Nintedanib, also known as BIBF 1120, is an orally bioavailable inhibitor of vascular endothelial growth factor receptor (VEGFR), fibroblast growth factor receptor (FGFR) and platelet derived growth factor receptor (PDGFR). Intedanib selectively binds to and inhibits vascular endothelial growth factor receptor (VEGFR), fibroblast growth factor receptor (FGFR) and platelet-derived growth factor receptor (PDGFR) tyrosine kinases, which may result in the induction of endothelial cell apoptosis; a reduction in tumor vasculature; and the inhibition of tumor cell proliferation and migration.
Roth, Gerald J.; Heckel, Armin; Colbatzky, Florian; Handschuh, Sandra; Kley, Jorg; Lehmann-Lintz, Thorsten; Lotz, Ralf; Tontsch-Grunt, Ulrike; Walter, Rainer; Hilberg, Frank. Design, Synthesis, and Evaluation of Indolinones as Triple Angiokinase Inhibitors and the Discovery of a Highly Specific 6-Methoxycarbonyl-Substituted Indolinone (BIBF 1120). Journal of Medicinal Chemistry. Volume 52. Issue 14. Pages 4466-4480. Journal. (2009).
Edupuganti, Ramakrishna; Taliaferro, Juliana M.; Wang, Qiantao; Xie, Xuemei; Cho, Eun Jeong; Vidhu, Fnu; Ren, Pengyu; Anslyn, Eric V.; Bartholomeusz, Chandra; Dalby, Kevin N. Discovery of a potent inhibitor of MELK that inhibits expression of the anti-apoptotic protein Mcl-1 and TNBC cell growth. Bioorganic & Medicinal Chemistry. Volume 25. Issue 9. Pages 2609-2616. Journal; Online Computer File. (2017).
Arava, Veerareddy; Gogireddy, Surendrareddy. An improved process for the synthesis of nintedanib esylate. Synthetic Communications. Volume 47. Issue 10. Pages 975-981. Journal; Online Computer File. (2017).
Li, Zeng; Cheng, Xiaosong; He, Xianliang; Zhang, Jicheng; Huang, Luning; Tao, Anping; Gu, Hong. Method for preparing Nintedanib and intermediate thereof. Assignee Shanghai SynCores Technologies, Inc., Peop. Rep. China. CN 107935908. (2018).
Arava, Veera Reddy; Gogireddy, Surendrareddy; Jasti, Venkateswarlu. Preparaton of a nintedanib ethanesulphonate polymorph, processes and novel intermediates thereof. Assignee Suven Life Sciences Limited, India. IN 2015CH02307. (2016).
Ji, Min; Chen, Hao; Cai, Jin; Liu, Haidong; Li, Rui. Preparation of Nintedanib and its intermediate. Assignee Southeast University, Peop. Rep. China. CN 105837493. (2016).
: Rao, Tadimeti; Zhang, Chengzhi. Preparation of deuterated nintedanib as inhibitors of tyrosine kinase. Assignee Auspex Pharmaceuticals, Inc., USA. US 20150284327. (2015).
Xu, Xuenong. Simple and green method for preparation of nintedanib. Assignee Suzhou Miracpharma Technology Co., Ltd., Peop. Rep. China. CN 104262232. 2015