You are using an unsupported browser. Please upgrade your browser to a newer version to get the best experience on DrugBank.
Identification
NameAxitinib
Accession NumberDB06626
TypeSmall Molecule
GroupsApproved, Investigational
DescriptionAxitinib is an oral, potent, and selective inhibitor of vascular endothelial growth factor receptors (VEGFR) 1, 2, and 3. Axitinib is marketed under the name Inlyta®, and if one previous systemic therapy for kidney cell cancer has failed, axitinib is indicated.
Structure
Thumb
SynonymsNot Available
External Identifiers
  • AG-013736
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
InlytaTablet7 mgOralPfizer Canada IncNot applicableNot applicableCanada
InlytaTablet, film coated1 mg/1OralPfizer Laboratories Div Pfizer Inc2012-01-27Not applicableUs
InlytaTablet, film coated3 mgOralPfizer Ltd2012-09-03Not applicableEu
InlytaTablet, film coated5 mgOralPfizer Ltd2012-09-03Not applicableEu
InlytaTablet, film coated7 mgOralPfizer Ltd2012-09-03Not applicableEu
InlytaTablet1 mgOralPfizer Canada Inc2012-08-17Not applicableCanada
InlytaTablet, film coated1 mgOralPfizer Ltd2012-09-03Not applicableEu
InlytaTablet, film coated5 mg/1OralPfizer Laboratories Div Pfizer Inc2012-01-27Not applicableUs
InlytaTablet, film coated3 mgOralPfizer Ltd2012-09-03Not applicableEu
InlytaTablet, film coated5 mgOralPfizer Ltd2012-09-03Not applicableEu
InlytaTablet5 mgOralPfizer Canada Inc2012-08-17Not applicableCanada
InlytaTablet, film coated1 mgOralPfizer Ltd2012-09-03Not applicableEu
InlytaTablet, film coated1 mg/1OralU.S. Pharmaceuticals2012-01-27Not applicableUs
InlytaTablet, film coated7 mgOralPfizer Ltd2012-09-03Not applicableEu
InlytaTablet, film coated5 mgOralPfizer Ltd2012-09-03Not applicableEu
InlytaTablet3 mgOralPfizer Canada IncNot applicableNot applicableCanada
InlytaTablet, film coated1 mgOralPfizer Ltd2012-09-03Not applicableEu
InlytaTablet, film coated5 mg/1OralU.S. Pharmaceuticals2012-01-27Not applicableUs
InlytaTablet, film coated7 mgOralPfizer Ltd2012-09-03Not applicableEu
InlytaTablet, film coated3 mgOralPfizer Ltd2012-09-03Not applicableEu
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIC9LVQ0YUXG
CAS number319460-85-0
WeightNot Available
Chemical FormulaNot Available
InChI KeyNot Available
InChINot Available
IUPAC NameNot Available
SMILESNot Available
Pharmacology
IndicationUsed in kidney cell cancer and investigated for use/treatment in pancreatic and thyroid cancer.
Structured Indications
PharmacodynamicsAxitinib prevents the progression of cancer by inhibiting angiogenesis and blocking tumor growth.
Mechanism of actionAxitinib selectively blocks the tyrosine kinase receptors VEGFR-1 (vascular endothelial growth factor receptor), VEGFR-2, and VEGFR-3.
TargetKindPharmacological actionActionsOrganismUniProt ID
Vascular endothelial growth factor receptor 1Proteinyes
inhibitor
HumanP17948 details
Vascular endothelial growth factor receptor 2Proteinyes
inhibitor
HumanP35968 details
Vascular endothelial growth factor receptor 3Proteinyes
inhibitor
HumanP35916 details
Related Articles
AbsorptionAfter one 5 mg dose of axitinib, it takes about 2.5 to 4.1 hours to reach maximum plasma concentration.
Volume of distribution

The volume of distribution is 160 L.

Protein bindingPlasma protein binding for axitinib is high at over 99% with most protein binding to albumin followed by α1-acid glycoprotein.
Metabolism

Axitinib undergoes mainly hepatic metabolism. CYP3A4 and CYP3A5 are the main hepatic enzymes while CYP1A2, CYP2C19, and UGT1A1 enzymes are secondary.

Route of eliminationAxitinib is mainly eliminated unchanged in the feces (41%) with 12% of the original dose as unchanged axitinib. There is also 23% eliminated in the urine, most of which are metabolites.
Half lifeAxitinib has a half life of 2.5 to 6.1 hours.
Clearance

The average clearance of axitinib is 38 L/h.

