Pexidartinib, also know as PLX-3397, is a CSF1R inhibitor with IC50 of 20 nM in development by Plexxikon for the treatment of tenosynovial giant cell tumors. It is in a phase 3 clinical trial for Pigmented Villonodular Synovitis (PVNS) or Giant Cell Tumor of the Tendon Sheath (GCT-TS).
Chen, Dongsheng; Zhang, Yi; Li, Jianqi; Liu, Yu. Exploratory Process Development of Pexidartinib through the Tandem Tsuji-Trost Reaction and Heck Coupling. Synthesis. Volume 51. Issue 12. Pages 2564-2571. Journal; Online Computer File. (2019).
Ibrahim, Prabha N.; Jin, Masayoshi; Matsuura, Shinji. A process for the preparation of chloropyrrolopyridinylmethylpyridinyltrifluoromethylpyridinylmethylamine for use as a kinase modulator. Assignee Plexxikon Inc., USA; Daiichi Sankyo Company, Limited. WO 2016179412. (2016).
