Identification

Name
Lenvatinib
Accession Number
DB09078
Type
Small Molecule
Groups
Approved
Description

Lenvatinib 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 IDs
E 7080 / E-7080 / E7080 / ER-203492-00 / UNII-EE083865G2
Product Ingredients
IngredientUNIICASInChI Key
Lenvatinib MesylateNot AvailableNot AvailableNot applicable
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
LenvimaCapsule14 mgOralEisai Limited2016-03-31Not applicableCanada
LenvimaCapsule10 mg/1OralEisai Limited2015-02-13Not applicableUs
LenvimaKitEisai Limited2015-02-13Not applicableUs
LenvimaCapsule18 mgOralEisai LimitedNot applicableNot applicableCanada
LenvimaCapsule24 mgOralEisai Limited2016-03-31Not applicableCanada
LenvimaCapsule10 mgOralEisai Limited2016-03-31Not applicableCanada
LenvimaKitEisai Limited2015-02-13Not applicableUs
LenvimaCapsule4 mg/1OralEisai Limited2016-05-13Not applicableUs
LenvimaCapsule20 mgOralEisai Limited2016-03-31Not applicableCanada
LenvimaCapsule10 mg/1OralEisai Limited2015-02-13Not applicableUs
Categories
UNII
EE083865G2
CAS number
417716-92-8
Weight
Average: 426.86
Monoisotopic: 426.1094828
Chemical Formula
C21H19ClN4O4
InChI Key
WOSKHXYHFSIKNG-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

Indication

Lenvatinib is indicated for the treatment of patients with locally recurrent or metastatic, progressive, radioactive iodine-refractory differentiated thyroid cancer.

Structured Indications
Pharmacodynamics

Based 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 action

Lenvatinib 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.

TargetActionsOrganism
AVascular endothelial growth factor receptor 1
inhibitor
Human
AVascular endothelial growth factor receptor 2
inhibitor
Human
AVascular endothelial growth factor receptor 3
inhibitor
Human
AFibroblast growth factor receptor 1
inhibitor
Human
AFibroblast growth factor receptor 2
inhibitor
Human
AFibroblast growth factor receptor 3
inhibitor
Human
AFibroblast growth factor receptor 4
inhibitor
Human
APlatelet derived growth factor receptor alpha
inhibitor
Human
ARET
inhibitor
Human
AMast/stem cell growth factor receptor Kit
inhibitor
Human
Absorption

Time 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 distribution
Not Available
Protein binding

In vitro binding of lenvatinib to human plasma proteins ranged from 98% to 99%.

Metabolism

Lenvatinib is metabolized by CYP3A and aldehyde oxidase.

Route of elimination

Following administration of a radiolabeled dose, approximately 64% and 25% of the radiolabel were eliminated in the feces and urine, respectively.

Half life

The terminal elimination half­life of lenvatinib is approximately 28 hours.