ToxicitySome of the more serious toxic effects seen in patients taking axitinib include, but are not limited to, hypertension, thrombotic events, hemorrhage, and GI perforation.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
AbirateroneThe serum concentration of Axitinib can be increased when it is combined with Abiraterone.Approved
AcetaminophenThe serum concentration of Axitinib can be increased when it is combined with Acetaminophen.Approved
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Axitinib.Approved
AfatinibThe serum concentration of Axitinib can be increased when it is combined with Afatinib.Approved
AlbendazoleThe serum concentration of Axitinib can be increased when it is combined with Albendazole.Approved, Vet Approved
AldosteroneThe serum concentration of Axitinib can be decreased when it is combined with Aldosterone.Experimental
AlectinibThe serum concentration of Axitinib can be increased when it is combined with Alectinib.Approved
AlfentanilThe serum concentration of Axitinib can be increased when it is combined with Alfentanil.Approved, Illicit
AmantadineThe serum concentration of Axitinib can be increased when it is combined with Amantadine.Approved
Aminohippuric acidThe serum concentration of Axitinib can be increased when it is combined with Aminohippuric acid.Approved
AmiodaroneThe serum concentration of Axitinib can be increased when it is combined with Amiodarone.Approved, Investigational
AmitriptylineThe serum concentration of Axitinib can be increased when it is combined with Amitriptyline.Approved
AmlodipineThe serum concentration of Axitinib can be increased when it is combined with Amlodipine.Approved
AmprenavirThe serum concentration of Axitinib can be decreased when it is combined with Amprenavir.Approved
AmsacrineThe serum concentration of Axitinib can be increased when it is combined with Amsacrine.Approved
AnvirzelAnvirzel may decrease the cardiotoxic activities of Axitinib.Investigational
AprepitantThe serum concentration of Axitinib can be increased when it is combined with Aprepitant.Approved, Investigational
ArmodafinilThe metabolism of Axitinib can be decreased when combined with Armodafinil.Approved, Investigational
AstemizoleThe serum concentration of Axitinib can be increased when it is combined with Astemizole.Approved, Withdrawn
AtazanavirThe serum concentration of Axitinib can be increased when it is combined with Atazanavir.Approved, Investigational
AtenololThe serum concentration of Axitinib can be increased when it is combined with Atenolol.Approved
AtomoxetineThe metabolism of Axitinib can be decreased when combined with Atomoxetine.Approved
AtorvastatinThe serum concentration of Axitinib can be increased when it is combined with Atorvastatin.Approved
AzelastineThe serum concentration of Axitinib can be increased when it is combined with Azelastine.Approved
AzithromycinThe serum concentration of Axitinib can be increased when it is combined with Azithromycin.Approved
BenzocaineThe serum concentration of Axitinib can be increased when it is combined with Benzocaine.Approved
BepridilThe serum concentration of Axitinib can be increased when it is combined with Bepridil.Approved, Withdrawn
BevacizumabBevacizumab may increase the cardiotoxic activities of Axitinib.Approved, Investigational
BexaroteneThe serum concentration of Axitinib can be decreased when it is combined with Bexarotene.Approved, Investigational
BiperidenThe serum concentration of Axitinib can be increased when it is combined with Biperiden.Approved
BoceprevirThe serum concentration of Axitinib can be increased when it is combined with Boceprevir.Approved
BortezomibThe metabolism of Axitinib can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Axitinib can be decreased when it is combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Axitinib can be increased when it is combined with Bosutinib.Approved
BromocriptineThe serum concentration of Axitinib can be increased when it is combined with Bromocriptine.Approved, Investigational
BuprenorphineThe serum concentration of Axitinib can be increased when it is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BuspironeThe serum concentration of Axitinib can be increased when it is combined with Buspirone.Approved, Investigational
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Axitinib.Approved
CaffeineThe serum concentration of Axitinib can be increased when it is combined with Caffeine.Approved
CanagliflozinThe serum concentration of Axitinib can be increased when it is combined with Canagliflozin.Approved
CandesartanThe serum concentration of Axitinib can be increased when it is combined with Candesartan.Approved
CaptoprilThe serum concentration of Axitinib can be increased when it is combined with Captopril.Approved
CarbamazepineThe serum concentration of Axitinib can be decreased when it is combined with Carbamazepine.Approved, Investigational
CarvedilolThe serum concentration of Axitinib can be increased when it is combined with Carvedilol.Approved, Investigational
CaspofunginThe serum concentration of Axitinib can be increased when it is combined with Caspofungin.Approved
CeritinibThe serum concentration of Axitinib can be increased when it is combined with Ceritinib.Approved
ChloramphenicolThe metabolism of Axitinib can be decreased when combined with Chloramphenicol.Approved, Vet Approved
ChloroquineThe serum concentration of Axitinib can be increased when it is combined with Chloroquine.Approved, Vet Approved
ChlorpromazineThe serum concentration of Axitinib can be increased when it is combined with Chlorpromazine.Approved, Vet Approved
ChlorpropamideThe serum concentration of Axitinib can be increased when it is combined with Chlorpropamide.Approved
ChlorprothixeneThe serum concentration of Axitinib can be increased when it is combined with Chlorprothixene.Approved, Withdrawn
CholecalciferolThe metabolism of Axitinib can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CholesterolThe serum concentration of Axitinib can be increased when it is combined with Cholesterol.Experimental
Cholic AcidThe serum concentration of Axitinib can be decreased when it is combined with Cholic Acid.Approved
CilazaprilThe serum concentration of Axitinib can be increased when it is combined with Cilazapril.Approved
CimetidineThe serum concentration of Axitinib can be decreased when it is combined with Cimetidine.Approved
CiprofloxacinThe serum concentration of Axitinib can be increased when it is combined with Ciprofloxacin.Approved, Investigational
CitalopramThe serum concentration of Axitinib can be increased when it is combined with Citalopram.Approved
