. Drugs. 2015 Apr;75(5):553-60. doi: 10.1007/s40265-015-0383-0. [PubMed:25795101 ]
  4. Killock D: Neuroendocrine cancer: SELECT-lenvatinib in thyroid cancer. Nat Rev Clin Oncol. 2015 Apr;12(4):189. doi: 10.1038/nrclinonc.2015.30. Epub 2015 Feb 24. [PubMed:25707627 ]
External Links
ATC CodesL01XE29
AHFS Codes
  • 10:00
PDB EntriesNot Available
FDA labelDownload (388 KB)
MSDSNot Available
ADMET
Predicted ADMET featuresNot Available
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
CapsuleOral10 mg
CapsuleOral10 mg/1
CapsuleOral14 mg
CapsuleOral20 mg
CapsuleOral24 mg
CapsuleOral4 mg/1
Kit
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US7253286 No2001-10-192021-10-19Us
US7612208 No2006-09-192026-09-19Us
US9006256 No2007-07-272027-07-27Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
logP3.30FDA Label
pKa5.05FDA Label
Predicted Properties
PropertyValueSource
Water Solubility0.0177 mg/mLALOGPS
logP3.25ALOGPS
logP2.16ChemAxon
logS-4.4ALOGPS
pKa (Strongest Acidic)3.56ChemAxon
pKa (Strongest Basic)6.1ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count7ChemAxon
Hydrogen Donor Count4ChemAxon
Polar Surface Area120.05 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity123.67 m3·mol-1ChemAxon
Polarizability42.74 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
Taxonomy
ClassificationNot classified

Targets

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. Matsui J, Yamamoto Y, Funahashi Y, Tsuruoka A, Watanabe T, Wakabayashi T, Uenaka T, Asada M: E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition. Int J Cancer. 2008 Feb 1;122(3):664-71. [PubMed:17943726 ]
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. Matsui J, Yamamoto Y, Funahashi Y, Tsuruoka A, Watanabe T, Wakabayashi T, Uenaka T, Asada M: E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition. Int J Cancer. 2008 Feb 1;122(3):664-71. [PubMed:17943726 ]
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. Matsui J, Yamamoto Y, Funahashi Y, Tsuruoka A, Watanabe T, Wakabayashi T, Uenaka T, Asada M: E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition. Int J Cancer. 2008 Feb 1;122(3):664-71. [PubMed:17943726 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
Inhibitor
General Function:
Protein tyrosine kinase activity
Specific Function:
Tyrosine-protein kinase that acts as cell-surface receptor for fibroblast growth factors and plays an essential role in the regulation of embryonic development, cell proliferation, differentiation and migration. Required for normal mesoderm patterning and correct axial organization during embryonic development, normal skeletogenesis and normal development of the gonadotropin-releasing hormone (...
Gene Name:
FGFR1
Uniprot ID:
P11362
Molecular Weight:
91866.935 Da
References
  1. Matsui J, Yamamoto Y, Funahashi Y, Tsuruoka A, Watanabe T, Wakabayashi T, Uenaka T, Asada M: E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition. Int J Cancer. 2008 Feb 1;122(3):664-71. [PubMed:17943726 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
Inhibitor
General Function:
Protein tyrosine kinase activity
Specific Function:
Tyrosine-protein kinase that acts as cell-surface receptor for fibroblast growth factors and plays an essential role in the regulation of cell proliferation, differentiation, migration and apoptosis, and in the regulation of embryonic development. Required for normal embryonic patterning, trophoblast function, limb bud development, lung morphogenesis, osteogenesis and skin development. Plays an...
Gene Name:
FGFR2
Uniprot ID:
P21802
Molecular Weight:
92024.29 Da
References
  1. Matsui J, Yamamoto Y, Funahashi Y, Tsuruoka A, Watanabe T, Wakabayashi T, Uenaka T, Asada M: E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition. Int J Cancer. 2008 Feb 1;122(3):664-71. [PubMed:17943726 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
Inhibitor
General Function:
Protein tyrosine kinase activity
Specific Function:
Tyrosine-protein kinase that acts as cell-surface receptor for fibroblast growth factors and plays an essential role in the regulation of cell proliferation, differentiation and apoptosis. Plays an essential role in the regulation of chondrocyte differentiation, proliferation and apoptosis, and is required for normal skeleton development. Regulates both osteogenesis and postnatal bone mineraliz...
Gene Name:
FGFR3
Uniprot ID:
P22607
Molecular Weight:
87708.905 Da
References
  1. Matsui J, Yamamoto Y, Funahashi Y, Tsuruoka A, Watanabe T, Wakabayashi T, Uenaka T, Asada M: E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition. Int J Cancer. 2008 Feb 1;122(3):664-71. [PubMed:17943726 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
Inhibitor
General Function:
Protein tyrosine kinase activity
Specific Function:
Tyrosine-protein kinase that acts as cell-surface receptor for fibroblast growth factors and plays a role in the regulation of cell proliferation, differentiation and migration, and in regulation of lipid metabolism, bile acid biosynthesis, glucose uptake, vitamin D metabolism and phosphate homeostasis. Required for normal down-regulation of the expression of CYP7A1, the rate-limiting enzyme in...
Gene Name:
FGFR4
Uniprot ID:
P22455
Molecular Weight:
87953.535 Da
References
  1. Matsui J, Yamamoto Y, Funahashi Y, Tsuruoka A, Watanabe T, Wakabayashi T, Uenaka T, Asada M: E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition. Int J Cancer. 2008 Feb 1;122(3):664-71. [PubMed:17943726 ]
8. Platelet derived growth factor receptor alpha
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
Inhibitor
References
  1. Matsui J, Yamamoto Y, Funahashi Y, Tsuruoka A, Watanabe T, Wakabayashi T, Uenaka T, Asada M: E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition. Int J Cancer. 2008 Feb 1;122(3):664-71. [PubMed:17943726 ]
9. RET
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
Inhibitor
References
  1. Matsui J, Yamamoto Y, Funahashi Y, Tsuruoka A, Watanabe T, Wakabayashi T, Uenaka T, Asada M: E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition. Int J Cancer. 2008 Feb 1;122(3):664-71. [PubMed:17943726 ]
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. Matsui J, Yamamoto Y, Funahashi Y, Tsuruoka A, Watanabe T, Wakabayashi T, Uenaka T, Asada M: E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition. Int J Cancer. 2008 Feb 1;122(3):664-71. [PubMed:17943726 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
no
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
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrate
General Function:
Xanthine dehydrogenase activity
Specific Function:
Oxidase with broad substrate specificity, oxidizing aromatic azaheterocycles, such as N1-methylnicotinamide and N-methylphthalazinium, as well as aldehydes, such as benzaldehyde, retinal, pyridoxal, and vanillin. Plays a key role in the metabolism of xenobiotics and drugs containing aromatic azaheterocyclic substituents. Participates in the bioactivation of prodrugs such as famciclovir, catalyz...
Gene Name:
AOX1
Uniprot ID:
Q06278
Molecular Weight:
147916.735 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrate
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
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrate
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both from mitochondria to cytosol and from cytosol to extracellular space, and cellular export of hemin, and heme. Xenobiotic transporter that may play an important role in the exclusion of xenobiotics from t...
Gene Name:
ABCG2
Uniprot ID:
Q9UNQ0
Molecular Weight:
72313.47 Da
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Drug created on June 22, 2015 07:20 / Updated on December 06, 2016 02:43