Repositioning Candidate Details
| Candidate ID: | R1051 |
| Source ID: | DB06589 |
| Source Type: | approved |
| Compound Type: | small molecule |
| Compound Name: | Pazopanib |
| Synonyms: | -- |
| Molecular Formula: | C21H23N7O2S |
| SMILES: | CN(C1=CC2=NN(C)C(C)=C2C=C1)C1=CC=NC(NC2=CC=C(C)C(=C2)S(N)(=O)=O)=N1 |
| Structure: |
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| DrugBank 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. |
| CAS Number: | 444731-52-6 |
| Molecular Weight: | 437.518 |
| DrugBank Indication: | Treatment of advanced renal cell cancer and advanced soft tissue sarcoma (in patients previously treated with chemotherapy) |
| DrugBank Pharmacology: | Pazopanib 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. |
| DrugBank MoA: | Pazopanib 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. |
| Targets: | Vascular endothelial growth factor receptor 1 inhibitor; Vascular endothelial growth factor receptor 2 inhibitor; Vascular endothelial growth factor receptor 3; Platelet-derived growth factor receptor alpha inhibitor; Platelet-derived growth factor receptor beta inhibitor; Mast/stem cell growth factor receptor Kit inhibitor; Fibroblast growth factor receptor 3 inhibitor; Tyrosine-protein kinase ITK/TSK inhibitor; Fibroblast growth factor 1 inhibitor; SH2B adapter protein 3 inhibitor |
| Inclusion Criteria: | Therapeutic strategy associated |