ClarithromycinThe serum concentration of Axitinib can be increased when it is combined with Clarithromycin.Approved
ClemastineThe metabolism of Axitinib can be decreased when combined with Clemastine.Approved
ClofazimineThe serum concentration of Axitinib can be increased when it is combined with Clofazimine.Approved, Investigational
ClomipramineThe serum concentration of Axitinib can be increased when it is combined with Clomipramine.Approved, Vet Approved
ClotrimazoleThe metabolism of Axitinib can be decreased when combined with Clotrimazole.Approved, Vet Approved
CobicistatThe serum concentration of Axitinib can be increased when it is combined with Cobicistat.Approved
ColchicineThe serum concentration of Axitinib can be increased when it is combined with Colchicine.Approved
ColforsinThe serum concentration of Axitinib can be increased when it is combined with Colforsin.Experimental
ConivaptanThe serum concentration of Axitinib can be increased when it is combined with Conivaptan.Approved, Investigational
CrizotinibThe metabolism of Axitinib can be decreased when combined with Crizotinib.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Axitinib.Approved, Investigational
CyclosporineThe metabolism of Axitinib can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
Cyproterone acetateThe serum concentration of Axitinib can be decreased when it is combined with Cyproterone acetate.Approved, Investigational
DabrafenibThe serum concentration of Axitinib can be decreased when it is combined with Dabrafenib.Approved
DaclatasvirThe serum concentration of Axitinib can be increased when it is combined with Daclatasvir.Approved
DactinomycinThe serum concentration of Axitinib can be increased when it is combined with Dactinomycin.Approved
DarunavirThe serum concentration of Axitinib can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Axitinib can be increased when it is combined with Dasatinib.Approved, Investigational
DaunorubicinThe serum concentration of Axitinib can be decreased when it is combined with Daunorubicin.Approved
DeferasiroxThe serum concentration of Axitinib can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Axitinib can be decreased when combined with Delavirdine.Approved
DesipramineThe serum concentration of Axitinib can be increased when it is combined with Desipramine.Approved
DeslanosideDeslanoside may decrease the cardiotoxic activities of Axitinib.Approved
DesloratadineThe serum concentration of Axitinib can be increased when it is combined with Desloratadine.Approved, Investigational
DexamethasoneThe serum concentration of Axitinib can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DextromethorphanThe serum concentration of Axitinib can be increased when it is combined with Dextromethorphan.Approved
DiclofenacThe serum concentration of Axitinib can be increased when it is combined with Diclofenac.Approved, Vet Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Axitinib.Approved
DigoxinDigoxin may decrease the cardiotoxic activities of Axitinib.Approved
DihydroergotamineThe metabolism of Axitinib can be decreased when combined with Dihydroergotamine.Approved
DiltiazemThe metabolism of Axitinib can be decreased when combined with Diltiazem.Approved
DipyridamoleThe serum concentration of Axitinib can be increased when it is combined with Dipyridamole.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Axitinib.Approved, Investigational
DoxazosinThe serum concentration of Axitinib can be increased when it is combined with Doxazosin.Approved
DoxepinThe serum concentration of Axitinib can be increased when it is combined with Doxepin.Approved
DoxorubicinThe serum concentration of Axitinib can be decreased when it is combined with Doxorubicin.Approved, Investigational
DoxycyclineThe metabolism of Axitinib can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronabinolThe serum concentration of Axitinib can be increased when it is combined with Dronabinol.Approved, Illicit
DronedaroneThe metabolism of Axitinib can be decreased when combined with Dronedarone.Approved
EfavirenzThe serum concentration of Axitinib can be decreased when it is combined with Efavirenz.Approved, Investigational
ElbasvirThe serum concentration of Axitinib can be increased when it is combined with Elbasvir.Approved
EltrombopagThe serum concentration of Axitinib can be increased when it is combined with Eltrombopag.Approved
EnalaprilThe serum concentration of Axitinib can be increased when it is combined with Enalapril.Approved, Vet Approved
EnzalutamideThe serum concentration of Axitinib can be decreased when it is combined with Enzalutamide.Approved
ErgonovineThe serum concentration of Axitinib can be increased when it is combined with Ergonovine.Approved
ErgotamineThe serum concentration of Axitinib can be increased when it is combined with Ergotamine.Approved
ErythromycinThe metabolism of Axitinib can be decreased when combined with Erythromycin.Approved, Vet Approved
Eslicarbazepine acetateThe serum concentration of Axitinib can be decreased when it is combined with Eslicarbazepine acetate.Approved
EsomeprazoleThe metabolism of Axitinib can be decreased when combined with Esomeprazole.Approved, Investigational
EstramustineThe serum concentration of Axitinib can be increased when it is combined with Estramustine.Approved
EstriolThe serum concentration of Axitinib can be decreased when it is combined with Estriol.Approved, Vet Approved
EstroneThe serum concentration of Axitinib can be decreased when it is combined with Estrone.Approved
EtoposideThe serum concentration of Axitinib can be increased when it is combined with Etoposide.Approved
EtravirineThe serum concentration of Axitinib can be decreased when it is combined with Etravirine.Approved
FelodipineThe serum concentration of Axitinib can be increased when it is combined with Felodipine.Approved, Investigational
FentanylThe serum concentration of Axitinib can be increased when it is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FexofenadineThe serum concentration of Axitinib can be increased when it is combined with Fexofenadine.Approved
FidaxomicinThe serum concentration of Axitinib can be increased when it is combined with Fidaxomicin.Approved
FluconazoleThe metabolism of Axitinib can be decreased when combined with Fluconazole.Approved
FluoxetineThe serum concentration of Axitinib can be increased when it is combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe serum concentration of Axitinib can be increased when it is combined with Flupentixol.Approved, Withdrawn
FluphenazineThe serum concentration of Axitinib can be increased when it is combined with Fluphenazine.Approved
