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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
Lenvimacapsule10 mgoralEisai Limited2016-03-31Not applicableCanada
Lenvimacapsule10 mg/1oralEisai Inc.2015-02-13Not applicableUs
Lenvimacapsule24 mgoralEisai Limited2016-03-31Not applicableCanada
LenvimakitEisai Inc.2015-02-13Not applicableUs
Lenvimacapsule20 mgoralEisai Limited2016-03-31Not applicableCanada
Lenvimacapsule10 mg/1oralEisai Inc.2015-02-13Not applicableUs
Lenvimacapsule14 mgoralEisai Limited2016-03-31Not applicableCanada
LenvimakitEisai Inc.2015-02-13Not applicableUs
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
Taxonomy
ClassificationNot classified
Pharmacology
IndicationLenvatinib is indicated for the treatment of patients with locally recurrent or metastatic, progressive, radioactive iodine-refractory differentiated thyroid cancer.
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.
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
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal AbsorptionNot AvailableNot Available
Blood Brain BarrierNot AvailableNot Available
Caco-2 permeableNot AvailableNot Available
P-glycoprotein substrateNot AvailableNot Available
P-glycoprotein inhibitor INot AvailableNot Available
P-glycoprotein inhibitor IINot AvailableNot Available
Renal organic cation transporterNot AvailableNot Available
CYP450 2C9 substrateNot AvailableNot Available
CYP450 2D6 substrateNot AvailableNot Available
CYP450 3A4 substrateNot AvailableNot Available
CYP450 1A2 substrateNot AvailableNot Available
CYP450 2C9 inhibitorNot AvailableNot Available
CYP450 2D6 inhibitorNot AvailableNot Available
CYP450 2C19 inhibitorNot AvailableNot Available
CYP450 3A4 inhibitorNot AvailableNot Available
CYP450 inhibitory promiscuityNot AvailableNot Available
Ames testNot AvailableNot Available
CarcinogenicityNot AvailableNot Available
BiodegradationNot AvailableNot Available
Rat acute toxicityNot AvailableNot applicable
hERG inhibition (predictor I)Not AvailableNot Available
hERG inhibition (predictor II)Not AvailableNot Available
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Capsuleoral10 mg/1
Capsuleoral10 mg
Capsuleoral14 mg
Capsuleoral20 mg
Capsuleoral24 mg
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
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
Interactions
Drug Interactions
Drug
AcetaminophenThe serum concentration of Lenvatinib can be increased when it is combined with Acetaminophen.
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Lenvatinib.
AfatinibThe serum concentration of Lenvatinib can be increased when it is combined with Afatinib.
AlbendazoleThe serum concentration of Lenvatinib can be increased when it is combined with Albendazole.
AldosteroneThe serum concentration of Lenvatinib can be decreased when it is combined with Aldosterone.
AlectinibThe serum concentration of Lenvatinib can be increased when it is combined with Alectinib.
AlfentanilThe serum concentration of Lenvatinib can be increased when it is combined with Alfentanil.
AlfuzosinAlfuzosin may increase the QTc-prolonging activities of Lenvatinib.
AmantadineAmantadine may increase the QTc-prolonging activities of Lenvatinib.
Aminohippuric acidThe serum concentration of Lenvatinib can be increased when it is combined with Aminohippuric acid.
AmiodaroneLenvatinib may increase the QTc-prolonging activities of Amiodarone.
AmiodaroneThe serum concentration of Lenvatinib can be decreased when it is combined with Amiodarone.
AmitriptylineAmitriptyline may increase the QTc-prolonging activities of Lenvatinib.
AmlodipineThe serum concentration of Lenvatinib can be increased when it is combined with Amlodipine.
AmoxapineAmoxapine may increase the QTc-prolonging activities of Lenvatinib.
AmprenavirThe serum concentration of Lenvatinib can be decreased when it is combined with Amprenavir.
AmsacrineThe serum concentration of Lenvatinib can be increased when it is combined with Amsacrine.
AnagrelideLenvatinib may increase the QTc-prolonging activities of Anagrelide.
ApomorphineApomorphine may increase the QTc-prolonging activities of Lenvatinib.
AprepitantThe serum concentration of Lenvatinib can be increased when it is combined with Aprepitant.
ArformoterolArformoterol may increase the QTc-prolonging activities of Lenvatinib.
AripiprazoleAripiprazole may increase the QTc-prolonging activities of Lenvatinib.
Arsenic trioxideLenvatinib may increase the QTc-prolonging activities of Arsenic trioxide.
ArtemetherLenvatinib may increase the QTc-prolonging activities of Artemether.
AsenapineLenvatinib may increase the QTc-prolonging activities of Asenapine.
AstemizoleThe serum concentration of Lenvatinib can be increased when it is combined with Astemizole.
AtazanavirAtazanavir may increase the QTc-prolonging activities of Lenvatinib.
AtenololThe serum concentration of Lenvatinib can be increased when it is combined with Atenolol.
