Description
Tivozanib (AV-951; KRN-951) is able to markedly inhibit VEGFR-1, VEGFR-2, VEGFR-3, c-Kit and PDGFR with IC50 of 0.21, 0.16, 0.24, 1.63 and 1.72 nM.
Storage
2 years at -20 centigrade
Targets
VEGFR-1, VEGFR-2, VEGFR-3, c-Kit, PDGFR
Molecular Formula
C22H19ClN4O5
Chemical Name
1-(2-chloro-4-(6,7-dimethoxyquinolin-4-yloxy)phenyl)-3-(5-methylisoxazol-3-yl)urea
Solubility
DSMO 20 mg/mL Water
In vitro
As an orally active, ATP-competitive, small-molecule, quinoline-urea derivative, Tivozanib (AV-951; KRN-951) is able to markedly inhibit VEGFR-1, VEGFR-2, VEGFR-3, c-Kit and PDGFR with IC50 of 0.21, 0.16, 0.24, 1.63 and 1.72 nM, respectively.
In vivo
Tivozanib produced a significant inhibition of tumor growth and angiogenesis in several different xenograft tumor models in athymic rats. In a phase I clinical trial, tivozanib was safe and tolerable when administered at oral doses up to 1.5 mg on a schedule of 4 weeks on, 2 weeks off treatment. Results from a phase II clinical trial in patients with advanced renal cell carcinoma reported an overall response rate of 25.4% and a median progression-free survival of 11.8 months in patients treated with tivozanib as a single agent. In a Phase II Randomized Discontinuation proved that tivozanib was active and well tolerated in patients with advanced RCC and supported additional development of tivozanib in advanced RCC.
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