Brivanib, a novel dual VEGF-R2/bFGF-R inhibitor.
The process of neo-vascularisation from pre-existing blood vessels (angiogenesis) plays a critical role in both tumour growth and dissemination in multiple cancer types. Tumour angiogenesis is an attractive target for cancer treatment, and the VEGF/VEGF-R and FGF/FGF-R systems have been identified as key factors for neo-angiogenesis. Several active compounds have been developed so far and some of them are already widely used in clinical protocols. However, currently, only very few drugs have been shown to act synergistically with VEGF. Brivanib (BMS-582664) is a novel, orally available and selective receptor tyrosine kinase inhibitor that targets the key angiogenesis receptors VEGF-R2 and FGF-R1 and -2. The drug is currently under clinical evaluation and published data as well as data on biomarker studies with brivanib are reviewed and discussed.
Elbland Clinic Riesa, Medical Oncology, Weinbergstrasse 8, D-01589 Riesa, Germany. wolfram.dempke@elblandkliniken.de
Wolfram C M
WC
Dempke
Roland
R
Zippel
D000409:Alanine / Q000031:analogs & derivatives; D002986:Clinical Trials as Topic; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy*; D011758:Pyrroles / Q000494:pharmacology*; D051496:Receptor, Fibroblast Growth Factor, Type 1 / Q000037:antagonists & inhibitors*; D014227:Triazines / Q000494:pharmacology*; D040301:Vascular Endothelial Growth Factor Receptor-2 / Q000037:antagonists & inhibitors*
D011758:Pyrroles; D014227:Triazines; C509922:brivanib; C496348:FGFR1 protein, human; D051496:Receptor, Fibroblast Growth Factor, Type 1; D040301:Vascular Endothelial Growth Factor Receptor-2; D000409:Alanine