FlurazepamThe serum concentration of Axitinib can be increased when it is combined with Flurazepam.Approved, Illicit
FluvoxamineThe metabolism of Axitinib can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Axitinib can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Axitinib can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe serum concentration of Axitinib can be decreased when it is combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Axitinib can be increased when it is combined with Fusidic Acid.Approved
GefitinibThe serum concentration of Axitinib can be increased when it is combined with Gefitinib.Approved, Investigational
GemfibrozilThe metabolism of Axitinib can be decreased when combined with Gemfibrozil.Approved
GenisteinThe serum concentration of Axitinib can be increased when it is combined with Genistein.Investigational
GlyburideThe serum concentration of Axitinib can be increased when it is combined with Glyburide.Approved
GlycerolThe serum concentration of Axitinib can be increased when it is combined with Glycerol.Experimental
Gramicidin DThe serum concentration of Axitinib can be increased when it is combined with Gramicidin D.Approved
GrepafloxacinThe serum concentration of Axitinib can be increased when it is combined with Grepafloxacin.Withdrawn
HaloperidolThe serum concentration of Axitinib can be increased when it is combined with Haloperidol.Approved
HydrocortisoneThe serum concentration of Axitinib can be increased when it is combined with Hydrocortisone.Approved, Vet Approved
IdelalisibThe serum concentration of Axitinib can be increased when it is combined with Idelalisib.Approved
ImatinibThe metabolism of Axitinib can be decreased when combined with Imatinib.Approved
ImipramineThe serum concentration of Axitinib can be increased when it is combined with Imipramine.Approved
IndinavirThe serum concentration of Axitinib can be increased when it is combined with Indinavir.Approved
IndomethacinThe serum concentration of Axitinib can be increased when it is combined with Indomethacin.Approved, Investigational
IsavuconazoniumThe metabolism of Axitinib can be decreased when combined with Isavuconazonium.Approved, Investigational
IsoniazidThe metabolism of Axitinib can be decreased when combined with Isoniazid.Approved
IsradipineThe metabolism of Axitinib can be decreased when combined with Isradipine.Approved
ItraconazoleThe serum concentration of Axitinib can be increased when it is combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Axitinib can be increased when it is combined with Ivacaftor.Approved
IvermectinThe serum concentration of Axitinib can be increased when it is combined with Ivermectin.Approved, Vet Approved
KetamineThe serum concentration of Axitinib can be increased when it is combined with Ketamine.Approved, Vet Approved
KetoconazoleThe serum concentration of Axitinib can be increased when it is combined with Ketoconazole.Approved, Investigational
LansoprazoleThe serum concentration of Axitinib can be increased when it is combined with Lansoprazole.Approved, Investigational
LapatinibThe serum concentration of Axitinib can be increased when it is combined with Lapatinib.Approved, Investigational
LevofloxacinThe serum concentration of Axitinib can be increased when it is combined with Levofloxacin.Approved, Investigational
LevothyroxineThe serum concentration of Axitinib can be decreased when it is combined with Levothyroxine.Approved
LidocaineThe serum concentration of Axitinib can be increased when it is combined with Lidocaine.Approved, Vet Approved
LiothyronineThe serum concentration of Axitinib can be decreased when it is combined with Liothyronine.Approved, Vet Approved
LiotrixThe serum concentration of Axitinib can be decreased when it is combined with Liotrix.Approved
LisinoprilThe serum concentration of Axitinib can be increased when it is combined with Lisinopril.Approved, Investigational
LomitapideThe serum concentration of Axitinib can be increased when it is combined with Lomitapide.Approved
LoperamideThe serum concentration of Axitinib can be increased when it is combined with Loperamide.Approved
LopinavirThe serum concentration of Axitinib can be increased when it is combined with Lopinavir.Approved
LoratadineThe serum concentration of Axitinib can be increased when it is combined with Loratadine.Approved
LosartanThe serum concentration of Axitinib can be increased when it is combined with Losartan.Approved
LovastatinThe metabolism of Axitinib can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Axitinib can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Axitinib can be decreased when it is combined with Lumacaftor.Approved
MaprotilineThe serum concentration of Axitinib can be increased when it is combined with Maprotiline.Approved
MebendazoleThe serum concentration of Axitinib can be increased when it is combined with Mebendazole.Approved, Vet Approved
MefloquineThe serum concentration of Axitinib can be increased when it is combined with Mefloquine.Approved
Megestrol acetateThe serum concentration of Axitinib can be increased when it is combined with Megestrol acetate.Approved, Vet Approved
MeprobamateThe serum concentration of Axitinib can be increased when it is combined with Meprobamate.Approved, Illicit
MethadoneThe serum concentration of Axitinib can be increased when it is combined with Methadone.Approved
MetoprololThe serum concentration of Axitinib can be increased when it is combined with Metoprolol.Approved, Investigational
MexiletineThe metabolism of Axitinib can be decreased when combined with Mexiletine.Approved
MibefradilThe serum concentration of Axitinib can be increased when it is combined with Mibefradil.Withdrawn
MiconazoleThe serum concentration of Axitinib can be increased when it is combined with Miconazole.Approved, Investigational, Vet Approved
MidazolamThe serum concentration of Axitinib can be decreased when it is combined with Midazolam.Approved, Illicit
MifepristoneThe serum concentration of Axitinib can be increased when it is combined with Mifepristone.Approved, Investigational
MitomycinThe serum concentration of Axitinib can be increased when it is combined with Mitomycin.Approved
MitotaneThe serum concentration of Axitinib can be decreased when it is combined with Mitotane.Approved
MitoxantroneThe serum concentration of Axitinib can be decreased when it is combined with Mitoxantrone.Approved, Investigational
MoclobemideThe metabolism of Axitinib can be decreased when combined with Moclobemide.Approved
ModafinilThe serum concentration of Axitinib can be decreased when it is combined with Modafinil.Approved, Investigational