Clearance
Not Available
Toxicity

The 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 organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Lenvatinib.Approved
AcetyldigoxinAcetyldigoxin may decrease the cardiotoxic activities of Lenvatinib.Experimental
AlfuzosinAlfuzosin may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
AmantadineAmantadine may increase the QTc-prolonging activities of Lenvatinib.Approved
AmiodaroneThe metabolism of Lenvatinib can be decreased when combined with Amiodarone.Approved, Investigational
AmitriptylineAmitriptyline may increase the QTc-prolonging activities of Lenvatinib.Approved
AmoxapineAmoxapine may increase the QTc-prolonging activities of Lenvatinib.Approved
AnagrelideLenvatinib may increase the QTc-prolonging activities of Anagrelide.Approved
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
AtazanavirThe metabolism of Lenvatinib can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineAtomoxetine may increase the QTc-prolonging activities of Lenvatinib.Approved
AzithromycinAzithromycin may increase the QTc-prolonging activities of Lenvatinib.Approved
BedaquilineBedaquiline may increase the QTc-prolonging activities of Lenvatinib.Approved
BevacizumabBevacizumab may increase the cardiotoxic activities of Lenvatinib.Approved, Investigational
BoceprevirThe metabolism of Lenvatinib can be decreased when combined with Boceprevir.Approved, Withdrawn
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
BuserelinBuserelin may increase the QTc-prolonging activities of Lenvatinib.Approved
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Lenvatinib.Approved
CarbamazepineThe metabolism of Lenvatinib can be increased when combined with Carbamazepine.Approved, Investigational
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
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
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
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
CymarinCymarin may decrease the cardiotoxic activities of Lenvatinib.Experimental
DabrafenibThe serum concentration of Lenvatinib can be decreased when it is combined with Dabrafenib.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
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
DigitoxinDigitoxin may decrease the cardiotoxic activities of Lenvatinib.Approved, Investigational
DigoxinDigoxin may decrease the cardiotoxic activities of Lenvatinib.Approved
Digoxin Immune Fab (Ovine)Digoxin Immune Fab (Ovine) 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
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
DoxepinDoxepin may increase the QTc-prolonging activities of Lenvatinib.Approved
DoxycyclineThe metabolism of Lenvatinib can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Lenvatinib can be decreased when combined with Dronedarone.Approved
DroperidolDroperidol may increase the QTc-prolonging activities of Lenvatinib.Approved, Vet 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
EnzalutamideThe serum concentration of Lenvatinib can be decreased when it is combined with Enzalutamide.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
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
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
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
GemifloxacinGemifloxacin may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
GitoformateGitoformate may decrease the cardiotoxic activities of Lenvatinib.Experimental
GoserelinGoserelin may increase the QTc-prolonging activities of Lenvatinib.Approved
GranisetronGranisetron may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
HaloperidolHaloperidol may increase the QTc-prolonging activities of Lenvatinib.Approved
HistrelinHistrelin may increase the QTc-prolonging activities of Lenvatinib.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
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
KetoconazoleThe metabolism of Lenvatinib can be decreased when combined with Ketoconazole.Approved, Investigational
Lanatoside CLanatoside C may decrease the cardiotoxic activities of Lenvatinib.Experimental
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
LithiumLithium may increase the QTc-prolonging activities of Lenvatinib.Approved
LopinavirThe metabolism of Lenvatinib can be decreased when combined with Lopinavir.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
MefloquineMefloquine may increase the QTc-prolonging activities of Lenvatinib.Approved
MethadoneMethadone may increase the QTc-prolonging activities of Lenvatinib.Approved
MethotrimeprazineMethotrimeprazine may increase the QTc-prolonging activities of Lenvatinib.Approved
MetildigoxinMetildigoxin may decrease the cardiotoxic activities of Lenvatinib.Experimental
