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Tivozanib(AV-951)

Tivozanib is an orally bioavailable inhibitor of vascular endothelial growth factor receptors (VEGFRs) 1, 2 and 3 with potential antiangiogenic and antineoplastic activities. Tivozanib binds to and inhibits VEGFRs 1, 2 and 3, which may result in the inhibition of endothelial cell migration and proliferation, inhibition of tumor angiogenesis and tumor cell death. VEGFR tyrosine kinases, frequently overexpressed by a variety of tumor cell types, play a key role in angiogenesis. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Current developer:  AVEO Pharmaceuticals, Inc. / Kirin Pharma (originator)

Antiturmor activity in clinical trials observed:  (1) Tivozanib demonstrated a statistically significant improvement in PFS with a median PFS of 11.9 months compared to a median PFS of 9.1 months for sorafenib in the overall study population. (2). Tivozanib demonstrated a statistically significant improvement in PFS with a median PFS of 12.7 months compared to a median PFS of 9.1 months for sorafenib in the pre-specified subpopulation of patients who were treatment naïve (no prior systemic anti-cancer therapy); this subpopulation was approximately 70% of the total study population. (3). Tivozanib demonstrated a well-tolerated safety profile consistent with the Phase 2 experience; the most commonly reported side effect was hypertension, a well established on-target and manageable effect of VEGFR inhibitors. (source: News-medical.net)

According to http://www.prnewswire.com, Decision Resources, one of the world's leading research and advisory firms for pharmaceutical and healthcare issues, finds that AVEO Pharmaceuticals' tivozanib, which is expected to launch in 2013 in the United States and Europe and in 2016 in Japan, will garner sales of up to $100 million by 2018 in the renal cell carcinoma drug market. 

1: Gross-Goupil M, Massard C, Ravaud A. Targeted therapies in metastatic renal cell carcinoma: overview of the past year. Curr Urol Rep. 2012 Feb;13(1):16-23. PubMed PMID: 22139625.

2: Gupta S, Fishman M. Progress and contrasts of the development of tivozanib for therapy of kidney cancer. Expert Opin Pharmacother. 2011 Dec;12(18):2915-22. PubMed PMID: 22098229.

3: Eskens FA, de Jonge MJ, Bhargava P, Isoe T, Cotreau MM, Esteves B, Hayashi K, Burger H, Thomeer M, van Doorn L, Verweij J. Biologic and clinical activity of tivozanib (AV-951, KRN-951), a selective inhibitor of VEGF receptor-1, -2, and -3 tyrosine kinases, in a 4-week-on, 2-week-off schedule in patients with advanced solid tumors. Clin Cancer Res. 2011 Nov 15;17(22):7156-63. Epub 2011 Oct 5. PubMed PMID: 21976547.

4: Coppin C, Kollmannsberger C, Le L, Porzsolt F, Wilt TJ. Targeted therapy for advanced renal cell cancer (RCC): a Cochrane systematic review of published randomised trials. BJU Int. 2011 Nov;108(10):1556-63. doi: 10.1111/j.1464-410X.2011.10629.x. Epub 2011 Sep 27. Review. PubMed PMID: 21952069.

5: Albiges L, Salem M, Rini B, Escudier B. Vascular endothelial growth factor-targeted therapies in advanced renal cell carcinoma. Hematol Oncol Clin North Am. 2011 Aug;25(4):813-33. Review. PubMed PMID: 21763969.

6: Négrier S, Raymond E. Antiangiogenic treatments and mechanisms of action in renal cell carcinoma. Invest New Drugs. 2011 May 15. [Epub ahead of print] PubMed PMID: 21573959.

7: Deal watch: Aveo and Astellas to develop VEGF inhibitor for renal cell carcinoma. Nat Rev Drug Discov. 2011 Apr;10(4):248. PubMed PMID: 21455225.

8: Bhargava P, Robinson MO. Development of second-generation VEGFR tyrosine kinase inhibitors: current status. Curr Oncol Rep. 2011 Apr;13(2):103-11. Review. PubMed PMID: 21318618; PubMed Central PMCID: PMC3047052.

9: Deissler HL, Deissler H, Lang GE. Inhibition of vascular endothelial growth factor (VEGF) is sufficient to completely restore barrier malfunction induced by growth factors in microvascular retinal endothelial cells. Br J Ophthalmol. 2011 Aug;95(8):1151-6. Epub 2011 Jan 27. PubMed PMID: 21273213.

10: De Luca A, Normanno N. Tivozanib, a pan-VEGFR tyrosine kinase inhibitor for the potential treatment of solid tumors. IDrugs. 2010 Sep;13(9):636-45. Review. Erratum in: IDrugs. 2010 Oct;13(10):742. Dosage error in article text. PubMed PMID: 20799147.

11: Heng DY, Kollmannsberger C, Chi KN. Targeted therapy for metastatic renal cell carcinoma: current treatment and future directions. Ther Adv Med Oncol. 2010 Jan;2(1):39-49. PubMed PMID: 21789125; PubMed Central PMCID: PMC3126007.