Selective VEGFR inhibitors for anticancer therapeutics in clinical use and clinical trials

Current Pharmaceutical Design
Cunlong ZhangYuyang Jiang

Abstract

Angiogenesis and vasculogenesis, regulated by VEGF/VEGFR signaling pathways, play key roles in tumor growth and metastasis. Selective inhibition of VEGFR kinase has been explored as a highly successful clinical strategy in cancer treatment. A number of VEGFR inhibitors have been approved in clinical use and many more are in various stages of drug development. This paper reviews selective small-molecule VEGFR inhibitors in clinical uses and in clinical trials, with particular focus on in vitro, in vivo and clinical trial results of these inhibitors. The VEGF/VEGFR genes and signaling pathways involved in tumor angiogenesis, and the strategies for accessing and improving the therapeutic efficacy of VEGFR inhibitors are also discussed.

Citations

Jun 19, 2013·Molecular Therapy : the Journal of the American Society of Gene Therapy·Yuan ZhangLeaf Huang
Nov 20, 2014·Future Medicinal Chemistry·Chao DingYuyang Jiang
Dec 3, 2015·Journal of Medicinal Chemistry·Guido BoldAmanda Littlewood-Evans
Jul 17, 2013·Molecular Cancer Therapeutics·Khalid A MohamedaliMichael G Rosenblum

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