MetoclopramideMetoclopramide may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
MetronidazoleMetronidazole may increase the QTc-prolonging activities of Lenvatinib.Approved
MifepristoneThe serum concentration of Lenvatinib can be increased when it is combined with Mifepristone.Approved, Investigational
MirabegronMirabegron may increase the QTc-prolonging activities of Lenvatinib.Approved
MirtazapineMirtazapine may increase the QTc-prolonging activities of Lenvatinib.Approved
MitotaneThe serum concentration of Lenvatinib can be decreased when it is combined with Mitotane.Approved
MoexiprilMoexipril may increase the QTc-prolonging activities of Lenvatinib.Approved
MoxifloxacinMoxifloxacin may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
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
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
NilotinibThe metabolism of Lenvatinib can be decreased when combined with Nilotinib.Approved, Investigational
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
OleandrinOleandrin may decrease the cardiotoxic activities of Lenvatinib.Experimental, Investigational
OlodaterolOlodaterol may increase the QTc-prolonging activities of Lenvatinib.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
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
PanobinostatPanobinostat may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
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
PeruvosidePeruvoside may decrease the cardiotoxic activities of Lenvatinib.Experimental
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
PosaconazoleThe metabolism of Lenvatinib can be decreased when combined with Posaconazole.Approved, Investigational, 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
ProcainamideLenvatinib may increase the QTc-prolonging activities of Procainamide.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
ProscillaridinProscillaridin may decrease the cardiotoxic activities of Lenvatinib.Experimental
ProtriptylineProtriptyline may increase the QTc-prolonging activities of Lenvatinib.Approved
QuetiapineLenvatinib may increase the QTc-prolonging activities of Quetiapine.Approved
QuinidineLenvatinib may increase the QTc-prolonging activities of Quinidine.Approved
QuinineLenvatinib may increase the QTc-prolonging activities of Quinine.Approved
RanolazineThe serum concentration of Lenvatinib can be increased when it is combined with Ranolazine.Approved, Investigational
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
RitonavirRitonavir may increase the QTc-prolonging activities of Lenvatinib.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
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
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
St. John's WortThe serum concentration of Lenvatinib can be decreased when it is combined with St. John's Wort.Investigational, Nutraceutical
StiripentolThe serum concentration of Lenvatinib can be increased when it is combined with Stiripentol.Approved
SulfamethoxazoleSulfamethoxazole may increase the QTc-prolonging activities of Lenvatinib.Approved
SulfisoxazoleSulfisoxazole may increase the QTc-prolonging activities of Lenvatinib.Approved, Vet Approved
SunitinibSunitinib may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
TamoxifenTamoxifen may increase the QTc-prolonging activities of Lenvatinib.Approved
TelaprevirThe metabolism of Lenvatinib can be decreased when combined with Telaprevir.Approved, Withdrawn
TelavancinTelavancin may increase the QTc-prolonging activities of Lenvatinib.Approved
TelithromycinTelithromycin may increase the QTc-prolonging activities of Lenvatinib.Approved
TerbutalineTerbutaline may increase the QTc-prolonging activities of Lenvatinib.Approved
TeriflunomideThe serum concentration of Lenvatinib can be increased when it is combined with Teriflunomide.Approved
TetrabenazineLenvatinib may increase the QTc-prolonging activities of Tetrabenazine.Approved
ThioridazineLenvatinib may increase the QTc-prolonging activities of Thioridazine.Approved, Withdrawn
ThiothixeneThiothixene may increase the QTc-prolonging activities of Lenvatinib.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
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
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
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
VoriconazoleThe metabolism of Lenvatinib can be decreased when combined with Voriconazole.Approved, Investigational
VorinostatVorinostat may increase the QTc-prolonging activities of Lenvatinib.Approved, Investigational
ZiprasidoneThe metabolism of Lenvatinib can be decreased when combined with Ziprasidone.Approved
ZuclopenthixolLenvatinib may increase the QTc-prolonging activities of Zuclopenthixol.Approved, Investigational
Food Interactions
Not Available

