tivozanib   Click here for help

GtoPdb Ligand ID: 6058

Synonyms: AV-951 | AV951 | Fotivda® | KRN-951 | KRN951 | VEGFR tyrosine kinase inhibitor IV
Approved drug PDB Ligand
tivozanib is an approved drug (EMA (2017), FDA (2021))
Compound class: Synthetic organic
Comment: Tivozanib is an oral VEGF receptor tyrosine kinase inhibitor.
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 4
Hydrogen bond donors 2
Rotatable bonds 8
Topological polar surface area 107.74
Molecular weight 454.1
XLogP 3.53
No. Lipinski's rules broken 0
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Canonical SMILES COc1cc2c(ccnc2cc1OC)Oc1ccc(c(c1)Cl)NC(=O)Nc1noc(c1)C
Isomeric SMILES COc1cc2c(ccnc2cc1OC)Oc1ccc(c(c1)Cl)NC(=O)Nc1noc(c1)C
InChI InChI=1S/C22H19ClN4O5/c1-12-8-21(27-32-12)26-22(28)25-16-5-4-13(9-15(16)23)31-18-6-7-24-17-11-20(30-3)19(29-2)10-14(17)18/h4-11H,1-3H3,(H2,25,26,27,28)
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Summary of Clinical Use Click here for help
Tivozanib was approved by the EMA in 2017, and it is also approved for use in Norway and Iceland. Tivozanib is indicated as a first line treatment of adult patients with advanced renal cell carcinoma (RCC) and for adult patients who are VEGFR and mTOR pathway inhibitor-naïve following disease progression after one prior treatment with cytokine therapy for advanced RCC.

Click here to view all tivozanib studies that are currently listed on ClinicalTrials.gov.

The first FDA approval for tivozanib was granted in March 2021; indicated for advanced RCC that has relapsed or is refractory following ≥2 systemic prior therapies.
Mechanism Of Action and Pharmacodynamic Effects Click here for help
Tivozanib selectively inhibits VEGFR activation which suppresses the downstream pro-angiogenic sequelae of VEGF activity at these receptor tyrosine linases.
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