Chemical Property of Pazopanib
Chemical Property:
- Appearance/Colour:White powder
- Vapor Pressure:4.26E-21mmHg at 25°C
- Melting Point:285-289°C (dec.)
- Boiling Point:728.814 °C at 760 mmHg
- PKA:10.19±0.60(Predicted)
- Flash Point:394.572 °C
- PSA：127.41000
- Density:1.40 g/cm3
- LogP:4.99310
- Storage Temp.:Refrigerator
- Solubility.:Aqueous Acid (Slightly), DMSO (Slightly, Heated), Methanol (Slightly, Heated)
- XLogP3:3.1
- Hydrogen Bond Donor Count:2
- Hydrogen Bond Acceptor Count:8
- Rotatable Bond Count:5
- Exact Mass:437.16339418
- Heavy Atom Count:31
- Complexity:717
- Purity/Quality:
-
99%, *data from raw suppliers
Pazopanib *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- Statements:
43-62/63
- Safety Statements:
36/37/39-28B
- MSDS Files:
-
Useful:
- Drug Classes:Antineoplastic Agents
- Canonical SMILES:CC1=C(C=C(C=C1)NC2=NC=CC(=N2)N(C)C3=CC4=NN(C(=C4C=C3)C)C)S(=O)(=O)N
- Recent ClinicalTrials:Sequential Two-agent Assessment in Renal Cell Carcinoma Therapy: The START Trial
- Recent EU Clinical Trials:RAR-Immune: A randomised, comparative, prospective, multicentre study of the efficacy of nivolumab + ipilimumab versus pazopanib alone in patients with metastatic or unresectable advanced sarcoma of rare subtype
- Recent NIPH Clinical Trials:JCOG1802: A randomized phase II trial of 2nd line treatment for advanced soft tissue sarcoma comparing trabectedin, eribulin and pazopanib
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Description
Pazopanib is a multi-kinase inhibitor that inhibits the VEGF receptors VEGFR1, VEGFR2, and VEGFR3 (IC50s = 10, 30, and 47 nM, respectively, in a cell-free enzyme assay). It also inhibits PDGFRα, PDGFRβ, and c-Kit (IC50s = 71, 84, and 74 nM, respectively, in a cell-free enzyme assay) as well as additional receptor tyrosine kinases. Pazopanib inhibits upregulation of the surface adhesion proteins ICAM-1 and VCAM-1 induced by VEGF in multiple myeloma cells cocultured with human umbilical vein endothelial cells (HUVECs) and decreases multiple myeloma cell adhesion to HUVECs. It also inhibits proliferation of multiple myeloma cells cocultured with HUVECs. Pazopanib (30 and 100 mg/kg) reduces tumor growth, induces apoptosis, decreases angiogenesis, and increases survival in a multiple myeloma mouse xenograft model. Formulations containing pazopanib have been used in the treatment of cancer.
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Uses
Pazopanib Hydrochloride (GW786034, Votrient, Armala) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM, respectively. Pazopanib is a potent and selective multi-targeted receptor tyrosine kinase inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR-α/β, and c-Kit. Pazopanib is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM, respectively. An oral angiogenesis inhibitor targeting VEGFR and PDGFR.
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Clinical Use
Tyrosine kinase inhibitor:
Treatment of metastatic renal cell carcinoma and soft
tissue sarcoma
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Drug interactions
Potentially hazardous interactions with other drugs
Antibacterials: avoid with clarithromycin, rifampicin
and telithromycin.
Antifungals: avoid with itraconazole, ketoconazole
and voriconazole.
Antipsychotics: avoid with clozapine (increased risk
of agranulocytosis).
Antivirals: avoid with atazanavir, boceprevir,
indinavir, ritonavir and saquinavir.
Grapefruit juice: avoid concomitant administration.
Avoid concomitant use with other inhibitors or
inducers of CYP3A4. Dose alterations may be
required.
