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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
InlytaFilm-coated tablet3 mgOral usePfizer Ltd  2012-09-03Not applicableEu
InlytaFilm-coated tablet5 mgOral usePfizer Ltd  2012-09-03Not applicableEu
InlytaFilm-coated tablet7 mgOral usePfizer Ltd  2012-09-03Not applicableEu
Inlytatablet1 mgoralPfizer Canada Inc2012-08-17Not applicableCanada
InlytaFilm-coated tablet1 mgOral usePfizer Ltd  2012-09-03Not applicableEu
Inlytatablet, film coated5 mg/1oralPfizer Laboratories Div Pfizer Inc2012-01-27Not applicableUs
InlytaFilm-coated tablet3 mgOral usePfizer Ltd  2012-09-03Not applicableEu
InlytaFilm-coated tablet5 mgOral usePfizer Ltd  2012-09-03Not applicableEu
Inlytatablet5 mgoralPfizer Canada Inc2012-08-17Not applicableCanada
InlytaFilm-coated tablet1 mgOral usePfizer Ltd  2012-09-03Not applicableEu
Inlytatablet, film coated1 mg/1oralU.S. Pharmaceuticals2012-01-27Not applicableUs
InlytaFilm-coated tablet7 mgOral usePfizer Ltd  2012-09-03Not applicableEu
InlytaFilm-coated tablet5 mgOral usePfizer Ltd  2012-09-03Not applicableEu
Inlytatablet3 mgoralPfizer Canada IncNot applicableNot applicableCanada
InlytaFilm-coated tablet1 mgOral usePfizer Ltd  2012-09-03Not applicableEu
Inlytatablet, film coated5 mg/1oralU.S. Pharmaceuticals2012-01-27Not applicableUs
InlytaFilm-coated tablet7 mgOral usePfizer Ltd  2012-09-03Not applicableEu
InlytaFilm-coated tablet3 mgOral usePfizer Ltd  2012-09-03Not 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
Taxonomy
ClassificationNot classified
Pharmacology
IndicationUsed in kidney cell cancer and investigated for use/treatment in pancreatic and thyroid cancer.
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.
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
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal AbsorptionNot AvailableNot Available
Blood Brain BarrierNot AvailableNot Available
Caco-2 permeableNot AvailableNot Available
P-glycoprotein substrateNot AvailableNot Available
P-glycoprotein inhibitor INot AvailableNot Available
P-glycoprotein inhibitor IINot AvailableNot Available
Renal organic cation transporterNot AvailableNot Available
CYP450 2C9 substrateNot AvailableNot Available
CYP450 2D6 substrateNot AvailableNot Available
CYP450 3A4 substrateNot AvailableNot Available
CYP450 1A2 substrateNot AvailableNot Available
CYP450 2C9 inhibitorNot AvailableNot Available
CYP450 2D6 inhibitorNot AvailableNot Available
CYP450 2C19 inhibitorNot AvailableNot Available
CYP450 3A4 inhibitorNot AvailableNot Available
CYP450 inhibitory promiscuityNot AvailableNot Available
Ames testNot AvailableNot Available
CarcinogenicityNot AvailableNot Available
BiodegradationNot AvailableNot Available
Rat acute toxicityNot AvailableNot applicable
hERG inhibition (predictor I)Not AvailableNot Available
hERG inhibition (predictor II)Not AvailableNot Available
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Film-coated tabletOral use1 mg
Film-coated tabletOral use3 mg
Film-coated tabletOral use5 mg
Film-coated tabletOral use7 mg
Tabletoral1 mg
Tabletoral3 mg
Tabletoral5 mg
Tabletoral7 mg
Tablet, film coatedoral1 mg/1
Tablet, film coatedoral5 mg/1
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
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)
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Axitinib can be increased when it is combined with Abiraterone.
AcetaminophenThe serum concentration of Axitinib can be increased when it is combined with Acetaminophen.
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Axitinib.
AfatinibThe serum concentration of Axitinib can be increased when it is combined with Afatinib.
AlbendazoleThe serum concentration of Axitinib can be increased when it is combined with Albendazole.
AldosteroneThe serum concentration of Axitinib can be decreased when it is combined with Aldosterone.
AlectinibThe serum concentration of Axitinib can be increased when it is combined with Alectinib.
AlfentanilThe serum concentration of Axitinib can be increased when it is combined with Alfentanil.