MorphineThe serum concentration of Axitinib can be increased when it is combined with Morphine.Approved, Investigational
NafcillinThe serum concentration of Axitinib can be decreased when it is combined with Nafcillin.Approved
NaltrexoneThe serum concentration of Axitinib can be increased when it is combined with Naltrexone.Approved, Investigational, Vet Approved
NaringeninThe serum concentration of Axitinib can be increased when it is combined with Naringenin.Experimental
NefazodoneThe serum concentration of Axitinib can be increased when it is combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Axitinib can be increased when it is combined with Nelfinavir.Approved
NeostigmineThe serum concentration of Axitinib can be increased when it is combined with Neostigmine.Approved, Vet Approved
NetupitantThe serum concentration of Axitinib can be increased when it is combined with Netupitant.Approved
NevirapineThe serum concentration of Axitinib can be decreased when it is combined with Nevirapine.Approved
NicardipineThe serum concentration of Axitinib can be increased when it is combined with Nicardipine.Approved
NifedipineThe serum concentration of Axitinib can be decreased when it is combined with Nifedipine.Approved
NilotinibThe metabolism of Axitinib can be decreased when combined with Nilotinib.Approved, Investigational
NisoldipineThe serum concentration of Axitinib can be increased when it is combined with Nisoldipine.Approved
NitrazepamThe serum concentration of Axitinib can be increased when it is combined with Nitrazepam.Approved
NitrendipineThe serum concentration of Axitinib can be increased when it is combined with Nitrendipine.Approved
NorethisteroneThe serum concentration of Axitinib can be decreased when it is combined with Norethisterone.Approved
OlaparibThe metabolism of Axitinib can be decreased when combined with Olaparib.Approved
OmeprazoleThe serum concentration of Axitinib can be increased when it is combined with Omeprazole.Approved, Investigational, Vet Approved
OsimertinibThe serum concentration of Axitinib can be increased when it is combined with Osimertinib.Approved
OuabainOuabain may decrease the cardiotoxic activities of Axitinib.Approved
P-NitrophenolThe serum concentration of Axitinib can be increased when it is combined with P-Nitrophenol.Experimental
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Axitinib.Approved, Vet Approved
PalbociclibThe serum concentration of Axitinib can be increased when it is combined with Palbociclib.Approved
Palmitic AcidThe serum concentration of Axitinib can be increased when it is combined with Palmitic Acid.Experimental
PantoprazoleThe serum concentration of Axitinib can be increased when it is combined with Pantoprazole.Approved
ParoxetineThe serum concentration of Axitinib can be increased when it is combined with Paroxetine.Approved, Investigational
Peginterferon alfa-2bThe serum concentration of Axitinib can be increased when it is combined with Peginterferon alfa-2b.Approved
PentobarbitalThe serum concentration of Axitinib can be decreased when it is combined with Pentobarbital.Approved, Vet Approved
PerindoprilThe serum concentration of Axitinib can be increased when it is combined with Perindopril.Approved
PhenobarbitalThe serum concentration of Axitinib can be decreased when it is combined with Phenobarbital.Approved
PhenytoinThe serum concentration of Axitinib can be decreased when it is combined with Phenytoin.Approved, Vet Approved
PimozideThe serum concentration of Axitinib can be increased when it is combined with Pimozide.Approved
Platelet Activating FactorThe serum concentration of Axitinib can be decreased when it is combined with Platelet Activating Factor.Experimental
PonatinibThe serum concentration of Axitinib can be increased when it is combined with Ponatinib.Approved
PosaconazoleThe serum concentration of Axitinib can be increased when it is combined with Posaconazole.Approved, Investigational, Vet Approved
PravastatinThe serum concentration of Axitinib can be increased when it is combined with Pravastatin.Approved
PrazosinThe serum concentration of Axitinib can be increased when it is combined with Prazosin.Approved
PrednisoneThe serum concentration of Axitinib can be increased when it is combined with Prednisone.Approved, Vet Approved
PrimidoneThe serum concentration of Axitinib can be decreased when it is combined with Primidone.Approved, Vet Approved
ProbenecidThe serum concentration of Axitinib can be increased when it is combined with Probenecid.Approved
ProgesteroneThe serum concentration of Axitinib can be decreased when it is combined with Progesterone.Approved, Vet Approved
PromethazineThe serum concentration of Axitinib can be increased when it is combined with Promethazine.Approved
PropafenoneThe serum concentration of Axitinib can be increased when it is combined with Propafenone.Approved
PropranololThe serum concentration of Axitinib can be increased when it is combined with Propranolol.Approved, Investigational
ProtriptylineThe serum concentration of Axitinib can be increased when it is combined with Protriptyline.Approved
QuercetinThe serum concentration of Axitinib can be increased when it is combined with Quercetin.Experimental
QuinacrineThe serum concentration of Axitinib can be increased when it is combined with Quinacrine.Approved
QuinidineThe serum concentration of Axitinib can be increased when it is combined with Quinidine.Approved
QuinineThe serum concentration of Axitinib can be increased when it is combined with Quinine.Approved
RanitidineThe serum concentration of Axitinib can be increased when it is combined with Ranitidine.Approved
RanolazineThe serum concentration of Axitinib can be increased when it is combined with Ranolazine.Approved, Investigational
ReboxetineThe serum concentration of Axitinib can be increased when it is combined with Reboxetine.Approved, Investigational
RegorafenibThe serum concentration of Axitinib can be increased when it is combined with Regorafenib.Approved
ReserpineThe serum concentration of Axitinib can be decreased when it is combined with Reserpine.Approved
RifabutinThe serum concentration of Axitinib can be decreased when it is combined with Rifabutin.Approved
RifampicinThe serum concentration of Axitinib can be decreased when it is combined with Rifampicin.Approved
RifapentineThe serum concentration of Axitinib can be decreased when it is combined with Rifapentine.Approved
RilpivirineThe serum concentration of Axitinib can be increased when it is combined with Rilpivirine.Approved
RitonavirThe serum concentration of Axitinib can be increased when it is combined with Ritonavir.Approved, Investigational
