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Identification
NamePazopanib
Accession NumberDB06589
TypeSmall Molecule
GroupsApproved
Description

Pazopanib is a small molecule inhibitor of multiple protein tyrosine kinases with potential antineoplastic activity. It is developed by GlaxoSmithKline and was FDA approved on October 19, 2009.

Structure
Thumb
Synonyms
GW 78603
GW786034
Pazopanibum
External Identifiers
  • GW-786034
  • GW786034
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Votrienttablet, film coated200 mg/1oralGlaxo Smith Kline Llc2009-10-19Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Votrienttablet200 mgoralNovartis Pharmaceuticals Canada Inc2010-08-13Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Votrienttablet400 mgoralNovartis Pharmaceuticals Canada IncNot applicableNot applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Generic Prescription ProductsNot Available
Over the Counter ProductsNot Available
International BrandsNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Pazopanib Hydrochloride
Thumb
  • InChI Key: MQHIQUBXFFAOMK-UHFFFAOYSA-N
  • Monoisotopic Mass: 473.140071444
  • Average Mass: 473.979
DBSALT000135
CategoriesNot Available
UNII7RN5DR86CK
CAS number444731-52-6
WeightAverage: 437.518
Monoisotopic: 437.163393705
Chemical FormulaC21H23N7O2S
InChI KeyInChIKey=CUIHSIWYWATEQL-UHFFFAOYSA-N
InChI
InChI=1S/C21H23N7O2S/c1-13-5-6-15(11-19(13)31(22,29)30)24-21-23-10-9-20(25-21)27(3)16-7-8-17-14(2)28(4)26-18(17)12-16/h5-12H,1-4H3,(H2,22,29,30)(H,23,24,25)
IUPAC Name
5-({4-[(2,3-dimethyl-2H-indazol-6-yl)(methyl)amino]pyrimidin-2-yl}amino)-2-methylbenzene-1-sulfonamide
SMILES
CN(C1=CC2=NN(C)C(C)=C2C=C1)C1=CC=NC(NC2=CC=C(C)C(=C2)S(N)(=O)=O)=N1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as alkyldiarylamines. These are tertiary alkylarylamines having two aryl and one alkyl groups attached to the amino group.
KingdomOrganic compounds
Super ClassOrganonitrogen compounds
ClassAmines
Sub ClassTertiary amines
Direct ParentAlkyldiarylamines
Alternative Parents
Substituents
  • Alkyldiarylamine
  • Benzenesulfonamide
  • Indazole
  • Benzopyrazole
  • Aminotoluene
  • Toluene
  • Aminopyrimidine
  • Imidolactam
  • Benzenoid
  • Pyrimidine
  • Monocyclic benzene moiety
  • Heteroaromatic compound
  • Aminosulfonyl compound
  • Sulfonyl
  • Sulfonic acid derivative
  • Sulfonamide
  • Pyrazole
  • Azole
  • Azacycle
  • Organoheterocyclic compound
  • Secondary amine
  • Hydrocarbon derivative
  • Organosulfur compound
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationTreatment of advanced renal cell cancer and advanced soft tissue sarcoma (in patients previously treated with chemotherapy)
PharmacodynamicsPazopanib is a synthetic indazolylpyrimidine and reaches steady state concentrations of >15 μg/ml. This concentration is high enough to observe maximal inhibition of VEGFR2 phosphorylation and some anti-tumour activity (concentration required to inhibit receptors is 0.01 - 0.084 μmol/L). A reduction in tumour blood flow, increased tumour apoptosis, inhibition of tumour growth, reduction in tumour interstitial fluid pressure, and hypoxia in cancer cells can be observed in patients receiving treatment.
Mechanism of actionPazopanib is a second-generation multitargeted tyrosine kinase inhibitor against vascular endothelial growth factor receptor-1, -2, and -3, platelet-derived growth factor receptor-alpha, platelet-derived growth factor receptor-beta, and c-kit. These receptor targets are part of the angiogenesis pathway that facilitates the formation of tumour blood vessel for tumour survival and growth.
AbsorptionAbsorption of pazopanib in cancer patients is slow and incomplete. In patients with solid tumour, over a dose range of 50-2000 mg, absorption is nonlinear. Significant accumulation of pazopanib can also be observed in patients receiving 800 mg once daily for 22 days. Crushing tablets may increase exposure (increase in Cmax and AUC, while Tmax decreases by 2 hours). Bioavailability, oral tablet 800 mg, cancer patient = 21%; Bioavailability may be low due to incomplete absorption from the gastrointestinal tract. The major circulating component of the drug in the systemic is pazopanib, and not its metabolites. Mean maximum plasma concentration= 58.1 µg/mL; Mean AUC= 1037 µg · h/mL;
Volume of distribution