AtomoxetineAtomoxetine may increase the QTc-prolonging activities of Lenvatinib.
AtorvastatinThe serum concentration of Lenvatinib can be increased when it is combined with Atorvastatin.
AzelastineThe serum concentration of Lenvatinib can be increased when it is combined with Azelastine.
AzithromycinLenvatinib may increase the QTc-prolonging activities of Azithromycin.
AzithromycinThe serum concentration of Lenvatinib can be increased when it is combined with Azithromycin.
BedaquilineBedaquiline may increase the QTc-prolonging activities of Lenvatinib.
BenzocaineThe serum concentration of Lenvatinib can be increased when it is combined with Benzocaine.
BepridilThe serum concentration of Lenvatinib can be increased when it is combined with Bepridil.
BevacizumabBevacizumab may increase the cardiotoxic activities of Lenvatinib.
BexaroteneThe serum concentration of Lenvatinib can be decreased when it is combined with Bexarotene.
BiperidenThe serum concentration of Lenvatinib can be increased when it is combined with Biperiden.
BoceprevirThe metabolism of Lenvatinib can be decreased when combined with Boceprevir.
BortezomibBortezomib may increase the QTc-prolonging activities of Lenvatinib.
BosentanThe serum concentration of Lenvatinib can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Lenvatinib can be increased when it is combined with Bosutinib.
BromocriptineThe serum concentration of Lenvatinib can be increased when it is combined with Bromocriptine.
BuprenorphineThe serum concentration of Lenvatinib can be increased when it is combined with Buprenorphine.
BuserelinBuserelin may increase the QTc-prolonging activities of Lenvatinib.
BuspironeThe serum concentration of Lenvatinib can be increased when it is combined with Buspirone.
CabazitaxelThe serum concentration of Lenvatinib can be increased when it is combined with Cabazitaxel.
CaffeineThe serum concentration of Lenvatinib can be increased when it is combined with Caffeine.
CanagliflozinThe serum concentration of Lenvatinib can be increased when it is combined with Canagliflozin.
CandesartanThe serum concentration of Lenvatinib can be increased when it is combined with Candesartan.
CaptoprilThe serum concentration of Lenvatinib can be increased when it is combined with Captopril.
CarbamazepineThe serum concentration of Lenvatinib can be decreased when it is combined with Carbamazepine.
CarvedilolThe serum concentration of Lenvatinib can be increased when it is combined with Carvedilol.
CaspofunginThe serum concentration of Lenvatinib can be increased when it is combined with Caspofungin.
CeritinibThe serum concentration of Lenvatinib can be increased when it is combined with Ceritinib.
CeritinibLenvatinib may increase the QTc-prolonging activities of Ceritinib.
ChloroquineLenvatinib may increase the QTc-prolonging activities of Chloroquine.
ChloroquineThe serum concentration of Lenvatinib can be increased when it is combined with Chloroquine.
ChlorpromazineLenvatinib may increase the QTc-prolonging activities of Chlorpromazine.
ChlorpromazineThe serum concentration of Lenvatinib can be increased when it is combined with Chlorpromazine.
ChlorpropamideThe serum concentration of Lenvatinib can be increased when it is combined with Chlorpropamide.
ChlorprothixeneThe serum concentration of Lenvatinib can be increased when it is combined with Chlorprothixene.
CholesterolThe serum concentration of Lenvatinib can be increased when it is combined with Cholesterol.
Cholic AcidThe serum concentration of Lenvatinib can be decreased when it is combined with Cholic Acid.
CilazaprilThe serum concentration of Lenvatinib can be increased when it is combined with Cilazapril.
CimetidineThe serum concentration of Lenvatinib can be decreased when it is combined with Cimetidine.
CiprofloxacinLenvatinib may increase the QTc-prolonging activities of Ciprofloxacin.
CiprofloxacinThe serum concentration of Lenvatinib can be increased when it is combined with Ciprofloxacin.
CisaprideLenvatinib may increase the QTc-prolonging activities of Cisapride.
CitalopramLenvatinib may increase the QTc-prolonging activities of Citalopram.
CitalopramThe serum concentration of Lenvatinib can be increased when it is combined with Citalopram.
ClarithromycinLenvatinib may increase the QTc-prolonging activities of Clarithromycin.
ClarithromycinThe serum concentration of Lenvatinib can be increased when it is combined with Clarithromycin.
ClemastineThe metabolism of Lenvatinib can be decreased when combined with Clemastine.
ClofazimineThe serum concentration of Lenvatinib can be increased when it is combined with Clofazimine.
ClomipramineClomipramine may increase the QTc-prolonging activities of Lenvatinib.
ClotrimazoleThe metabolism of Lenvatinib can be decreased when combined with Clotrimazole.
ClozapineClozapine may increase the QTc-prolonging activities of Lenvatinib.
CobicistatThe serum concentration of Lenvatinib can be increased when it is combined with Cobicistat.
ColchicineThe serum concentration of Lenvatinib can be increased when it is combined with Colchicine.
