title: Selective VEGFR inhibitors for anticancer therapeutics in clinical use and clinical trials.
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.
authors.affiliation: Graduate School at Shenzhen, Tsinghua University, Shenzhen 518055, China.
authors.forename: Cunlong
authors.initials: C
authors.lastname: Zhang
authors.forename: Chunyan
authors.initials: C
authors.lastname: Tan
authors.forename: Huaiwei
authors.initials: H
authors.lastname: Ding
authors.forename: Tian
authors.initials: T
authors.lastname: Xin
authors.forename: Yuyang
authors.initials: Y
authors.lastname: Jiang
mesh_terms: D020533:Angiogenesis Inhibitors / Q000494:pharmacology*; D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology; D015195:Drug Design; D006801:Humans; D009369:Neoplasms / Q000098:blood supply / Q000188:drug therapy; D009389:Neovascularization, Pathologic / Q000188:drug therapy / Q000473:pathology; D047428:Protein Kinase Inhibitors / Q000494:pharmacology*; D040262:Receptors, Vascular Endothelial Growth Factor / Q000037:antagonists & inhibitors* / Q000378:metabolism; D015398:Signal Transduction / Q000187:drug effects; D042461:Vascular Endothelial Growth Factor A / Q000037:antagonists & inhibitors
chemical_list: D020533:Angiogenesis Inhibitors; D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D042461:Vascular Endothelial Growth Factor A; D040262:Receptors, Vascular Endothelial Growth Factor