Vd steady state, IV administration 5 mg, cancer patient = 11.1 L (range of 9.15 – 13.4)

Protein binding>99% protein bound, independent of concentrations over a range of 10-100 μg/mL.
Metabolism

Metabolized by CYP3A4 and to a lesser extent by CYP1A2 and CYP2C8. Metabolites are less active than pazopanib (10 to 20-fold less active). Three of its metabolites can be observed in the systemic and account for <10% of plasma radioactivity.

Route of eliminationPrimarily excreted via feces (82.2%) and to a negligible extent via urine (<4%) in cancer patients. Most of the administered dose is excreted unchanged. Approximately 10% of dose are oxidative metabolites and are mostly eliminated via the feces.
Half life35 hours. Oral absorption is not the rate limiting step of elimination from the plasma.
Clearance

CL, cancer patient, IV administration 5 mg = 4mL/min
Half of the absorbed dose is cleared via oxidative metabolism.

ToxicityNot Available
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 Absorption+1.0
Blood Brain Barrier+0.8788
Caco-2 permeable+0.5
P-glycoprotein substrateNon-substrate0.8307
P-glycoprotein inhibitor INon-inhibitor0.8126
P-glycoprotein inhibitor IIInhibitor0.5
Renal organic cation transporterNon-inhibitor0.8152
CYP450 2C9 substrateNon-substrate0.7797
CYP450 2D6 substrateNon-substrate0.8008
CYP450 3A4 substrateNon-substrate0.6024
CYP450 1A2 substrateNon-inhibitor0.5
CYP450 2C9 inhibitorNon-inhibitor0.5065
CYP450 2D6 inhibitorNon-inhibitor0.7779
CYP450 2C19 inhibitorNon-inhibitor0.6811
CYP450 3A4 inhibitorNon-inhibitor0.5385
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.5668
Ames testNon AMES toxic0.6543
CarcinogenicityNon-carcinogens0.8567
BiodegradationNot ready biodegradable0.9935
Rat acute toxicity2.3961 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9219
hERG inhibition (predictor II)Non-inhibitor0.7129
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Tabletoral200 mg
Tabletoral400 mg
Tablet, film coatedoral200 mg/1
PricesNot Available
Patents
CountryPatent NumberApprovedExpires (estimated)
United States71055302009-10-192023-10-19
United States72622032009-10-192021-12-19
United States81148852009-10-192021-12-19
Properties
StateSolid
Experimental PropertiesNot Available
Predicted Properties
PropertyValueSource
Water Solubility0.0433 mg/mLALOGPS
logP3.59ALOGPS
logP3.55ChemAxon
logS-4ALOGPS
pKa (Strongest Acidic)10.41ChemAxon
pKa (Strongest Basic)5.07ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count7ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area119.03 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity132.18 m3·mol-1ChemAxon
Polarizability45.41 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis ReferenceNot Available
General References
  1. Sonpavde G, Hutson TE, Sternberg CN: Pazopanib, a potent orally administered small-molecule multitargeted tyrosine kinase inhibitor for renal cell carcinoma. Expert Opin Investig Drugs. 2008 Feb;17(2):253-61. Pubmed
  2. Verweij J, Sleijfer S: Pazopanib , a new therapy for metastatic soft tissue sarcoma. Expert Opin Pharmacother. 2013 May;14(7):929-35. doi: 10.1517/14656566.2013.780030. Epub 2013 Mar 14. Pubmed
  3. Deng Y, Sychterz C, Suttle AB, Dar MM, Bershas D, Negash K, Qian Y, Chen EP, Gorycki PD, Ho MY: Bioavailability, metabolism and disposition of oral pazopanib in patients with advanced cancer. Xenobiotica. 2013 May;43(5):443-53. doi: 10.3109/00498254.2012.734642. Epub 2012 Nov 16. Pubmed
  4. Deeks ED: Pazopanib: in advanced soft tissue sarcoma. Drugs. 2012 Nov 12;72(16):2129-40. doi: 10.2165/11209950-000000000-00000. Pubmed
External Links
ATC CodesL01XE11
AHFS Codes
  • 10:00
PDB EntriesNot Available
FDA labelDownload (593 KB)
MSDSDownload (70.4 KB)
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Pazopanib can be increased when it is combined with Abiraterone.
Aluminum hydroxideThe serum concentration of Pazopanib can be decreased when it is combined with Aluminum hydroxide.
AmiodaroneThe serum concentration of Pazopanib can be increased when it is combined with Amiodarone.