AmantadineThe serum concentration of Axitinib can be increased when it is combined with Amantadine.
Aminohippuric acidThe serum concentration of Axitinib can be increased when it is combined with Aminohippuric acid.
AmiodaroneThe serum concentration of Axitinib can be increased when it is combined with Amiodarone.
AmitriptylineThe serum concentration of Axitinib can be increased when it is combined with Amitriptyline.
AmlodipineThe serum concentration of Axitinib can be increased when it is combined with Amlodipine.
AmprenavirThe serum concentration of Axitinib can be decreased when it is combined with Amprenavir.
AmsacrineThe serum concentration of Axitinib can be increased when it is combined with Amsacrine.
AprepitantThe serum concentration of Axitinib can be increased when it is combined with Aprepitant.
ArmodafinilThe metabolism of Axitinib can be decreased when combined with Armodafinil.
AstemizoleThe serum concentration of Axitinib can be increased when it is combined with Astemizole.
AtazanavirThe serum concentration of Axitinib can be increased when it is combined with Atazanavir.
AtenololThe serum concentration of Axitinib can be increased when it is combined with Atenolol.
AtomoxetineThe metabolism of Axitinib can be decreased when combined with Atomoxetine.
AtorvastatinThe serum concentration of Axitinib can be increased when it is combined with Atorvastatin.
AzelastineThe serum concentration of Axitinib can be increased when it is combined with Azelastine.
AzithromycinThe serum concentration of Axitinib can be increased when it is combined with Azithromycin.
BenzocaineThe serum concentration of Axitinib can be increased when it is combined with Benzocaine.
BepridilThe serum concentration of Axitinib can be increased when it is combined with Bepridil.
BevacizumabBevacizumab may increase the cardiotoxic activities of Axitinib.
BexaroteneThe serum concentration of Axitinib can be decreased when it is combined with Bexarotene.
BiperidenThe serum concentration of Axitinib can be increased when it is combined with Biperiden.
BoceprevirThe serum concentration of Axitinib can be increased when it is combined with Boceprevir.
BortezomibThe metabolism of Axitinib can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Axitinib can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Axitinib can be increased when it is combined with Bosutinib.
BromocriptineThe serum concentration of Axitinib can be increased when it is combined with Bromocriptine.
BuprenorphineThe serum concentration of Axitinib can be increased when it is combined with Buprenorphine.
BuspironeThe serum concentration of Axitinib can be increased when it is combined with Buspirone.
CabazitaxelThe serum concentration of Axitinib can be increased when it is combined with Cabazitaxel.
CaffeineThe serum concentration of Axitinib can be increased when it is combined with Caffeine.
CanagliflozinThe serum concentration of Axitinib can be increased when it is combined with Canagliflozin.
CandesartanThe serum concentration of Axitinib can be increased when it is combined with Candesartan.
CaptoprilThe serum concentration of Axitinib can be increased when it is combined with Captopril.
CarbamazepineThe serum concentration of Axitinib can be decreased when it is combined with Carbamazepine.
CarvedilolThe serum concentration of Axitinib can be increased when it is combined with Carvedilol.
CaspofunginThe serum concentration of Axitinib can be increased when it is combined with Caspofungin.
CeritinibThe serum concentration of Axitinib can be increased when it is combined with Ceritinib.
ChloramphenicolThe metabolism of Axitinib can be decreased when combined with Chloramphenicol.
ChloroquineThe serum concentration of Axitinib can be increased when it is combined with Chloroquine.
ChlorpromazineThe serum concentration of Axitinib can be increased when it is combined with Chlorpromazine.
ChlorpropamideThe serum concentration of Axitinib can be increased when it is combined with Chlorpropamide.
ChlorprothixeneThe serum concentration of Axitinib can be increased when it is combined with Chlorprothixene.
CholecalciferolThe metabolism of Axitinib can be decreased when combined with Cholecalciferol.
CholesterolThe serum concentration of Axitinib can be increased when it is combined with Cholesterol.
Cholic AcidThe serum concentration of Axitinib can be decreased when it is combined with Cholic Acid.
CilazaprilThe serum concentration of Axitinib can be increased when it is combined with Cilazapril.
CimetidineThe serum concentration of Axitinib can be decreased when it is combined with Cimetidine.
CiprofloxacinThe serum concentration of Axitinib can be increased when it is combined with Ciprofloxacin.
