tivozanib   

GtoPdb Ligand ID: 6058

Synonyms: AV-951 | AV951 | Fotivda® | KRN-951 | KRN951 | VEGFR tyrosine kinase inhibitor IV
tivozanib is an approved drug (EMA (2017))
Compound class: Synthetic organic
Comment: Tivozanib is an oral VEGF receptor tyrosine kinase inhibitor.
2D Structure
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Physico-chemical Properties
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
SMILES / InChI / InChIKey
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)
InChI Key SPMVMDHWKHCIDT-UHFFFAOYSA-N
No information available.
Summary of Clinical Use
Tivozanib was approved by the EMA in 2017, and it is also approved for use in Norway and Iceland. It is not FDA approved. 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.

A press release from the drug's developer Aveo Oncology, announced that the FDA would not recommend submission of a New Drug Application (NDA) for tivozanib for RCC with the preliminary overall survival results from the Phase 3 TIVO-3 trial (tivozanib vs sorafenib). Aveo is awaiting more mature overall survival results before making any further NDA filing decisions (as of July 2019).
Mechanism Of Action and Pharmacodynamic Effects
Tivozanib selectively inhibits VEGFR activation which suppresses the downstream pro-angiogenic sequelae of VEGF activity at these receptor tyrosine linases.
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