AmodiaquineThe serum concentration of Amodiaquine can be increased when it is combined with Pazopanib.
AprepitantThe serum concentration of Pazopanib can be increased when it is combined with Aprepitant.
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Pazopanib.
AtazanavirThe serum concentration of Pazopanib can be increased when it is combined with Atazanavir.
AtorvastatinThe serum concentration of Pazopanib can be increased when it is combined with Atorvastatin.
AzithromycinThe serum concentration of Pazopanib can be increased when it is combined with Azithromycin.
BexaroteneThe serum concentration of Pazopanib can be decreased when it is combined with Bexarotene.
BoceprevirThe serum concentration of Pazopanib can be increased when it is combined with Boceprevir.
BosentanThe serum concentration of Pazopanib can be decreased when it is combined with Bosentan.
Calcium carbonateThe serum concentration of Pazopanib can be decreased when it is combined with Calcium carbonate.
CarbamazepineThe serum concentration of Pazopanib can be decreased when it is combined with Carbamazepine.
CarvedilolThe serum concentration of Pazopanib can be increased when it is combined with Carvedilol.
CeritinibThe serum concentration of Pazopanib can be increased when it is combined with Ceritinib.
CimetidineThe serum concentration of Pazopanib can be decreased when it is combined with Cimetidine.
CitalopramPazopanib may increase the QTc-prolonging activities of Citalopram.
ClarithromycinThe serum concentration of Pazopanib can be increased when it is combined with Clarithromycin.
CobicistatThe serum concentration of Pazopanib can be increased when it is combined with Cobicistat.
ConivaptanThe serum concentration of Pazopanib can be increased when it is combined with Conivaptan.
CrizotinibThe serum concentration of Pazopanib can be increased when it is combined with Crizotinib.
CyclosporineThe serum concentration of Pazopanib can be increased when it is combined with Cyclosporine.
DabrafenibThe serum concentration of Pazopanib can be increased when it is combined with Dabrafenib.
DaclatasvirThe serum concentration of Pazopanib can be increased when it is combined with Daclatasvir.
DarunavirThe serum concentration of Pazopanib can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Pazopanib can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Pazopanib can be decreased when it is combined with Deferasirox.
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Pazopanib.
DipyridamoleThe serum concentration of Pazopanib can be increased when it is combined with Dipyridamole.
DofetilidePazopanib may increase the QTc-prolonging activities of Dofetilide.
DronedaroneThe serum concentration of Pazopanib can be increased when it is combined with Dronedarone.
EliglustatThe serum concentration of Pazopanib can be increased when it is combined with Eliglustat.
EltrombopagThe serum concentration of Pazopanib can be increased when it is combined with Eltrombopag.
EnzalutamideThe serum concentration of Pazopanib can be decreased when it is combined with Enzalutamide.
ErythromycinThe serum concentration of Pazopanib can be increased when it is combined with Erythromycin.
EsomeprazoleThe serum concentration of Pazopanib can be decreased when it is combined with Esomeprazole.
FamotidineThe serum concentration of Pazopanib can be decreased when it is combined with Famotidine.
FlibanserinThe serum concentration of Pazopanib can be increased when it is combined with Flibanserin.
FluconazoleThe metabolism of Pazopanib can be decreased when combined with Fluconazole.
FluvastatinFluvastatin may increase the hepatotoxic activities of Pazopanib.
FosaprepitantThe serum concentration of Pazopanib can be increased when it is combined with Fosaprepitant.
FosphenytoinThe serum concentration of Pazopanib can be decreased when it is combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Pazopanib can be increased when it is combined with Fusidic Acid.
GefitinibThe serum concentration of Pazopanib can be increased when it is combined with Gefitinib.