ColforsinThe serum concentration of Lenvatinib can be increased when it is combined with Colforsin.
ConivaptanThe serum concentration of Lenvatinib can be increased when it is combined with Conivaptan.
CrizotinibLenvatinib may increase the QTc-prolonging activities of Crizotinib.
CrizotinibThe metabolism of Lenvatinib can be decreased when combined with Crizotinib.
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Lenvatinib.
CyclosporineThe metabolism of Lenvatinib can be decreased when combined with Cyclosporine.
DabrafenibDabrafenib may increase the QTc-prolonging activities of Lenvatinib.
DaclatasvirThe serum concentration of Lenvatinib can be increased when it is combined with Daclatasvir.
DactinomycinThe serum concentration of Lenvatinib can be increased when it is combined with Dactinomycin.
DarunavirThe metabolism of Lenvatinib can be decreased when combined with Darunavir.
DasatinibThe serum concentration of Lenvatinib can be increased when it is combined with Dasatinib.
DaunorubicinThe serum concentration of Lenvatinib can be decreased when it is combined with Daunorubicin.
DeferasiroxThe serum concentration of Lenvatinib can be decreased when it is combined with Deferasirox.
DegarelixDegarelix may increase the QTc-prolonging activities of Lenvatinib.
DelavirdineThe metabolism of Lenvatinib can be decreased when combined with Delavirdine.
DesfluraneDesflurane may increase the QTc-prolonging activities of Lenvatinib.
DesipramineDesipramine may increase the QTc-prolonging activities of Lenvatinib.
DeslanosideDeslanoside may decrease the cardiotoxic activities of Lenvatinib.
DesloratadineThe serum concentration of Lenvatinib can be increased when it is combined with Desloratadine.
DexamethasoneThe serum concentration of Lenvatinib can be decreased when it is combined with Dexamethasone.
DextromethorphanThe serum concentration of Lenvatinib can be increased when it is combined with Dextromethorphan.
DiclofenacThe serum concentration of Lenvatinib can be increased when it is combined with Diclofenac.
DigitoxinDigitoxin may decrease the cardiotoxic activities of Lenvatinib.
DigoxinDigoxin may decrease the cardiotoxic activities of Lenvatinib.
DihydroergotamineThe metabolism of Lenvatinib can be decreased when combined with Dihydroergotamine.
DiltiazemThe metabolism of Lenvatinib can be decreased when combined with Diltiazem.
DiphenhydramineDiphenhydramine may increase the QTc-prolonging activities of Lenvatinib.
DipyridamoleThe serum concentration of Lenvatinib can be increased when it is combined with Dipyridamole.
DisopyramideLenvatinib may increase the QTc-prolonging activities of Disopyramide.
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Lenvatinib.
DofetilideLenvatinib may increase the QTc-prolonging activities of Dofetilide.
DolasetronDolasetron may increase the QTc-prolonging activities of Lenvatinib.
DomperidoneLenvatinib may increase the QTc-prolonging activities of Domperidone.
DoxazosinThe serum concentration of Lenvatinib can be increased when it is combined with Doxazosin.
DoxepinDoxepin may increase the QTc-prolonging activities of Lenvatinib.
DoxorubicinThe serum concentration of Lenvatinib can be decreased when it is combined with Doxorubicin.
DoxycyclineThe metabolism of Lenvatinib can be decreased when combined with Doxycycline.
DronabinolThe serum concentration of Lenvatinib can be increased when it is combined with Dronabinol.
DronedaroneLenvatinib may increase the QTc-prolonging activities of Dronedarone.
DronedaroneThe metabolism of Lenvatinib can be decreased when combined with Dronedarone.
DroperidolDroperidol may increase the QTc-prolonging activities of Lenvatinib.
EfavirenzThe serum concentration of Lenvatinib can be decreased when it is combined with Efavirenz.
ElbasvirThe serum concentration of Lenvatinib can be increased when it is combined with Elbasvir.
EliglustatLenvatinib may increase the QTc-prolonging activities of Eliglustat.
EltrombopagThe serum concentration of Lenvatinib can be increased when it is combined with Eltrombopag.
EnalaprilThe serum concentration of Lenvatinib can be increased when it is combined with Enalapril.
EnzalutamideThe serum concentration of Lenvatinib can be increased when it is combined with Enzalutamide.
ErgonovineThe serum concentration of Lenvatinib can be increased when it is combined with Ergonovine.
ErgotamineThe serum concentration of Lenvatinib can be increased when it is combined with Ergotamine.
EribulinEribulin may increase the QTc-prolonging activities of Lenvatinib.
ErythromycinLenvatinib may increase the QTc-prolonging activities of Erythromycin.
ErythromycinThe metabolism of Lenvatinib can be decreased when combined with Erythromycin.
EscitalopramLenvatinib may increase the QTc-prolonging activities of Escitalopram.
Eslicarbazepine acetateThe serum concentration of Lenvatinib can be decreased when it is combined with Eslicarbazepine acetate.
