tivozanib
Tivozanib is an oral, once-daily, vascular endothelial growth factor (VEGF) tyrosine kinase inhibitor (TKI). It is a potent, selective and long half-life inhibitor of all three VEGF receptors and is designed to optimize VEGF blockade while minimizing off-target toxicities, potentially resulting in improved efficacy and minimal dose modifications. Tivozanib is indicated as first line treatment of adult patients with advanced renal cell carcinoma (RCC) and for adult patients who are VEGFR and mTOR pathway inhibitor-naive following disease progression after one prior treatment with cytokine therapy for advanced RCC.
Ligand Summary
UNII: 172030934T
PubChem: 9911830
Guide to Pharmacology: 6058
ChEMBL: CHEMBL1289494
DrugCentral: 5258
LyCHI: G8GCH7A2RSAN
Target Activities
KDR
Vascular endothelial growth factor receptor 2
5 Activities
Items per page:
1 – 5 of 5
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 9.8 | |||||
IC50 | 9.8 | Eur. J. Med. Chem., (2010) 45:11:5420 | ||||
IC50 | 9.8 | J. Med. Chem., (2012) 55:24:10797 | ||||
IC50 | 8.67 | Bioorg. Med. Chem. Lett., (2015) 25:11:2425 | ||||
IC50 | 9.8 | INHIBITOR | ||||
FLT1
Vascular endothelial growth factor receptor 1
4 Activities
Items per page:
1 – 4 of 4
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 9.68 | |||||
IC50 | 9.68 | J. Med. Chem., (2012) 55:24:10797 | ||||
IC50 | 8.2 | Bioorg. Med. Chem. Lett., (2015) 25:11:2425 | ||||
IC50 | 9.68 | INHIBITOR | ||||
FLT4
Vascular endothelial growth factor receptor 3
4 Activities
Items per page:
1 – 4 of 4
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 9.62 | |||||
IC50 | 9.62 | J. Med. Chem., (2012) 55:24:10797 | ||||
IC50 | 8.51 | Bioorg. Med. Chem. Lett., (2015) 25:11:2425 | ||||
IC50 | 9.62 | INHIBITOR | ||||
EPHB2
Ephrin type-B receptor 2
2 Activities
Items per page:
1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.76 | Bioorg. Med. Chem. Lett., (2015) 25:11:2425 | ||||
IC50 | 7.76 | |||||
PDGFRA
Platelet-derived growth factor receptor alpha
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 8.65 | Bioorg. Med. Chem. Lett., (2015) 25:11:2425 | ||||
BCR
Breakpoint cluster region protein
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 6.8 | Science, (2017) 358:6367:None | ||||
PEBP1
Phosphatidylethanolamine-binding protein 1
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 8.52 | Science, (2017) 358:6367:None | ||||
RET
Proto-oncogene tyrosine-protein kinase receptor Ret
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.92 | Science, (2017) 358:6367:None | ||||