CitalopramThe serum concentration of Axitinib can be increased when it is combined with Citalopram.
ClarithromycinThe serum concentration of Axitinib can be increased when it is combined with Clarithromycin.
ClemastineThe metabolism of Axitinib can be decreased when combined with Clemastine.
ClofazimineThe serum concentration of Axitinib can be increased when it is combined with Clofazimine.
ClomipramineThe serum concentration of Axitinib can be increased when it is combined with Clomipramine.
ClotrimazoleThe metabolism of Axitinib can be decreased when combined with Clotrimazole.
CobicistatThe serum concentration of Axitinib can be increased when it is combined with Cobicistat.
ColchicineThe serum concentration of Axitinib can be increased when it is combined with Colchicine.
ColforsinThe serum concentration of Axitinib can be increased when it is combined with Colforsin.
ConivaptanThe serum concentration of Axitinib can be increased when it is combined with Conivaptan.
CrizotinibThe metabolism of Axitinib can be decreased when combined with Crizotinib.
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Axitinib.
CyclosporineThe metabolism of Axitinib can be decreased when combined with Cyclosporine.
Cyproterone acetateThe serum concentration of Axitinib can be decreased when it is combined with Cyproterone acetate.
DabrafenibThe serum concentration of Axitinib can be decreased when it is combined with Dabrafenib.
DaclatasvirThe serum concentration of Axitinib can be increased when it is combined with Daclatasvir.
DactinomycinThe serum concentration of Axitinib can be increased when it is combined with Dactinomycin.
DarunavirThe serum concentration of Axitinib can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Axitinib can be increased when it is combined with Dasatinib.
DaunorubicinThe serum concentration of Axitinib can be decreased when it is combined with Daunorubicin.
DeferasiroxThe serum concentration of Axitinib can be decreased when it is combined with Deferasirox.
DelavirdineThe metabolism of Axitinib can be decreased when combined with Delavirdine.
DesipramineThe serum concentration of Axitinib can be increased when it is combined with Desipramine.
DeslanosideDeslanoside may decrease the cardiotoxic activities of Axitinib.
DesloratadineThe serum concentration of Axitinib can be increased when it is combined with Desloratadine.
DexamethasoneThe serum concentration of Axitinib can be decreased when it is combined with Dexamethasone.
DextromethorphanThe serum concentration of Axitinib can be increased when it is combined with Dextromethorphan.
DiclofenacThe serum concentration of Axitinib can be increased when it is combined with Diclofenac.
DigitoxinDigitoxin may decrease the cardiotoxic activities of Axitinib.
DigoxinDigoxin may decrease the cardiotoxic activities of Axitinib.
DihydroergotamineThe metabolism of Axitinib can be decreased when combined with Dihydroergotamine.
DiltiazemThe metabolism of Axitinib can be decreased when combined with Diltiazem.
DipyridamoleThe serum concentration of Axitinib can be increased when it is combined with Dipyridamole.
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Axitinib.
DoxazosinThe serum concentration of Axitinib can be increased when it is combined with Doxazosin.
DoxepinThe serum concentration of Axitinib can be increased when it is combined with Doxepin.
DoxorubicinThe serum concentration of Axitinib can be decreased when it is combined with Doxorubicin.
DoxycyclineThe metabolism of Axitinib can be decreased when combined with Doxycycline.
DronabinolThe serum concentration of Axitinib can be increased when it is combined with Dronabinol.
DronedaroneThe metabolism of Axitinib can be decreased when combined with Dronedarone.
EfavirenzThe serum concentration of Axitinib can be decreased when it is combined with Efavirenz.
ElbasvirThe serum concentration of Axitinib can be increased when it is combined with Elbasvir.
EltrombopagThe serum concentration of Axitinib can be increased when it is combined with Eltrombopag.
EnalaprilThe serum concentration of Axitinib can be increased when it is combined with Enalapril.
EnzalutamideThe serum concentration of Axitinib can be decreased when it is combined with Enzalutamide.
ErgonovineThe serum concentration of Axitinib can be increased when it is combined with Ergonovine.
ErgotamineThe serum concentration of Axitinib can be increased when it is combined with Ergotamine.
ErythromycinThe metabolism of Axitinib can be decreased when combined with Erythromycin.
Eslicarbazepine acetateThe serum concentration of Axitinib can be decreased when it is combined with Eslicarbazepine acetate.