GoserelinGoserelin may increase the QTc-prolonging activities of Pazopanib.
HydrocodoneThe serum concentration of Hydrocodone can be increased when it is combined with Pazopanib.
IbrutinibThe serum concentration of Pazopanib can be increased when it is combined with Ibrutinib.
IdelalisibThe serum concentration of Pazopanib can be increased when it is combined with Idelalisib.
ImatinibThe serum concentration of Pazopanib can be increased when it is combined with Imatinib.
IndinavirThe serum concentration of Pazopanib can be increased when it is combined with Indinavir.
IrinotecanThe serum concentration of the active metabolites of Irinotecan can be increased when Irinotecan is used in combination with Pazopanib.
ItraconazoleThe serum concentration of Pazopanib can be increased when it is combined with Itraconazole.
IvabradineIvabradine may increase the QTc-prolonging activities of Pazopanib.
IvacaftorThe serum concentration of Pazopanib can be increased when it is combined with Ivacaftor.
KetoconazoleThe serum concentration of Pazopanib can be increased when it is combined with Ketoconazole.
LansoprazoleThe serum concentration of Pazopanib can be decreased when it is combined with Lansoprazole.
LapatinibLapatinib may increase the QTc-prolonging activities of Pazopanib.
LeflunomideThe risk or severity of adverse effects can be increased when Pazopanib is combined with Leflunomide.
LeuprolideLeuprolide may increase the QTc-prolonging activities of Pazopanib.
LomitapideThe serum concentration of Pazopanib can be increased when it is combined with Lomitapide.
LovastatinLovastatin may increase the hepatotoxic activities of Pazopanib.
LuliconazoleThe serum concentration of Pazopanib can be increased when it is combined with Luliconazole.
Magnesium hydroxideThe serum concentration of Pazopanib can be decreased when it is combined with Magnesium hydroxide.
Magnesium oxideThe serum concentration of Pazopanib can be decreased when it is combined with Magnesium oxide.
MefloquineThe serum concentration of Pazopanib can be increased when it is combined with Mefloquine.
MifepristoneMifepristone may increase the QTc-prolonging activities of Pazopanib.
MirabegronThe serum concentration of Pazopanib can be increased when it is combined with Mirabegron.
MitotaneThe serum concentration of Pazopanib can be decreased when it is combined with Mitotane.
NatalizumabThe risk or severity of adverse effects can be increased when Pazopanib is combined with Natalizumab.
NefazodoneThe serum concentration of Pazopanib can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Pazopanib can be increased when it is combined with Nelfinavir.
NetupitantThe serum concentration of Pazopanib can be increased when it is combined with Netupitant.
NicardipineThe serum concentration of Pazopanib can be increased when it is combined with Nicardipine.
NilotinibThe serum concentration of Pazopanib can be increased when it is combined with Nilotinib.
NimodipineThe serum concentration of Nimodipine can be increased when it is combined with Pazopanib.
NizatidineThe serum concentration of Pazopanib can be decreased when it is combined with Nizatidine.
OctreotideOctreotide may increase the QTc-prolonging activities of Pazopanib.
OmeprazoleThe serum concentration of Pazopanib can be decreased when it is combined with Omeprazole.
PalbociclibThe serum concentration of Pazopanib can be increased when it is combined with Palbociclib.
PamidronateThe risk or severity of adverse effects can be increased when Pazopanib is combined with Pamidronate.
PantoprazoleThe serum concentration of Pazopanib can be increased when it is combined with Pantoprazole.
PhenobarbitalThe serum concentration of Pazopanib can be decreased when it is combined with Phenobarbital.
PhenytoinThe serum concentration of Pazopanib can be decreased when it is combined with Phenytoin.
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Pazopanib.
PimozideThe serum concentration of Pimozide can be increased when it is combined with Pazopanib.