EstramustineThe serum concentration of Lenvatinib can be increased when it is combined with Estramustine.
EstriolThe serum concentration of Lenvatinib can be decreased when it is combined with Estriol.
EstroneThe serum concentration of Lenvatinib can be decreased when it is combined with Estrone.
EtoposideThe serum concentration of Lenvatinib can be increased when it is combined with Etoposide.
EtravirineThe serum concentration of Lenvatinib can be decreased when it is combined with Etravirine.
EzogabineEzogabine may increase the QTc-prolonging activities of Lenvatinib.
FamotidineFamotidine may increase the QTc-prolonging activities of Lenvatinib.
FelbamateFelbamate may increase the QTc-prolonging activities of Lenvatinib.
FelodipineThe serum concentration of Lenvatinib can be increased when it is combined with Felodipine.
FentanylThe serum concentration of Lenvatinib can be increased when it is combined with Fentanyl.
FexofenadineThe serum concentration of Lenvatinib can be increased when it is combined with Fexofenadine.
FidaxomicinThe serum concentration of Lenvatinib can be increased when it is combined with Fidaxomicin.
FingolimodFingolimod may increase the QTc-prolonging activities of Lenvatinib.
FlecainideFlecainide may increase the QTc-prolonging activities of Lenvatinib.
FluconazoleFluconazole may increase the QTc-prolonging activities of Lenvatinib.
FluoxetineLenvatinib may increase the QTc-prolonging activities of Fluoxetine.
FluoxetineThe serum concentration of Lenvatinib can be increased when it is combined with Fluoxetine.
FlupentixolLenvatinib may increase the QTc-prolonging activities of Flupentixol.
FlupentixolThe serum concentration of Lenvatinib can be increased when it is combined with Flupentixol.
FluphenazineThe serum concentration of Lenvatinib can be increased when it is combined with Fluphenazine.
FlurazepamThe serum concentration of Lenvatinib can be increased when it is combined with Flurazepam.
FluvoxamineThe metabolism of Lenvatinib can be decreased when combined with Fluvoxamine.
FormoterolFormoterol may increase the QTc-prolonging activities of Lenvatinib.
FosamprenavirThe metabolism of Lenvatinib can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Lenvatinib can be increased when it is combined with Fosaprepitant.
FoscarnetFoscarnet may increase the QTc-prolonging activities of Lenvatinib.
FosphenytoinThe metabolism of Lenvatinib can be increased when combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Lenvatinib can be increased when it is combined with Fusidic Acid.
Gadobenic acidGadobenic acid may increase the QTc-prolonging activities of Lenvatinib.
GalantamineGalantamine may increase the QTc-prolonging activities of Lenvatinib.
GefitinibThe serum concentration of Lenvatinib can be increased when it is combined with Gefitinib.
GemifloxacinGemifloxacin may increase the QTc-prolonging activities of Lenvatinib.
GenisteinThe serum concentration of Lenvatinib can be increased when it is combined with Genistein.
GlyburideThe serum concentration of Lenvatinib can be increased when it is combined with Glyburide.
GlycerolThe serum concentration of Lenvatinib can be increased when it is combined with Glycerol.
GoserelinGoserelin may increase the QTc-prolonging activities of Lenvatinib.
Gramicidin DThe serum concentration of Lenvatinib can be increased when it is combined with Gramicidin D.
GranisetronGranisetron may increase the QTc-prolonging activities of Lenvatinib.
GrepafloxacinThe serum concentration of Lenvatinib can be increased when it is combined with Grepafloxacin.
HaloperidolLenvatinib may increase the QTc-prolonging activities of Haloperidol.
HaloperidolThe serum concentration of Lenvatinib can be increased when it is combined with Haloperidol.
HistrelinHistrelin may increase the QTc-prolonging activities of Lenvatinib.
HydrocortisoneThe serum concentration of Lenvatinib can be increased when it is combined with Hydrocortisone.
HydroxyzineHydroxyzine may increase the QTc-prolonging activities of Lenvatinib.
IbandronateIbandronate may increase the QTc-prolonging activities of Lenvatinib.
IbutilideLenvatinib may increase the QTc-prolonging activities of Ibutilide.
IdelalisibThe serum concentration of Lenvatinib can be increased when it is combined with Idelalisib.
IloperidoneLenvatinib may increase the QTc-prolonging activities of Iloperidone.
ImatinibThe metabolism of Lenvatinib can be decreased when combined with Imatinib.
ImipramineImipramine may increase the QTc-prolonging activities of Lenvatinib.
IndacaterolIndacaterol may increase the QTc-prolonging activities of Lenvatinib.
IndapamideIndapamide may increase the QTc-prolonging activities of Lenvatinib.
IndinavirThe serum concentration of Lenvatinib can be decreased when it is combined with Indinavir.
IndomethacinThe serum concentration of Lenvatinib can be increased when it is combined with Indomethacin.
IsavuconazoniumThe metabolism of Lenvatinib can be decreased when combined with Isavuconazonium.