EsomeprazoleThe metabolism of Axitinib can be decreased when combined with Esomeprazole.
EstramustineThe serum concentration of Axitinib can be increased when it is combined with Estramustine.
EstriolThe serum concentration of Axitinib can be decreased when it is combined with Estriol.
EstroneThe serum concentration of Axitinib can be decreased when it is combined with Estrone.
EtoposideThe serum concentration of Axitinib can be increased when it is combined with Etoposide.
EtravirineThe serum concentration of Axitinib can be decreased when it is combined with Etravirine.
FelodipineThe serum concentration of Axitinib can be increased when it is combined with Felodipine.
FentanylThe serum concentration of Axitinib can be increased when it is combined with Fentanyl.
FexofenadineThe serum concentration of Axitinib can be increased when it is combined with Fexofenadine.
FidaxomicinThe serum concentration of Axitinib can be increased when it is combined with Fidaxomicin.
FluconazoleThe metabolism of Axitinib can be decreased when combined with Fluconazole.
FluoxetineThe serum concentration of Axitinib can be increased when it is combined with Fluoxetine.
FlupentixolThe serum concentration of Axitinib can be increased when it is combined with Flupentixol.
FluphenazineThe serum concentration of Axitinib can be increased when it is combined with Fluphenazine.
FlurazepamThe serum concentration of Axitinib can be increased when it is combined with Flurazepam.
FluvoxamineThe metabolism of Axitinib can be decreased when combined with Fluvoxamine.
FosamprenavirThe metabolism of Axitinib can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Axitinib can be increased when it is combined with Fosaprepitant.
FosphenytoinThe serum concentration of Axitinib can be decreased when it is combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Axitinib can be increased when it is combined with Fusidic Acid.
GefitinibThe serum concentration of Axitinib can be increased when it is combined with Gefitinib.
GemfibrozilThe metabolism of Axitinib can be decreased when combined with Gemfibrozil.
GenisteinThe serum concentration of Axitinib can be increased when it is combined with Genistein.
GlyburideThe serum concentration of Axitinib can be increased when it is combined with Glyburide.
GlycerolThe serum concentration of Axitinib can be increased when it is combined with Glycerol.
Gramicidin DThe serum concentration of Axitinib can be increased when it is combined with Gramicidin D.
GrepafloxacinThe serum concentration of Axitinib can be increased when it is combined with Grepafloxacin.
HaloperidolThe serum concentration of Axitinib can be increased when it is combined with Haloperidol.
HydrocortisoneThe serum concentration of Axitinib can be increased when it is combined with Hydrocortisone.
IdelalisibThe serum concentration of Axitinib can be increased when it is combined with Idelalisib.
ImatinibThe metabolism of Axitinib can be decreased when combined with Imatinib.
ImipramineThe serum concentration of Axitinib can be increased when it is combined with Imipramine.
IndinavirThe serum concentration of Axitinib can be increased when it is combined with Indinavir.
IndomethacinThe serum concentration of Axitinib can be increased when it is combined with Indomethacin.
IsavuconazoniumThe metabolism of Axitinib can be decreased when combined with Isavuconazonium.
IsoniazidThe metabolism of Axitinib can be decreased when combined with Isoniazid.
IsradipineThe metabolism of Axitinib can be decreased when combined with Isradipine.
ItraconazoleThe serum concentration of Axitinib can be increased when it is combined with Itraconazole.
IvacaftorThe serum concentration of Axitinib can be increased when it is combined with Ivacaftor.
IvermectinThe serum concentration of Axitinib can be increased when it is combined with Ivermectin.
KetamineThe serum concentration of Axitinib can be increased when it is combined with Ketamine.
KetoconazoleThe serum concentration of Axitinib can be increased when it is combined with Ketoconazole.
LansoprazoleThe serum concentration of Axitinib can be increased when it is combined with Lansoprazole.
LapatinibThe serum concentration of Axitinib can be increased when it is combined with Lapatinib.
LevofloxacinThe serum concentration of Axitinib can be increased when it is combined with Levofloxacin.
LevothyroxineThe serum concentration of Axitinib can be decreased when it is combined with Levothyroxine.
LidocaineThe serum concentration of Axitinib can be increased when it is combined with Lidocaine.
LiothyronineThe serum concentration of Axitinib can be decreased when it is combined with Liothyronine.