RolapitantThe serum concentration of Axitinib can be increased when it is combined with Rolapitant.Approved
RopiniroleThe metabolism of Axitinib can be decreased when combined with Ropinirole.Approved, Investigational
SaquinavirThe serum concentration of Axitinib can be increased when it is combined with Saquinavir.Approved, Investigational
ScopolamineThe serum concentration of Axitinib can be increased when it is combined with Scopolamine.Approved
SelegilineThe serum concentration of Axitinib can be increased when it is combined with Selegiline.Approved, Investigational, Vet Approved
SertralineThe serum concentration of Axitinib can be increased when it is combined with Sertraline.Approved
SildenafilThe metabolism of Axitinib can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Axitinib can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Axitinib can be increased when it is combined with Simeprevir.Approved
SimvastatinThe serum concentration of Axitinib can be increased when it is combined with Simvastatin.Approved
SirolimusThe serum concentration of Axitinib can be decreased when it is combined with Sirolimus.Approved, Investigational
SorafenibThe serum concentration of Axitinib can be increased when it is combined with Sorafenib.Approved, Investigational
SpironolactoneThe serum concentration of Axitinib can be increased when it is combined with Spironolactone.Approved
St. John's WortThe serum concentration of Axitinib can be decreased when it is combined with St. John's Wort.Nutraceutical
StaurosporineThe serum concentration of Axitinib can be increased when it is combined with Staurosporine.Experimental
StiripentolThe serum concentration of Axitinib can be increased when it is combined with Stiripentol.Approved
StreptozocinThe serum concentration of Axitinib can be decreased when it is combined with Streptozocin.Approved
SulfinpyrazoneThe serum concentration of Axitinib can be increased when it is combined with Sulfinpyrazone.Approved
SulfisoxazoleThe metabolism of Axitinib can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SumatriptanThe serum concentration of Axitinib can be increased when it is combined with Sumatriptan.Approved, Investigational
SunitinibThe serum concentration of Axitinib can be increased when it is combined with Sunitinib.Approved, Investigational
TacrineThe serum concentration of Axitinib can be increased when it is combined with Tacrine.Withdrawn
TacrolimusThe serum concentration of Axitinib can be decreased when it is combined with Tacrolimus.Approved, Investigational
TamoxifenThe serum concentration of Axitinib can be decreased when it is combined with Tamoxifen.Approved
Taurocholic AcidThe serum concentration of Axitinib can be increased when it is combined with Taurocholic Acid.Experimental
TelaprevirThe serum concentration of Axitinib can be increased when it is combined with Telaprevir.Approved
TelithromycinThe serum concentration of Axitinib can be increased when it is combined with Telithromycin.Approved
TelmisartanThe serum concentration of Axitinib can be increased when it is combined with Telmisartan.Approved, Investigational
TemsirolimusThe serum concentration of Axitinib can be increased when it is combined with Temsirolimus.Approved
TenofovirThe metabolism of Axitinib can be decreased when combined with Tenofovir.Approved, Investigational
TerazosinThe serum concentration of Axitinib can be increased when it is combined with Terazosin.Approved
TerfenadineThe serum concentration of Axitinib can be increased when it is combined with Terfenadine.Withdrawn
TeriflunomideThe serum concentration of Axitinib can be increased when it is combined with Teriflunomide.Approved
TesmilifeneThe serum concentration of Axitinib can be decreased when it is combined with Tesmilifene.Investigational
TestosteroneThe serum concentration of Axitinib can be increased when it is combined with Testosterone.Approved, Investigational
TheophyllineThe metabolism of Axitinib can be decreased when combined with Theophylline.Approved
TicagrelorThe serum concentration of Axitinib can be increased when it is combined with Ticagrelor.Approved
TiclopidineThe metabolism of Axitinib can be decreased when combined with Ticlopidine.Approved
TocilizumabThe serum concentration of Axitinib can be decreased when it is combined with Tocilizumab.Approved
TolvaptanThe serum concentration of Axitinib can be increased when it is combined with Tolvaptan.Approved
TopiramateThe metabolism of Axitinib can be decreased when combined with Topiramate.Approved
TranylcypromineThe metabolism of Axitinib can be decreased when combined with Tranylcypromine.Approved
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Axitinib.Approved, Investigational
TrazodoneThe serum concentration of Axitinib can be decreased when it is combined with Trazodone.Approved, Investigational
TrifluoperazineThe serum concentration of Axitinib can be increased when it is combined with Trifluoperazine.Approved
TriflupromazineThe serum concentration of Axitinib can be increased when it is combined with Triflupromazine.Approved, Vet Approved
TrimethoprimThe serum concentration of Axitinib can be decreased when it is combined with Trimethoprim.Approved, Vet Approved
TrimipramineThe serum concentration of Axitinib can be increased when it is combined with Trimipramine.Approved
TroleandomycinThe serum concentration of Axitinib can be increased when it is combined with Troleandomycin.Approved
VemurafenibThe serum concentration of Axitinib can be increased when it is combined with Vemurafenib.Approved
VenlafaxineThe metabolism of Axitinib can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Axitinib can be decreased when combined with Verapamil.Approved
VinblastineThe serum concentration of Axitinib can be decreased when it is combined with Vinblastine.Approved
VincristineThe serum concentration of Axitinib can be decreased when it is combined with Vincristine.Approved, Investigational
VinorelbineThe serum concentration of Axitinib can be increased when it is combined with Vinorelbine.Approved, Investigational
VoriconazoleThe serum concentration of Axitinib can be increased when it is combined with Voriconazole.Approved, Investigational
ZimelidineThe serum concentration of Axitinib can be increased when it is combined with Zimelidine.Withdrawn
ZiprasidoneThe metabolism of Axitinib can be decreased when combined with Ziprasidone.Approved
Food Interactions
  • Avoid combination with strong CYP3A4 inhibitors such as grapefruit juice due to the likely increased levels of axitinib. If the combination cannot be avoided, reduce axitinib dose by 50%.
