Development of Second-Generation VEGFR Tyrosine Kinase Inhibitors: Current Status
- نوع فایل : کتاب
- زبان : انگلیسی
- مؤلف : Pankaj Bhargava & Murray O. Robinson
- چاپ و سال / کشور: 2011
Description
The vascular endothelial growth factor (VEGF) signaling pathway appears to be the dominant pathway involved in tumor angiogenesis, providing a rationale for targeting the VEGF receptors (VEGFR-1, -2, and -3) in the treatment of cancers. In particular, VEGF signaling is thought to be important in renal cell carcinoma (RCC) because of the deregulation of the pathway through nearly uniform loss of the von Hippel Lindau protein. The tyrosine kinase inhibitors (TKIs) sorafenib, sunitinib, and pazopanib are approved by the US Food and Drug Administration for the treatment of advanced RCC; however, these multitargeted agents inhibit a wide range of kinase targets in addition to the VEGFRs, resulting in a range of adverse effects unrelated to efficient VEGF blockade. This article reviews recent advances in the development of the secondgeneration VEGFR TKIs, including the more selective VEGFR TKIs tivozanib and axitinib, and focuses on the potential benefits of novel inhibitors with improved potency and selectivity
Curr Oncol Rep (2011) 13:103–111 DOI 10.1007/s11912-011-0154-3 Published online: 12 February 2011