LiotrixThe serum concentration of Axitinib can be decreased when it is combined with Liotrix.
LisinoprilThe serum concentration of Axitinib can be increased when it is combined with Lisinopril.
LomitapideThe serum concentration of Axitinib can be increased when it is combined with Lomitapide.
LoperamideThe serum concentration of Axitinib can be increased when it is combined with Loperamide.
LopinavirThe serum concentration of Axitinib can be increased when it is combined with Lopinavir.
LoratadineThe serum concentration of Axitinib can be increased when it is combined with Loratadine.
LosartanThe serum concentration of Axitinib can be increased when it is combined with Losartan.
LovastatinThe metabolism of Axitinib can be decreased when combined with Lovastatin.
LuliconazoleThe serum concentration of Axitinib can be increased when it is combined with Luliconazole.
LumacaftorThe serum concentration of Axitinib can be decreased when it is combined with Lumacaftor.
MaprotilineThe serum concentration of Axitinib can be increased when it is combined with Maprotiline.
MebendazoleThe serum concentration of Axitinib can be increased when it is combined with Mebendazole.
MefloquineThe serum concentration of Axitinib can be increased when it is combined with Mefloquine.
Megestrol acetateThe serum concentration of Axitinib can be increased when it is combined with Megestrol acetate.
MeprobamateThe serum concentration of Axitinib can be increased when it is combined with Meprobamate.
MethadoneThe serum concentration of Axitinib can be increased when it is combined with Methadone.
MetoprololThe serum concentration of Axitinib can be increased when it is combined with Metoprolol.
MexiletineThe metabolism of Axitinib can be decreased when combined with Mexiletine.
MibefradilThe serum concentration of Axitinib can be increased when it is combined with Mibefradil.
MiconazoleThe serum concentration of Axitinib can be increased when it is combined with Miconazole.
MidazolamThe serum concentration of Axitinib can be decreased when it is combined with Midazolam.
MifepristoneThe metabolism of Axitinib can be decreased when combined with Mifepristone.
MitomycinThe serum concentration of Axitinib can be increased when it is combined with Mitomycin.
MitotaneThe serum concentration of Axitinib can be decreased when it is combined with Mitotane.
MitoxantroneThe serum concentration of Axitinib can be decreased when it is combined with Mitoxantrone.
MoclobemideThe metabolism of Axitinib can be decreased when combined with Moclobemide.
ModafinilThe serum concentration of Axitinib can be decreased when it is combined with Modafinil.
MorphineThe serum concentration of Axitinib can be increased when it is combined with Morphine.
NafcillinThe serum concentration of Axitinib can be decreased when it is combined with Nafcillin.
NaltrexoneThe serum concentration of Axitinib can be increased when it is combined with Naltrexone.
NaringeninThe serum concentration of Axitinib can be increased when it is combined with Naringenin.
NefazodoneThe serum concentration of Axitinib can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Axitinib can be increased when it is combined with Nelfinavir.
NeostigmineThe serum concentration of Axitinib can be increased when it is combined with Neostigmine.
NetupitantThe serum concentration of Axitinib can be increased when it is combined with Netupitant.
NevirapineThe serum concentration of Axitinib can be decreased when it is combined with Nevirapine.
NicardipineThe serum concentration of Axitinib can be increased when it is combined with Nicardipine.
NifedipineThe serum concentration of Axitinib can be decreased when it is combined with Nifedipine.
NilotinibThe metabolism of Axitinib can be decreased when combined with Nilotinib.
NisoldipineThe serum concentration of Axitinib can be increased when it is combined with Nisoldipine.
NitrazepamThe serum concentration of Axitinib can be increased when it is combined with Nitrazepam.
NitrendipineThe serum concentration of Axitinib can be increased when it is combined with Nitrendipine.
NorethisteroneThe serum concentration of Axitinib can be decreased when it is combined with Norethisterone.
OlaparibThe metabolism of Axitinib can be decreased when combined with Olaparib.
OmeprazoleThe serum concentration of Axitinib can be increased when it is combined with Omeprazole.
OsimertinibThe serum concentration of Axitinib can be increased when it is combined with Osimertinib.
OuabainOuabain may decrease the cardiotoxic activities of Axitinib.
P-NitrophenolThe serum concentration of Axitinib can be increased when it is combined with P-Nitrophenol.