  • Axitinib can be taken with or without food.
References
Synthesis Reference

Hu-Lowe D, Hallin M, Feeley R, Zou H, Rewolinski D, Wickman G, Chen E, Kim Y, Riney S, Reed J, Heller D, Simmons B, Kania R, McTigue M, Niesman M, Gregory S, Shalinsky D, Bender S. Characterization of potency and activity of the VEGF/PDGF receptor tyrosine kinase inhibitor AG013736. Proc Am Assoc Cancer Res. 2002;43:A5357.

General References
  1. Cohen EE, Rosen LS, Vokes EE, Kies MS, Forastiere AA, Worden FP, Kane MA, Sherman E, Kim S, Bycott P, Tortorici M, Shalinsky DR, Liau KF, Cohen RB: Axitinib is an active treatment for all histologic subtypes of advanced thyroid cancer: results from a phase II study. J Clin Oncol. 2008 Oct 10;26(29):4708-13. doi: 10.1200/JCO.2007.15.9566. Epub 2008 Jun 9. [PubMed:18541897 ]
  2. Inai T, Mancuso M, Hashizume H, Baffert F, Haskell A, Baluk P, Hu-Lowe DD, Shalinsky DR, Thurston G, Yancopoulos GD, McDonald DM: Inhibition of vascular endothelial growth factor (VEGF) signaling in cancer causes loss of endothelial fenestrations, regression of tumor vessels, and appearance of basement membrane ghosts. Am J Pathol. 2004 Jul;165(1):35-52. [PubMed:15215160 ]
  3. Rugo HS, Herbst RS, Liu G, Park JW, Kies MS, Steinfeldt HM, Pithavala YK, Reich SD, Freddo JL, Wilding G: Phase I trial of the oral antiangiogenesis agent AG-013736 in patients with advanced solid tumors: pharmacokinetic and clinical results. J Clin Oncol. 2005 Aug 20;23(24):5474-83. Epub 2005 Jul 18. [PubMed:16027439 ]
  4. Rini BI: SU11248 and AG013736: current data and future trials in renal cell carcinoma. Clin Genitourin Cancer. 2005 Dec;4(3):175-80. [PubMed:16425985 ]
  5. Gilbert JA, Adhikari LJ, Lloyd RV, Halfdanarson TR, Muders MH, Ames MM: Molecular markers for novel therapeutic strategies in pancreatic endocrine tumors. Pancreas. 2013 Apr;42(3):411-21. doi: 10.1097/MPA.0b013e31826cb243. [PubMed:23211371 ]
External Links
ATC CodesL01XE17
AHFS Codes
  • 10:00
PDB EntriesNot Available
FDA labelDownload (307 KB)
MSDSDownload (36.8 KB)
ADMET
Predicted ADMET featuresNot Available
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
TabletOral1 mg
TabletOral3 mg
TabletOral5 mg
TabletOral7 mg
Tablet, film coatedOral1 mg/1
Tablet, film coatedOral1 mg
Tablet, film coatedOral3 mg
Tablet, film coatedOral5 mg
Tablet, film coatedOral5 mg/1
Tablet, film coatedOral7 mg
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6534524 No2000-06-302020-06-30Us
US7141581 No2000-06-302020-06-30Us
US8791140 No2010-08-052030-08-05Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubilityIn aqueous media with a pH between 1.1 to 7.8, axitinib has a solubility of over 0.2 μg/mL. From FDA label.
pKa4.8From FDA label.
Predicted PropertiesNot Available
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Taxonomy
ClassificationNot classified

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Vegf-b-activated receptor activity
Specific Function:
Tyrosine-protein kinase that acts as a cell-surface receptor for VEGFA, VEGFB and PGF, and plays an essential role in the development of embryonic vasculature, the regulation of angiogenesis, cell survival, cell migration, macrophage function, chemotaxis, and cancer cell invasion. May play an essential role as a negative regulator of embryonic angiogenesis by inhibiting excessive proliferation ...