IsofluraneIsoflurane may increase the QTc-prolonging activities of Lenvatinib.
IsradipineIsradipine may increase the QTc-prolonging activities of Lenvatinib.
ItraconazoleItraconazole may increase the QTc-prolonging activities of Lenvatinib.
IvabradineIvabradine may increase the QTc-prolonging activities of Lenvatinib.
IvacaftorThe serum concentration of Lenvatinib can be increased when it is combined with Ivacaftor.
IvermectinThe serum concentration of Lenvatinib can be increased when it is combined with Ivermectin.
KetamineThe serum concentration of Lenvatinib can be increased when it is combined with Ketamine.
KetoconazoleKetoconazole may increase the QTc-prolonging activities of Lenvatinib.
LansoprazoleThe serum concentration of Lenvatinib can be increased when it is combined with Lansoprazole.
LapatinibLapatinib may increase the QTc-prolonging activities of Lenvatinib.
LeuprolideLeuprolide may increase the QTc-prolonging activities of Lenvatinib.
LevofloxacinLenvatinib may increase the QTc-prolonging activities of Levofloxacin.
LevofloxacinThe serum concentration of Lenvatinib can be increased when it is combined with Levofloxacin.
LevothyroxineThe serum concentration of Lenvatinib can be decreased when it is combined with Levothyroxine.
LidocaineThe serum concentration of Lenvatinib can be increased when it is combined with Lidocaine.
LiothyronineThe serum concentration of Lenvatinib can be decreased when it is combined with Liothyronine.
LiotrixThe serum concentration of Lenvatinib can be decreased when it is combined with Liotrix.
LisinoprilThe serum concentration of Lenvatinib can be increased when it is combined with Lisinopril.
LithiumLithium may increase the QTc-prolonging activities of Lenvatinib.
LomitapideThe serum concentration of Lenvatinib can be increased when it is combined with Lomitapide.
LoperamideThe serum concentration of Lenvatinib can be increased when it is combined with Loperamide.
LopinavirLenvatinib may increase the QTc-prolonging activities of Lopinavir.
LopinavirThe serum concentration of Lenvatinib can be increased when it is combined with Lopinavir.
LoratadineThe serum concentration of Lenvatinib can be increased when it is combined with Loratadine.
LosartanThe serum concentration of Lenvatinib can be increased when it is combined with Losartan.
LovastatinThe metabolism of Lenvatinib can be decreased when combined with Lovastatin.
LuliconazoleThe serum concentration of Lenvatinib can be increased when it is combined with Luliconazole.
LumacaftorThe serum concentration of Lenvatinib can be decreased when it is combined with Lumacaftor.
LumefantrineLenvatinib may increase the QTc-prolonging activities of Lumefantrine.
MaprotilineMaprotiline may increase the QTc-prolonging activities of Lenvatinib.
MebendazoleThe serum concentration of Lenvatinib can be increased when it is combined with Mebendazole.
MefloquineMefloquine may increase the QTc-prolonging activities of Lenvatinib.
Megestrol acetateThe serum concentration of Lenvatinib can be increased when it is combined with Megestrol acetate.
MeprobamateThe serum concentration of Lenvatinib can be increased when it is combined with Meprobamate.
MethadoneLenvatinib may increase the QTc-prolonging activities of Methadone.
MethadoneThe serum concentration of Lenvatinib can be increased when it is combined with Methadone.
MethotrimeprazineMethotrimeprazine may increase the QTc-prolonging activities of Lenvatinib.
MetoclopramideMetoclopramide may increase the QTc-prolonging activities of Lenvatinib.
MetoprololThe serum concentration of Lenvatinib can be increased when it is combined with Metoprolol.
MetronidazoleMetronidazole may increase the QTc-prolonging activities of Lenvatinib.
MibefradilThe serum concentration of Lenvatinib can be increased when it is combined with Mibefradil.
MiconazoleThe serum concentration of Lenvatinib can be increased when it is combined with Miconazole.
MidazolamThe serum concentration of Lenvatinib can be decreased when it is combined with Midazolam.
MifepristoneMifepristone may increase the QTc-prolonging activities of Lenvatinib.
MirabegronMirabegron may increase the QTc-prolonging activities of Lenvatinib.
MirtazapineMirtazapine may increase the QTc-prolonging activities of Lenvatinib.
MitomycinThe serum concentration of Lenvatinib can be increased when it is combined with Mitomycin.
MitotaneThe serum concentration of Lenvatinib can be decreased when it is combined with Mitotane.
MitoxantroneThe serum concentration of Lenvatinib can be decreased when it is combined with Mitoxantrone.
ModafinilThe serum concentration of Lenvatinib can be decreased when it is combined with Modafinil.
MoexiprilMoexipril may increase the QTc-prolonging activities of Lenvatinib.
MorphineThe serum concentration of Lenvatinib can be increased when it is combined with Morphine.
MoxifloxacinMoxifloxacin may increase the QTc-prolonging activities of Lenvatinib.