PaclitaxelThe serum concentration of Axitinib can be increased when it is combined with Paclitaxel.
PalbociclibThe serum concentration of Axitinib can be increased when it is combined with Palbociclib.
Palmitic AcidThe serum concentration of Axitinib can be increased when it is combined with Palmitic Acid.
PantoprazoleThe serum concentration of Axitinib can be increased when it is combined with Pantoprazole.
ParoxetineThe serum concentration of Axitinib can be increased when it is combined with Paroxetine.
Peginterferon alfa-2bThe serum concentration of Axitinib can be increased when it is combined with Peginterferon alfa-2b.
PentobarbitalThe serum concentration of Axitinib can be decreased when it is combined with Pentobarbital.
PerindoprilThe serum concentration of Axitinib can be increased when it is combined with Perindopril.
PhenobarbitalThe serum concentration of Axitinib can be decreased when it is combined with Phenobarbital.
PhenytoinThe serum concentration of Axitinib can be decreased when it is combined with Phenytoin.
PimozideThe serum concentration of Axitinib can be increased when it is combined with Pimozide.
Platelet Activating FactorThe serum concentration of Axitinib can be decreased when it is combined with Platelet Activating Factor.
PonatinibThe serum concentration of Axitinib can be increased when it is combined with Ponatinib.
PosaconazoleThe serum concentration of Axitinib can be increased when it is combined with Posaconazole.
PravastatinThe serum concentration of Axitinib can be increased when it is combined with Pravastatin.
PrazosinThe serum concentration of Axitinib can be increased when it is combined with Prazosin.
PrednisoneThe serum concentration of Axitinib can be increased when it is combined with Prednisone.
PrimidoneThe serum concentration of Axitinib can be decreased when it is combined with Primidone.
ProbenecidThe serum concentration of Axitinib can be increased when it is combined with Probenecid.
ProgesteroneThe serum concentration of Axitinib can be decreased when it is combined with Progesterone.
PromethazineThe serum concentration of Axitinib can be increased when it is combined with Promethazine.
PropafenoneThe serum concentration of Axitinib can be increased when it is combined with Propafenone.
PropranololThe serum concentration of Axitinib can be increased when it is combined with Propranolol.
ProtriptylineThe serum concentration of Axitinib can be increased when it is combined with Protriptyline.
QuercetinThe serum concentration of Axitinib can be increased when it is combined with Quercetin.
QuinacrineThe serum concentration of Axitinib can be increased when it is combined with Quinacrine.
QuinidineThe serum concentration of Axitinib can be increased when it is combined with Quinidine.
QuinineThe serum concentration of Axitinib can be increased when it is combined with Quinine.
RanitidineThe serum concentration of Axitinib can be increased when it is combined with Ranitidine.
RanolazineThe serum concentration of Axitinib can be increased when it is combined with Ranolazine.
ReboxetineThe serum concentration of Axitinib can be increased when it is combined with Reboxetine.
RegorafenibThe serum concentration of Axitinib can be increased when it is combined with Regorafenib.
ReserpineThe serum concentration of Axitinib can be decreased when it is combined with Reserpine.
RifabutinThe serum concentration of Axitinib can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Axitinib can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Axitinib can be decreased when it is combined with Rifapentine.
RilpivirineThe serum concentration of Axitinib can be increased when it is combined with Rilpivirine.
RitonavirThe serum concentration of Axitinib can be increased when it is combined with Ritonavir.
RolapitantThe serum concentration of Axitinib can be increased when it is combined with Rolapitant.
RopiniroleThe metabolism of Axitinib can be decreased when combined with Ropinirole.
SaquinavirThe serum concentration of Axitinib can be increased when it is combined with Saquinavir.
ScopolamineThe serum concentration of Axitinib can be increased when it is combined with Scopolamine.
SelegilineThe serum concentration of Axitinib can be increased when it is combined with Selegiline.
SertralineThe serum concentration of Axitinib can be increased when it is combined with Sertraline.
SildenafilThe metabolism of Axitinib can be decreased when combined with Sildenafil.
SiltuximabThe serum concentration of Axitinib can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Axitinib can be increased when it is combined with Simeprevir.
SimvastatinThe serum concentration of Axitinib can be increased when it is combined with Simvastatin.
SirolimusThe serum concentration of Axitinib can be decreased when it is combined with Sirolimus.
SorafenibThe serum concentration of Axitinib can be increased when it is combined with Sorafenib.
