Cabozantinib, also known as XL-184 or BMS-907351, is an orally bioavailable, small molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity. Cabozantinib strongly binds to and inhibits several tyrosine receptor kinases. Specifically, cabozantinib appears to have a strong affinity for the hepatocyte growth factor receptor (Met) and vascular endothelial growth factor receptor 2 (VEGFR2), which may result in inhibition of tumor growth and angiogenesis, and tumor regression. Cabozantinib was approved by the U.S. FDA in November 2012 for the treatment of medullary thyroid cancer.
Laus, Gerhard; Schreiner, Erwin; Nerdinger, Sven; Kahlenberg, Volker; Wurst, Klaus; Vergeiner, Stefan; Schottenberger, Herwig. Crystal structures of intermediates in a new synthesis of antitumor drug cabozantinib. Heterocycles. Volume 93. Issue 1, Spec. Issue. Pages 323-332. Journal; Online Computer File. (2016).
Lien, Vegard Torp; Klaveness, Jo; Olberg, Dag Erlend. One-step synthesis of [18F]cabozantinib for use in positron emission tomography imaging of c-Met. Journal of Labelled Compounds and Radiopharmaceuticals. Volume 61. Issue 1. Pages 11-17. Journal; Online Computer File. (2018).
Xu, Wei; Donnelly, David J.; Chow, Patrick L.; Henley, Benjamin J. Method of preparing fluorine-18 labeled cabozantinib and its analogs. Assignee Exelixis, Inc., USA. WO 2016019285. (2016).
Shi, Xiangfei; Zhao, Rui; Meng, Qingyi; Zhang, Xiquan. Process for the preparation of cabozantinib and its intermediate. Assignee Chia Tai Tianqing Pharmaceutical Group Co., Ltd., Peop. Rep. China. CN 103664776. (2014).
Wang, Zhiguo; Song, Yanhong; Ma, Xiujuan; Tian, Beibei; Li, Shijiang; Li, Chao; Li, Tao; Zhang, Xin. Preparation method of Cabozantinib from diethyl malonate and 4-fluoroaniline. Assignee Shanghai Zaiqi Bio-Tech Co., Ltd., Peop. Rep. China. CN 106632028. (2015).
Wang, Kunpeng; Han, Yuelin. New preparation method of cabozantinib. Assignee Nanjing Finetech Chemical Co., Ltd., Peop. Rep. China. CN 110240563. (2019).