PitavastatinPitavastatin may increase the hepatotoxic activities of Pazopanib.
PosaconazoleThe serum concentration of Pazopanib can be increased when it is combined with Posaconazole.
PravastatinPravastatin may increase the hepatotoxic activities of Pazopanib.
PrimidoneThe serum concentration of Pazopanib can be decreased when it is combined with Primidone.
ProgesteroneThe serum concentration of Pazopanib can be increased when it is combined with Progesterone.
PropranololThe serum concentration of Pazopanib can be increased when it is combined with Propranolol.
QuinidineThe serum concentration of Pazopanib can be increased when it is combined with Quinidine.
QuinineThe serum concentration of Pazopanib can be increased when it is combined with Quinine.
RabeprazoleThe serum concentration of Pazopanib can be decreased when it is combined with Rabeprazole.
RanitidineThe serum concentration of Pazopanib can be decreased when it is combined with Ranitidine.
RanolazineThe serum concentration of Pazopanib can be increased when it is combined with Ranolazine.
ReserpineThe serum concentration of Pazopanib can be increased when it is combined with Reserpine.
RifabutinThe serum concentration of Pazopanib can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Pazopanib can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Pazopanib can be decreased when it is combined with Rifapentine.
RitonavirThe serum concentration of Pazopanib can be increased when it is combined with Ritonavir.
RoflumilastRoflumilast may increase the immunosuppressive activities of Pazopanib.
RolapitantThe serum concentration of Pazopanib can be increased when it is combined with Rolapitant.
RosuvastatinRosuvastatin may increase the hepatotoxic activities of Pazopanib.
SaquinavirThe serum concentration of Pazopanib can be increased when it is combined with Saquinavir.
SiltuximabThe serum concentration of Pazopanib can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Pazopanib can be increased when it is combined with Simeprevir.
SimvastatinSimvastatin may increase the hepatotoxic activities of Pazopanib.
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Pazopanib.
Sodium bicarbonateThe serum concentration of Pazopanib can be decreased when it is combined with Sodium bicarbonate.
St. John's WortThe serum concentration of Pazopanib can be decreased when it is combined with St. John&#39;s Wort.
StiripentolThe serum concentration of Pazopanib can be increased when it is combined with Stiripentol.
SunitinibThe serum concentration of Pazopanib can be increased when it is combined with Sunitinib.
TacrolimusThe serum concentration of Pazopanib can be increased when it is combined with Tacrolimus.
TamoxifenThe serum concentration of Pazopanib can be increased when it is combined with Tamoxifen.
TelaprevirThe serum concentration of Pazopanib can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Pazopanib can be increased when it is combined with Telithromycin.
TeriflunomideThe serum concentration of Pazopanib can be increased when it is combined with Teriflunomide.
TesmilifeneThe serum concentration of Pazopanib can be decreased when it is combined with Tesmilifene.
TocilizumabThe serum concentration of Pazopanib can be decreased when it is combined with Tocilizumab.
TofacitinibPazopanib may increase the immunosuppressive activities of Tofacitinib.
TrastuzumabTrastuzumab may increase the neutropenic activities of Pazopanib.
VandetanibThe serum concentration of Pazopanib can be increased when it is combined with Vandetanib.
VemurafenibThe serum concentration of Pazopanib can be increased when it is combined with Vemurafenib.
VerapamilThe serum concentration of Pazopanib can be increased when it is combined with Verapamil.
VoriconazoleThe serum concentration of Pazopanib can be increased when it is combined with Voriconazole.
Food Interactions
  • Avoid drinking grapefruit juice as it is a CYP 3A4 inhibitor and will increase exposure of pazopanib
  • Bioavailability increases with food. Take pazopanib on empty stomach.