NafcillinThe serum concentration of Lenvatinib can be decreased when it is combined with Nafcillin.
NaltrexoneThe serum concentration of Lenvatinib can be increased when it is combined with Naltrexone.
NaringeninThe serum concentration of Lenvatinib can be increased when it is combined with Naringenin.
NefazodoneThe serum concentration of Lenvatinib can be decreased when it is combined with Nefazodone.
NelfinavirNelfinavir may increase the QTc-prolonging activities of Lenvatinib.
NeostigmineThe serum concentration of Lenvatinib can be increased when it is combined with Neostigmine.
NetupitantThe serum concentration of Lenvatinib can be increased when it is combined with Netupitant.
NevirapineThe metabolism of Lenvatinib can be decreased when combined with Nevirapine.
NicardipineNicardipine may increase the QTc-prolonging activities of Lenvatinib.
NifedipineThe serum concentration of Lenvatinib can be decreased when it is combined with Nifedipine.
NilotinibLenvatinib may increase the QTc-prolonging activities of Nilotinib.
NilotinibThe metabolism of Lenvatinib can be decreased when combined with Nilotinib.
NisoldipineThe serum concentration of Lenvatinib can be increased when it is combined with Nisoldipine.
NitrazepamThe serum concentration of Lenvatinib can be increased when it is combined with Nitrazepam.
NitrendipineThe serum concentration of Lenvatinib can be increased when it is combined with Nitrendipine.
NorethisteroneThe serum concentration of Lenvatinib can be decreased when it is combined with Norethisterone.
NorfloxacinNorfloxacin may increase the QTc-prolonging activities of Lenvatinib.
NortriptylineNortriptyline may increase the QTc-prolonging activities of Lenvatinib.
OctreotideOctreotide may increase the QTc-prolonging activities of Lenvatinib.
OfloxacinOfloxacin may increase the QTc-prolonging activities of Lenvatinib.
OlanzapineOlanzapine may increase the QTc-prolonging activities of Lenvatinib.
OlaparibThe metabolism of Lenvatinib can be decreased when combined with Olaparib.
OlodaterolOlodaterol may increase the QTc-prolonging activities of Lenvatinib.
OmeprazoleThe serum concentration of Lenvatinib can be increased when it is combined with Omeprazole.
OndansetronOndansetron may increase the QTc-prolonging activities of Lenvatinib.
OsimertinibThe serum concentration of Lenvatinib can be increased when it is combined with Osimertinib.
OuabainOuabain may decrease the cardiotoxic activities of Lenvatinib.
OxytocinOxytocin may increase the QTc-prolonging activities of Lenvatinib.
P-NitrophenolThe serum concentration of Lenvatinib can be increased when it is combined with P-Nitrophenol.
PaclitaxelThe serum concentration of Lenvatinib can be increased when it is combined with Paclitaxel.
PalbociclibThe serum concentration of Lenvatinib can be increased when it is combined with Palbociclib.
PaliperidoneLenvatinib may increase the QTc-prolonging activities of Paliperidone.
Palmitic AcidThe serum concentration of Lenvatinib can be increased when it is combined with Palmitic Acid.
PanobinostatPanobinostat may increase the QTc-prolonging activities of Lenvatinib.
PantoprazoleThe serum concentration of Lenvatinib can be increased when it is combined with Pantoprazole.
ParoxetineParoxetine may increase the QTc-prolonging activities of Lenvatinib.
PasireotidePasireotide may increase the QTc-prolonging activities of Lenvatinib.
PazopanibPazopanib may increase the QTc-prolonging activities of Lenvatinib.
PentamidinePentamidine may increase the QTc-prolonging activities of Lenvatinib.
PentobarbitalThe metabolism of Lenvatinib can be increased when combined with Pentobarbital.
PerflutrenPerflutren may increase the QTc-prolonging activities of Lenvatinib.
PerindoprilThe serum concentration of Lenvatinib can be increased when it is combined with Perindopril.
PhenobarbitalThe serum concentration of Lenvatinib can be decreased when it is combined with Phenobarbital.
PhenytoinThe metabolism of Lenvatinib can be increased when combined with Phenytoin.
PimozideLenvatinib may increase the QTc-prolonging activities of Pimozide.
PimozideThe serum concentration of Lenvatinib can be increased when it is combined with Pimozide.
Platelet Activating FactorThe serum concentration of Lenvatinib can be decreased when it is combined with Platelet Activating Factor.
PonatinibThe serum concentration of Lenvatinib can be increased when it is combined with Ponatinib.
PosaconazolePosaconazole may increase the QTc-prolonging activities of Lenvatinib.
PravastatinThe serum concentration of Lenvatinib can be increased when it is combined with Pravastatin.
PrazosinThe serum concentration of Lenvatinib can be increased when it is combined with Prazosin.
PrednisoneThe serum concentration of Lenvatinib can be increased when it is combined with Prednisone.
PrimaquinePrimaquine may increase the QTc-prolonging activities of Lenvatinib.