Gene Name:
FLT1
Uniprot ID:
P17948
Molecular Weight:
150767.185 Da
References
  1. Cohen EE, Rosen LS, Vokes EE, Kies MS, Forastiere AA, Worden FP, Kane MA, Sherman E, Kim S, Bycott P, Tortorici M, Shalinsky DR, Liau KF, Cohen RB: Axitinib is an active treatment for all histologic subtypes of advanced thyroid cancer: results from a phase II study. J Clin Oncol. 2008 Oct 10;26(29):4708-13. doi: 10.1200/JCO.2007.15.9566. Epub 2008 Jun 9. [PubMed:18541897 ]
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. Cohen EE, Rosen LS, Vokes EE, Kies MS, Forastiere AA, Worden FP, Kane MA, Sherman E, Kim S, Bycott P, Tortorici M, Shalinsky DR, Liau KF, Cohen RB: Axitinib is an active treatment for all histologic subtypes of advanced thyroid cancer: results from a phase II study. J Clin Oncol. 2008 Oct 10;26(29):4708-13. doi: 10.1200/JCO.2007.15.9566. Epub 2008 Jun 9. [PubMed:18541897 ]
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. Cohen EE, Rosen LS, Vokes EE, Kies MS, Forastiere AA, Worden FP, Kane MA, Sherman E, Kim S, Bycott P, Tortorici M, Shalinsky DR, Liau KF, Cohen RB: Axitinib is an active treatment for all histologic subtypes of advanced thyroid cancer: results from a phase II study. J Clin Oncol. 2008 Oct 10;26(29):4708-13. doi: 10.1200/JCO.2007.15.9566. Epub 2008 Jun 9. [PubMed:18541897 ]

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
References
  1. Brennan M, Williams JA, Chen Y, Tortorici M, Pithavala Y, Liu YC: Meta-analysis of contribution of genetic polymorphisms in drug-metabolizing enzymes or transporters to axitinib pharmacokinetics. Eur J Clin Pharmacol. 2012 May;68(5):645-55. doi: 10.1007/s00228-011-1171-8. Epub 2011 Dec 15. [PubMed:22170007 ]
  2. Chen Y, Tortorici MA, Garrett M, Hee B, Klamerus KJ, Pithavala YK: Clinical pharmacology of axitinib. Clin Pharmacokinet. 2013 Sep;52(9):713-25. doi: 10.1007/s40262-013-0068-3. [PubMed:23677771 ]
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrate
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. Brennan M, Williams JA, Chen Y, Tortorici M, Pithavala Y, Liu YC: Meta-analysis of contribution of genetic polymorphisms in drug-metabolizing enzymes or transporters to axitinib pharmacokinetics. Eur J Clin Pharmacol. 2012 May;68(5):645-55. doi: 10.1007/s00228-011-1171-8. Epub 2011 Dec 15. [PubMed:22170007 ]
  2. Chen Y, Tortorici MA, Garrett M, Hee B, Klamerus KJ, Pithavala YK: Clinical pharmacology of axitinib. Clin Pharmacokinet. 2013 Sep;52(9):713-25. doi: 10.1007/s40262-013-0068-3. [PubMed:23677771 ]
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrate
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Brennan M, Williams JA, Chen Y, Tortorici M, Pithavala Y, Liu YC: Meta-analysis of contribution of genetic polymorphisms in drug-metabolizing enzymes or transporters to axitinib pharmacokinetics. Eur J Clin Pharmacol. 2012 May;68(5):645-55. doi: 10.1007/s00228-011-1171-8. Epub 2011 Dec 15. [PubMed:22170007 ]
  2. Chen Y, Tortorici MA, Garrett M, Hee B, Klamerus KJ, Pithavala YK: Clinical pharmacology of axitinib. Clin Pharmacokinet. 2013 Sep;52(9):713-25. doi: 10.1007/s40262-013-0068-3. [PubMed:23677771 ]
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Brennan M, Williams JA, Chen Y, Tortorici M, Pithavala Y, Liu YC: Meta-analysis of contribution of genetic polymorphisms in drug-metabolizing enzymes or transporters to axitinib pharmacokinetics. Eur J Clin Pharmacol. 2012 May;68(5):645-55. doi: 10.1007/s00228-011-1171-8. Epub 2011 Dec 15. [PubMed:22170007 ]
  2. Chen Y, Tortorici MA, Garrett M, Hee B, Klamerus KJ, Pithavala YK: Clinical pharmacology of axitinib. Clin Pharmacokinet. 2013 Sep;52(9):713-25. doi: 10.1007/s40262-013-0068-3. [PubMed:23677771 ]
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrate
General Function:
Steroid binding
Specific Function:
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the IX-alpha-C8 and IX-alpha-C12 monoconjugates and diconjugate. Is also able to catalyze the glucuronidation of 17beta-estradiol, 17alpha-ethinylestradiol, 1-hydroxypyrene, 4-methylumbelliferone, 1-naph...
Gene Name:
UGT1A1
Uniprot ID:
P22309
Molecular Weight:
59590.91 Da
References
  1. Brennan M, Williams JA, Chen Y, Tortorici M, Pithavala Y, Liu YC: Meta-analysis of contribution of genetic polymorphisms in drug-metabolizing enzymes or transporters to axitinib pharmacokinetics. Eur J Clin Pharmacol. 2012 May;68(5):645-55. doi: 10.1007/s00228-011-1171-8. Epub 2011 Dec 15. [PubMed:22170007 ]
  2. Chen Y, Tortorici MA, Garrett M, Hee B, Klamerus KJ, Pithavala YK: Clinical pharmacology of axitinib. Clin Pharmacokinet. 2013 Sep;52(9):713-25. doi: 10.1007/s40262-013-0068-3. [PubMed:23677771 ]

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
References
  1. Brennan M, Williams JA, Chen Y, Tortorici M, Pithavala Y, Liu YC: Meta-analysis of contribution of genetic polymorphisms in drug-metabolizing enzymes or transporters to axitinib pharmacokinetics. Eur J Clin Pharmacol. 2012 May;68(5):645-55. doi: 10.1007/s00228-011-1171-8. Epub 2011 Dec 15. [PubMed:22170007 ]
  2. Chen Y, Tortorici MA, Garrett M, Hee B, Klamerus KJ, Pithavala YK: Clinical pharmacology of axitinib. Clin Pharmacokinet. 2013 Sep;52(9):713-25. doi: 10.1007/s40262-013-0068-3. [PubMed:23677771 ]
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrate
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostaglandin E2, thromboxane B2, leukotriene C3, leukotriene E4, thyroxine and triiodothyronine. Involved in the clearance of bile acids and organic anions from the liver.
Gene Name:
SLCO1B1
Uniprot ID:
Q9Y6L6
Molecular Weight:
76447.99 Da
References
  1. Brennan M, Williams JA, Chen Y, Tortorici M, Pithavala Y, Liu YC: Meta-analysis of contribution of genetic polymorphisms in drug-metabolizing enzymes or transporters to axitinib pharmacokinetics. Eur J Clin Pharmacol. 2012 May;68(5):645-55. doi: 10.1007/s00228-011-1171-8. Epub 2011 Dec 15. [PubMed:22170007 ]
Comments
comments powered by Disqus
Drug created on March 19, 2008 10:41 / Updated on December 09, 2016 02:40