Targets

1. Vascular endothelial growth factor receptor 1

Kind: Protein

Organism: Human

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
Vascular endothelial growth factor receptor 1 P17948 Details

References:

  1. Sonpavde G, Hutson TE: Pazopanib: a novel multitargeted tyrosine kinase inhibitor. Curr Oncol Rep. 2007 Mar;9(2):115-9. Pubmed

2. Vascular endothelial growth factor receptor 2

Kind: Protein

Organism: Human

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
Vascular endothelial growth factor receptor 2 P35968 Details

References:

  1. Sonpavde G, Hutson TE: Pazopanib: a novel multitargeted tyrosine kinase inhibitor. Curr Oncol Rep. 2007 Mar;9(2):115-9. Pubmed

3. Vascular endothelial growth factor receptor 3

Kind: Protein

Organism: Human

Pharmacological action: yes

Components

Name UniProt ID Details
Vascular endothelial growth factor receptor 3 P35916 Details

References:

  1. Sonpavde G, Hutson TE: Pazopanib: a novel multitargeted tyrosine kinase inhibitor. Curr Oncol Rep. 2007 Mar;9(2):115-9. Pubmed

4. Platelet-derived growth factor receptor alpha

Kind: Protein

Organism: Human

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
Platelet-derived growth factor receptor alpha P16234 Details

References:

  1. Sonpavde G, Hutson TE: Pazopanib: a novel multitargeted tyrosine kinase inhibitor. Curr Oncol Rep. 2007 Mar;9(2):115-9. Pubmed

5. Platelet-derived growth factor receptor beta

Kind: Protein

Organism: Human

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
Platelet-derived growth factor receptor beta P09619 Details

References:

  1. Sonpavde G, Hutson TE: Pazopanib: a novel multitargeted tyrosine kinase inhibitor. Curr Oncol Rep. 2007 Mar;9(2):115-9. Pubmed

6. Mast/stem cell growth factor receptor Kit

Kind: Protein

Organism: Human

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
Mast/stem cell growth factor receptor Kit P10721 Details

References:

  1. Sonpavde G, Hutson TE: Pazopanib: a novel multitargeted tyrosine kinase inhibitor. Curr Oncol Rep. 2007 Mar;9(2):115-9. Pubmed

7. Fibroblast growth factor receptor 3

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Fibroblast growth factor receptor 3 P22607 Details

References:

  1. Deeks ED: Pazopanib: in advanced soft tissue sarcoma. Drugs. 2012 Nov 12;72(16):2129-40. doi: 10.2165/11209950-000000000-00000. Pubmed

8. Tyrosine-protein kinase ITK/TSK

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Tyrosine-protein kinase ITK/TSK Q08881 Details

References:

  1. Deeks ED: Pazopanib: in advanced soft tissue sarcoma. Drugs. 2012 Nov 12;72(16):2129-40. doi: 10.2165/11209950-000000000-00000. Pubmed

9. Fibroblast growth factor 1

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Fibroblast growth factor 1 P05230 Details

References:

  1. Deeks ED: Pazopanib: in advanced soft tissue sarcoma. Drugs. 2012 Nov 12;72(16):2129-40. doi: 10.2165/11209950-000000000-00000. Pubmed

10. SH2B adapter protein 3

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
SH2B adapter protein 3 Q9UQQ2 Details

References:

  1. Deeks ED: Pazopanib: in advanced soft tissue sarcoma. Drugs. 2012 Nov 12;72(16):2129-40. doi: 10.2165/11209950-000000000-00000. Pubmed

Enzymes

1. Cytochrome P450 3A4

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Cytochrome P450 3A4 P08684 Details

References:

  1. Keisner SV, Shah SR: Pazopanib: the newest tyrosine kinase inhibitor for the treatment of advanced or metastatic renal cell carcinoma. Drugs. 2011 Mar 5;71(4):443-54. doi: 10.2165/11588960-000000000-00000. Pubmed
  2. Goh BC, Reddy NJ, Dandamudi UB, Laubscher KH, Peckham T, Hodge JP, Suttle AB, Arumugham T, Xu Y, Xu CF, Lager J, Dar MM, Lewis LD: An evaluation of the drug interaction potential of pazopanib, an oral vascular endothelial growth factor receptor tyrosine kinase inhibitor, using a modified Cooperstown 5+1 cocktail in patients with advanced solid tumors. Clin Pharmacol Ther. 2010 Nov;88(5):652-9. Epub 2010 Sep 29. Pubmed
  3. Verweij J, Sleijfer S: Pazopanib , a new therapy for metastatic soft tissue sarcoma. Expert Opin Pharmacother. 2013 May;14(7):929-35. doi: 10.1517/14656566.2013.780030. Epub 2013 Mar 14. Pubmed