References

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
KEGG Drug
D09920
PubChem Compound
9823820
PubChem Substance
310265006
ChemSpider
7999567
BindingDB
50331094
ChEBI
85994
ChEMBL
CHEMBL1289601
PharmGKB
PA166153472
HET
LEV
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Lenvatinib
ATC Codes
L01XE29 — Lenvatinib
AHFS Codes
  • 10:00.00 — Antineoplastic Agents
PDB Entries
3wzd
FDA label
Download (388 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1Active Not RecruitingTreatmentRenal Cell Adenocarcinoma1
1Active Not RecruitingTreatmentSolid Tumor or Lymphoma1
1Active Not RecruitingTreatmentTumors1
1Active Not RecruitingTreatmentTumors, Solid1
1Active Not RecruitingTreatmentUnresectable Hepatocellular Carcinoma (HCC)1
1CompletedBasic ScienceMalignant Lymphomas / Refractory Solid Tumors1
1CompletedTreatmentAdvanced Solid Tumors / Malignant Lymphomas1
1CompletedTreatmentCancer: Solid Tumors1
1CompletedTreatmentCancers2
1CompletedTreatmentDisease Severity / Impaired Renal Function1
1CompletedTreatmentHealthy Volunteers3
1CompletedTreatmentHealthy Volunteers / P-glycoprotein1
1CompletedTreatmentHepatic Function / Hepatic Impairment1
1CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
1CompletedTreatmentMetastatic Melanoma1
1Not Yet RecruitingTreatmentCancer, Advanced / Malignant Neoplasm of Breast / Malignant Neoplasms of Bone and Articular Cartilage / Malignant Neoplasms of Digestive Organs / Malignant Neoplasms of Eye Brain and Other Parts of Central Nervous System / Malignant Neoplasms of Female Genital Organs / Malignant Neoplasms of Ill-defined Secondary and Unspecified Sites / Malignant Neoplasms of Independent (Primary) Multiple Sites / Malignant Neoplasms of Lip Oral Cavity and Pharynx / Malignant Neoplasms of Male Genital Organs / Malignant Neoplasms of Mesothelial and Soft Tissue / Malignant Neoplasms of Respiratory and Intrathoracic Organs / Malignant Neoplasms of Thyroid and Other Endocrine Glands / Malignant Neoplasms of Urinary Tract1
1Not Yet RecruitingTreatmentTumors, Solid1
1RecruitingTreatmentFallopian Tube Carcinoma / Primary Peritoneal Carcinoma / Recurrent Endometrial Cancer / Recurrent Ovarian Cancer1
1RecruitingTreatmentHepatocellular,Carcinoma1
1RecruitingTreatmentRectal Adenocarcinoma / Rectal Carcinoma1
1, 2Active Not RecruitingTreatmentMetastatic Renal Cell Carcinoma1
1, 2CompletedTreatmentHepatocellular,Carcinoma1
1, 2CompletedTreatmentStage IV Melanoma1
1, 2Not Yet RecruitingTreatmentRecurrent and Refractory Solid Tumors1
1, 2RecruitingTreatmentCancer, Breast1
1, 2RecruitingTreatmentDifferentiated Thyroid Cancer (DTC) / Sarcoma, Osteogenic / Solid Malignant Tumors / Tumors1
1, 2RecruitingTreatmentTumors1
1, 2TerminatedTreatmentCancer, Ovarian1
2Active Not RecruitingTreatmentAdenoid Cystic Carcinomas of the Salivary Glands1
2Active Not RecruitingTreatmentBiliary Tract Cancer1
2Active Not RecruitingTreatmentCarcinoma, Adenoid Cystic1
2Active Not RecruitingTreatmentKIF5B-RET-Positive Adenocarcinoma of the Lung1
2Active Not RecruitingTreatmentThyroid Cancer, Anaplastic1
2CompletedTreatmentEndometrial Cancers1
2CompletedTreatmentGliomas1
2CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
2CompletedTreatmentStage IV Melanoma / Unresectable Stage III1
2CompletedTreatmentThyroid Cancers2
2Not Yet RecruitingTreatmentCancers1
2Not Yet RecruitingTreatmentColumnar Cell Variant Thyroid Gland Papillary Carcinoma / Follicular Variant Thyroid Gland Papillary Carcinoma / Poorly Differentiated Thyroid Gland Carcinoma / Recurrent Thyroid Gland Carcinoma / Stage III Differentiated Thyroid Gland Carcinoma / Stage III Thyroid Gland Follicular Carcinoma / Stage III Thyroid Gland Papillary Carcinoma / Stage IV Thyroid Gland Follicular Carcinoma / Stage IV Thyroid Gland Papillary Carcinoma / Stage IVA Differentiated Thyroid Gland Carcinoma / Stage IVA Thyroid Gland Follicular Carcinoma / Stage IVA Thyroid Gland Papillary Carcinoma / Stage IVB Differentiated Thyroid Gland Carcinoma / Stage IVB Thyroid Gland Follicular Carcinoma / Stage IVB Thyroid Gland Papillary Carcinoma / Stage IVC Differentiated Thyroid Gland Carcinoma / Stage IVC Thyroid Gland Follicular Carcinoma / Stage IVC Thyroid Gland Papillary Carcinoma / Tall Cell Variant Thyroid Gland Papillary Carcinoma / Thyroid Gland Oncocytic Follicular Carcinoma1
2Not Yet RecruitingTreatmentRenal Cell Adenocarcinoma1
2RecruitingTreatmentAnaplastic Thyroid Cancers1
2RecruitingTreatmentCancer, Breast1
2RecruitingTreatmentCancers / Tumors, Solid1
2RecruitingTreatmentGastrooesophageal Cancer1
2RecruitingTreatmentMalignant Adrenal Gland Pheochromocytoma / Metastatic Adrenal Gland Pheochromocytoma / Paraganglion neoplasm malignant1
2RecruitingTreatmentNeuroendocrine Tumors1
2RecruitingTreatmentNon Clear Cell Renal Cell Carcinoma (nccRCC)1
2RecruitingTreatmentRenal Cell Adenocarcinoma1
2RecruitingTreatmentThyroid Cancers2
2WithdrawnTreatmentNeoplasms, Endometrial1
3Active Not RecruitingTreatmentHepatocellular Carcinoma (HCC)1
3Active Not RecruitingTreatmentThyroid Cancers1
3RecruitingTreatmentDifferentiated Thyroid Cancer (DTC)1
3RecruitingTreatmentRenal Cell Adenocarcinoma1
Not AvailableApproved for MarketingNot AvailableDifferentiated Thyroid Cancer (DTC)1
Not AvailableRecruitingNot AvailableNeoplasms, Thyroid1
Not AvailableRecruitingDiagnosticAdvanced Cancers / Endocrine Tumors1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
CapsuleOral10 mg/1
CapsuleOral10 mg
CapsuleOral14 mg
CapsuleOral18 mg
CapsuleOral20 mg
CapsuleOral24 mg
CapsuleOral4 mg/1
CapsuleOral8 mg
Kit
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US9006256No2007-07-272027-07-27Us
US7253286No2001-10-192021-10-19Us
US7612208No2006-09-192026-09-19Us

