Tivozanib
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| Names | |
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IUPAC name
1-{2-Chloro-4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-3-(5-methylisoxazol-3-yl)urea
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| Other names
AV-951
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| Identifiers | |
| 3D model (Jmol) | Interactive image |
| ChEMBL | ChEMBL1289494 |
| ChemSpider | 8087481 |
| 6058 | |
| PubChem | 9911830 |
| UNII |
172030934T 
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| Properties | |
| C22H19ClN4O5 | |
| Molar mass | 454.87 g·mol−1 |
| Pharmacology | |
| L01XE34 (WHO) | |
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Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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| Infobox references | |
Tivozanib (AV-951) is an oral VEGF receptor tyrosine kinase inhibitor. It completed a trial investigation for the treatment of renal cell carcinomas. The results did not result in FDA approval.
An oral quinoline urea derivative, tivozanib suppresses angiogenesis by being selectively inhibitory against vascular endothelial growth factor. It was developed by AVEO Pharmaceuticals. It is designed to inhibit all three VEGF receptors.
Phase III results on advanced renal cell carcinoma suggested a 30% or 3 months improvement in median PFS compared to sorafenib but showed an inferior overall survival rate of the experimental arm versus the control arm. The Food and Drug Administration's Oncologic Drugs Advisory Committee voted in May 2013 13 to 1 against recommending approval of tivozanib for renal cell carcinoma. The committee felt the drug failed to show a favorable risk-benefit ratio and questioned the equipose of the trial design, which allowed control arm patients who used sorafenib to transition to tivozanib following progression disease but not those on the experimental arm using tivozanib to transition to sorafenib. The application was formally rejected by the FDA in June 2013, saying that approval would require additional clinical studies.
In 2016 AVEO Oncology published data in conjunction with the ASCO meeting showing a geographical location effect on Overall Survival in the Pivotal PhIII trial
In 2016 AVEO Oncology announced the start of a second Pivotal PhIII clinical study in Third Line advanced RCC patients.
In 2016 EUSA Pharma and AVEO Oncology announced that Tivozanib had been submitted to the European Medicines Agency for review under the Centralised Procedure.
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