SpironolactoneThe serum concentration of Axitinib can be increased when it is combined with Spironolactone.
St. John's WortThe serum concentration of Axitinib can be decreased when it is combined with St. John's Wort.
StaurosporineThe serum concentration of Axitinib can be increased when it is combined with Staurosporine.
StiripentolThe serum concentration of Axitinib can be increased when it is combined with Stiripentol.
StreptozocinThe serum concentration of Axitinib can be decreased when it is combined with Streptozocin.
SulfinpyrazoneThe serum concentration of Axitinib can be increased when it is combined with Sulfinpyrazone.
SulfisoxazoleThe metabolism of Axitinib can be decreased when combined with Sulfisoxazole.
SumatriptanThe serum concentration of Axitinib can be increased when it is combined with Sumatriptan.
SunitinibThe serum concentration of Axitinib can be increased when it is combined with Sunitinib.
TacrineThe serum concentration of Axitinib can be increased when it is combined with Tacrine.
TacrolimusThe serum concentration of Axitinib can be decreased when it is combined with Tacrolimus.
TamoxifenThe serum concentration of Axitinib can be decreased when it is combined with Tamoxifen.
Taurocholic AcidThe serum concentration of Axitinib can be increased when it is combined with Taurocholic Acid.
TelaprevirThe serum concentration of Axitinib can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Axitinib can be increased when it is combined with Telithromycin.
TelmisartanThe serum concentration of Axitinib can be increased when it is combined with Telmisartan.
TemsirolimusThe serum concentration of Axitinib can be increased when it is combined with Temsirolimus.
TenofovirThe metabolism of Axitinib can be decreased when combined with Tenofovir.
TerazosinThe serum concentration of Axitinib can be increased when it is combined with Terazosin.
TerfenadineThe serum concentration of Axitinib can be increased when it is combined with Terfenadine.
TeriflunomideThe serum concentration of Axitinib can be increased when it is combined with Teriflunomide.
TesmilifeneThe serum concentration of Axitinib can be decreased when it is combined with Tesmilifene.
TestosteroneThe serum concentration of Axitinib can be increased when it is combined with Testosterone.
TheophyllineThe metabolism of Axitinib can be decreased when combined with Theophylline.
TicagrelorThe serum concentration of Axitinib can be increased when it is combined with Ticagrelor.
TiclopidineThe metabolism of Axitinib can be decreased when combined with Ticlopidine.
TocilizumabThe serum concentration of Axitinib can be decreased when it is combined with Tocilizumab.
TolvaptanThe serum concentration of Axitinib can be increased when it is combined with Tolvaptan.
TopiramateThe metabolism of Axitinib can be decreased when combined with Topiramate.
TranylcypromineThe metabolism of Axitinib can be decreased when combined with Tranylcypromine.
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Axitinib.
TrazodoneThe serum concentration of Axitinib can be decreased when it is combined with Trazodone.
TrifluoperazineThe serum concentration of Axitinib can be increased when it is combined with Trifluoperazine.
TriflupromazineThe serum concentration of Axitinib can be increased when it is combined with Triflupromazine.
TrimethoprimThe serum concentration of Axitinib can be decreased when it is combined with Trimethoprim.
TrimipramineThe serum concentration of Axitinib can be increased when it is combined with Trimipramine.
TroleandomycinThe serum concentration of Axitinib can be increased when it is combined with Troleandomycin.
VemurafenibThe serum concentration of Axitinib can be increased when it is combined with Vemurafenib.
VenlafaxineThe metabolism of Axitinib can be decreased when combined with Venlafaxine.
VerapamilThe metabolism of Axitinib can be decreased when combined with Verapamil.
VinblastineThe serum concentration of Axitinib can be decreased when it is combined with Vinblastine.
VincristineThe serum concentration of Axitinib can be decreased when it is combined with Vincristine.
VinorelbineThe serum concentration of Axitinib can be increased when it is combined with Vinorelbine.
VoriconazoleThe serum concentration of Axitinib can be increased when it is combined with Voriconazole.
ZimelidineThe serum concentration of Axitinib can be increased when it is combined with Zimelidine.
ZiprasidoneThe metabolism of Axitinib can be decreased when combined with Ziprasidone.
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.

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 ]
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Drug created on March 19, 2008 10:41 / Updated on September 27, 2016 02:27