PrimidoneThe metabolism of Lenvatinib can be increased when combined with Primidone.
ProbenecidThe serum concentration of Lenvatinib can be increased when it is combined with Probenecid.
ProcainamideLenvatinib may increase the QTc-prolonging activities of Procainamide.
ProgesteroneThe serum concentration of Lenvatinib can be decreased when it is combined with Progesterone.
PromazinePromazine may increase the QTc-prolonging activities of Lenvatinib.
PromethazinePromethazine may increase the QTc-prolonging activities of Lenvatinib.
PropafenoneLenvatinib may increase the QTc-prolonging activities of Propafenone.
PropafenoneThe serum concentration of Lenvatinib can be increased when it is combined with Propafenone.
PropofolPropofol may increase the QTc-prolonging activities of Lenvatinib.
PropranololThe serum concentration of Lenvatinib can be increased when it is combined with Propranolol.
ProtriptylineProtriptyline may increase the QTc-prolonging activities of Lenvatinib.
QuercetinThe serum concentration of Lenvatinib can be increased when it is combined with Quercetin.
QuetiapineLenvatinib may increase the QTc-prolonging activities of Quetiapine.
QuinacrineThe serum concentration of Lenvatinib can be increased when it is combined with Quinacrine.
QuinidineLenvatinib may increase the QTc-prolonging activities of Quinidine.
QuinidineThe serum concentration of Lenvatinib can be increased when it is combined with Quinidine.
QuinineLenvatinib may increase the QTc-prolonging activities of Quinine.
QuinineThe serum concentration of Lenvatinib can be increased when it is combined with Quinine.
RanitidineThe serum concentration of Lenvatinib can be increased when it is combined with Ranitidine.
RanolazineThe serum concentration of Lenvatinib can be increased when it is combined with Ranolazine.
ReboxetineThe serum concentration of Lenvatinib can be increased when it is combined with Reboxetine.
RegorafenibThe serum concentration of Lenvatinib can be increased when it is combined with Regorafenib.
ReserpineThe serum concentration of Lenvatinib can be decreased when it is combined with Reserpine.
RifabutinThe metabolism of Lenvatinib can be increased when combined with Rifabutin.
RifampicinThe serum concentration of Lenvatinib can be decreased when it is combined with Rifampicin.
RifapentineThe metabolism of Lenvatinib can be increased when combined with Rifapentine.
RilpivirineRilpivirine may increase the QTc-prolonging activities of Lenvatinib.
RisperidoneRisperidone may increase the QTc-prolonging activities of Lenvatinib.
RitonavirRitonavir may increase the QTc-prolonging activities of Lenvatinib.
RolapitantThe serum concentration of Lenvatinib can be increased when it is combined with Rolapitant.
SalbutamolSalbutamol may increase the QTc-prolonging activities of Lenvatinib.
SalmeterolSalmeterol may increase the QTc-prolonging activities of Lenvatinib.
SaquinavirLenvatinib may increase the QTc-prolonging activities of Saquinavir.
SaquinavirThe serum concentration of Lenvatinib can be decreased when it is combined with Saquinavir.
ScopolamineThe serum concentration of Lenvatinib can be increased when it is combined with Scopolamine.
SelegilineThe serum concentration of Lenvatinib can be increased when it is combined with Selegiline.
SertralineSertraline may increase the QTc-prolonging activities of Lenvatinib.
SevofluraneSevoflurane may increase the QTc-prolonging activities of Lenvatinib.
SildenafilThe metabolism of Lenvatinib can be decreased when combined with Sildenafil.
SiltuximabThe serum concentration of Lenvatinib can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Lenvatinib can be increased when it is combined with Simeprevir.
SimvastatinThe serum concentration of Lenvatinib can be increased when it is combined with Simvastatin.
SirolimusThe serum concentration of Lenvatinib can be decreased when it is combined with Sirolimus.
SolifenacinSolifenacin may increase the QTc-prolonging activities of Lenvatinib.
SorafenibSorafenib may increase the QTc-prolonging activities of Lenvatinib.
SotalolLenvatinib may increase the QTc-prolonging activities of Sotalol.
SpironolactoneThe serum concentration of Lenvatinib can be increased when it is combined with Spironolactone.
St. John's WortThe serum concentration of Lenvatinib can be decreased when it is combined with St. John's Wort.
StaurosporineThe serum concentration of Lenvatinib can be increased when it is combined with Staurosporine.
StiripentolThe serum concentration of Lenvatinib can be increased when it is combined with Stiripentol.
StreptozocinThe serum concentration of Lenvatinib can be decreased when it is combined with Streptozocin.
SulfamethoxazoleSulfamethoxazole may increase the QTc-prolonging activities of Lenvatinib.
SulfinpyrazoneThe serum concentration of Lenvatinib can be increased when it is combined with Sulfinpyrazone.
SulfisoxazoleLenvatinib may increase the QTc-prolonging activities of Sulfisoxazole.
