期刊
EXPERT OPINION ON INVESTIGATIONAL DRUGS
卷 21, 期 12, 页码 1851-1859出版社
TAYLOR & FRANCIS LTD
DOI: 10.1517/13543784.2012.733695
关键词
AV-951; breast cancer; gastrointestinal; phase I; renal cell carcinoma; tivozanib
资金
- NCI NIH HHS [K12 2K12CA001727-16A1, K12 CA001727] Funding Source: Medline
Introduction: Tivozanib is a novel tyrosine kinase inhibitor (TKI) which inhibits vascular endothelial growth factor (VEGF) receptors-1, -2, and -3 at nanomolar concentrations. Areas covered: A comprehensive MEDLINE and American Society of Clinical Oncology abstract search was performed to gather all relevant clinical and translational data related to tivozanib. We discuss pre-clinical studies associated with tivozanib, and the results of a Phase I assessment in advanced solid tumors. We highlight combination studies with tivozanib, including pairings of tivozanib with cytotoxic therapy in patients with colorectal cancer and breast cancer. A randomized discontinuation Phase II study and a randomized Phase III study assessing the activity of tivozanib in metastatic renal cell carcinoma (mRCC) are described in detail. Expert opinion: Tivozanib will face the challenge of entering an already crowded therapeutic space in mRCC-emerging combination studies and biomarker assessments may distinguish this agent among other VEGF-TKIs. The current review will outline the development pathway of tivozanib to date, and offer lessons learned and future opportunities.
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