Properties

State
Solid
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 RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as quinoline carboxamides. These are quinolines in which the quinoline ring system is substituted by one or more carboxamide groups.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Quinolines and derivatives
Sub Class
Quinoline carboxamides
Direct Parent
Quinoline carboxamides
Alternative Parents
Diarylethers / N-phenylureas / Phenoxy compounds / Anisoles / Alkyl aryl ethers / Chlorobenzenes / Pyridines and derivatives / Aryl chlorides / Heteroaromatic compounds / Ureas
show 8 more
Substituents
Quinoline-6-carboxamide / Diaryl ether / N-phenylurea / Phenoxy compound / Anisole / Phenol ether / Alkyl aryl ether / Halobenzene / Chlorobenzene / Aryl chloride
show 23 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
aromatic ether, quinolines, ureas, monocarboxylic acid amide, cyclopropanes, monochlorobenzenes, aromatic amide (CHEBI:85994)

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 ...
Gene Name
FLT1
Uniprot ID
P17948
Uniprot Name
Vascular endothelial growth factor receptor 1
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 ...
Gene Name
KDR
Uniprot ID
P35968
Uniprot Name
Vascular endothelial growth factor receptor 2
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 cardi...
Gene Name
FLT4
Uniprot ID
P35916
Uniprot Name
Vascular endothelial growth factor receptor 3
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 ...
Gene Name
FGFR1
Uniprot ID
P11362
Uniprot Name
Fibroblast growth factor receptor 1
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 apoptosi...
Gene Name
FGFR2
Uniprot ID
P21802
Uniprot Name
Fibroblast growth factor receptor 2
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...
Gene Name
FGFR3
Uniprot ID
P22607
Uniprot Name
Fibroblast growth factor receptor 3
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 o...
Gene Name
FGFR4
Uniprot ID
P22455
Uniprot Name
Fibroblast growth factor receptor 4
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 main...
Gene Name
KIT
Uniprot ID
P10721
Uniprot Name
Mast/stem cell growth factor receptor Kit
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
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...
Gene Name
AOX1
Uniprot ID
Q06278
Uniprot Name
Aldehyde oxidase
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
Uniprot Name
Multidrug resistance protein 1
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 fro...
Gene Name
ABCG2
Uniprot ID
Q9UNQ0
Uniprot Name
ATP-binding cassette sub-family G member 2
Molecular Weight
72313.47 Da

Drug created on June 22, 2015 07:20 / Updated on November 22, 2017 12:38