SulfisoxazoleThe metabolism of Lenvatinib can be decreased when combined with Sulfisoxazole.
SumatriptanThe serum concentration of Lenvatinib can be increased when it is combined with Sumatriptan.
SunitinibSunitinib may increase the QTc-prolonging activities of Lenvatinib.
TacrineThe serum concentration of Lenvatinib can be increased when it is combined with Tacrine.
TacrolimusThe serum concentration of Lenvatinib can be decreased when it is combined with Tacrolimus.
TamoxifenTamoxifen may increase the QTc-prolonging activities of Lenvatinib.
Taurocholic AcidThe serum concentration of Lenvatinib can be increased when it is combined with Taurocholic Acid.
TelaprevirThe metabolism of Lenvatinib can be decreased when combined with Telaprevir.
TelavancinTelavancin may increase the QTc-prolonging activities of Lenvatinib.
TelithromycinTelithromycin may increase the QTc-prolonging activities of Lenvatinib.
TelmisartanThe serum concentration of Lenvatinib can be increased when it is combined with Telmisartan.
TemsirolimusThe serum concentration of Lenvatinib can be increased when it is combined with Temsirolimus.
TerazosinThe serum concentration of Lenvatinib can be increased when it is combined with Terazosin.
TerbutalineTerbutaline may increase the QTc-prolonging activities of Lenvatinib.
TerfenadineThe serum concentration of Lenvatinib can be increased when it is combined with Terfenadine.
TeriflunomideThe serum concentration of Lenvatinib can be increased when it is combined with Teriflunomide.
TesmilifeneThe serum concentration of Lenvatinib can be decreased when it is combined with Tesmilifene.
TestosteroneThe serum concentration of Lenvatinib can be increased when it is combined with Testosterone.
TetrabenazineLenvatinib may increase the QTc-prolonging activities of Tetrabenazine.
ThioridazineLenvatinib may increase the QTc-prolonging activities of Thioridazine.
ThiothixeneThiothixene may increase the QTc-prolonging activities of Lenvatinib.
TicagrelorThe serum concentration of Lenvatinib can be increased when it is combined with Ticagrelor.
TiclopidineThe metabolism of Lenvatinib can be decreased when combined with Ticlopidine.
TizanidineTizanidine may increase the QTc-prolonging activities of Lenvatinib.
TocilizumabThe serum concentration of Lenvatinib can be decreased when it is combined with Tocilizumab.
TolterodineTolterodine may increase the QTc-prolonging activities of Lenvatinib.
TolvaptanThe serum concentration of Lenvatinib can be increased when it is combined with Tolvaptan.
ToremifeneLenvatinib may increase the QTc-prolonging activities of Toremifene.
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Lenvatinib.
TrazodoneTrazodone may increase the QTc-prolonging activities of Lenvatinib.
TreprostinilTreprostinil may increase the QTc-prolonging activities of Lenvatinib.
TrifluoperazineThe serum concentration of Lenvatinib can be increased when it is combined with Trifluoperazine.
TriflupromazineThe serum concentration of Lenvatinib can be increased when it is combined with Triflupromazine.
TrimethoprimTrimethoprim may increase the QTc-prolonging activities of Lenvatinib.
TrimipramineTrimipramine may increase the QTc-prolonging activities of Lenvatinib.
TriptorelinTriptorelin may increase the QTc-prolonging activities of Lenvatinib.
TroleandomycinThe serum concentration of Lenvatinib can be increased when it is combined with Troleandomycin.
VandetanibLenvatinib may increase the QTc-prolonging activities of Vandetanib.
VardenafilVardenafil may increase the QTc-prolonging activities of Lenvatinib.
VemurafenibLenvatinib may increase the QTc-prolonging activities of Vemurafenib.
VenlafaxineVenlafaxine may increase the QTc-prolonging activities of Lenvatinib.
VerapamilThe metabolism of Lenvatinib can be decreased when combined with Verapamil.
VilanterolVilanterol may increase the QTc-prolonging activities of Lenvatinib.
VinblastineThe serum concentration of Lenvatinib can be decreased when it is combined with Vinblastine.
VincristineThe serum concentration of Lenvatinib can be decreased when it is combined with Vincristine.
VinorelbineThe serum concentration of Lenvatinib can be increased when it is combined with Vinorelbine.
VoriconazoleVoriconazole may increase the QTc-prolonging activities of Lenvatinib.
VorinostatVorinostat may increase the QTc-prolonging activities of Lenvatinib.
ZimelidineThe serum concentration of Lenvatinib can be increased when it is combined with Zimelidine.
ZiprasidoneLenvatinib may increase the QTc-prolonging activities of Ziprasidone.
ZiprasidoneThe metabolism of Lenvatinib can be decreased when combined with Ziprasidone.
ZuclopenthixolLenvatinib may increase the QTc-prolonging activities of Zuclopenthixol.
Food InteractionsNot Available

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
Comments
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Drug created on June 22, 2015 07:20 / Updated on September 27, 2016 02:28