2. Cytochrome P450 2D6

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 2D6 P10635 Details

References:

  1. Keisner SV, Shah SR: Pazopanib: the newest tyrosine kinase inhibitor for the treatment of advanced or metastatic renal cell carcinoma. Drugs. 2011 Mar 5;71(4):443-54. doi: 10.2165/11588960-000000000-00000. Pubmed
  2. Goh BC, Reddy NJ, Dandamudi UB, Laubscher KH, Peckham T, Hodge JP, Suttle AB, Arumugham T, Xu Y, Xu CF, Lager J, Dar MM, Lewis LD: An evaluation of the drug interaction potential of pazopanib, an oral vascular endothelial growth factor receptor tyrosine kinase inhibitor, using a modified Cooperstown 5+1 cocktail in patients with advanced solid tumors. Clin Pharmacol Ther. 2010 Nov;88(5):652-9. Epub 2010 Sep 29. Pubmed

3. Cytochrome P450 2C8

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 2C8 P10632 Details

References:

  1. Keisner SV, Shah SR: Pazopanib: the newest tyrosine kinase inhibitor for the treatment of advanced or metastatic renal cell carcinoma. Drugs. 2011 Mar 5;71(4):443-54. doi: 10.2165/11588960-000000000-00000. Pubmed
  2. Verweij J, Sleijfer S: Pazopanib , a new therapy for metastatic soft tissue sarcoma. Expert Opin Pharmacother. 2013 May;14(7):929-35. doi: 10.1517/14656566.2013.780030. Epub 2013 Mar 14. Pubmed

4. Cytochrome P450 1A2

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 1A2 P05177 Details

References:

  1. Verweij J, Sleijfer S: Pazopanib , a new therapy for metastatic soft tissue sarcoma. Expert Opin Pharmacother. 2013 May;14(7):929-35. doi: 10.1517/14656566.2013.780030. Epub 2013 Mar 14. Pubmed

Transporters

1. Multidrug resistance protein 1

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Multidrug resistance protein 1 P08183 Details

References:

  1. Deng Y, Sychterz C, Suttle AB, Dar MM, Bershas D, Negash K, Qian Y, Chen EP, Gorycki PD, Ho MY: Bioavailability, metabolism and disposition of oral pazopanib in patients with advanced cancer. Xenobiotica. 2013 May;43(5):443-53. doi: 10.3109/00498254.2012.734642. Epub 2012 Nov 16. Pubmed

2. ATP-binding cassette sub-family G member 2

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
ATP-binding cassette sub-family G member 2 Q9UNQ0 Details

References:

  1. Deng Y, Sychterz C, Suttle AB, Dar MM, Bershas D, Negash K, Qian Y, Chen EP, Gorycki PD, Ho MY: Bioavailability, metabolism and disposition of oral pazopanib in patients with advanced cancer. Xenobiotica. 2013 May;43(5):443-53. doi: 10.3109/00498254.2012.734642. Epub 2012 Nov 16. Pubmed

3. Solute carrier organic anion transporter family member 1B1

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier organic anion transporter family member 1B1 Q9Y6L6 Details

References:

  1. Deeks ED: Pazopanib: in advanced soft tissue sarcoma. Drugs. 2012 Nov 12;72(16):2129-40. doi: 10.2165/11209950-000000000-00000. Pubmed

4. UDP-glucuronosyltransferase 1-1

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
UDP-glucuronosyltransferase 1-1 P22309 Details

References:

  1. Deeks ED: Pazopanib: in advanced soft tissue sarcoma. Drugs. 2012 Nov 12;72(16):2129-40. doi: 10.2165/11209950-000000000-00000. Pubmed

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Drug created on March 19, 2008 10:38 / Updated on September 16, 2013 18:04