Feiyang Liu, Fengming Zou, Cheng Chen, Kailin Yu, Xiaochuan Liu, Shuang Qi, Jiaxin Wu, Chen Hu, Zhenquan Hu, Juan Liu, Xuesong Liu, Li Wang, Juan Ge, Wenchao Wang, Tao Ren, Mingfeng Bai, Yujiao Cai, Xudong Xiao, Feng Qian, Jun Tang, Qingsong Liu, Jing Liu
Background: cKIT kinase overexpression and gain-of-function mutations are the critical pathogenesis of gastrointestinal stromal tumors (GISTs). Although the multiple kinase inhibitors such as imatinib, sunitinib, and regorafenib have been approved for GISTs, the acquisition of polyclonal secondary resistance mutations in KIT is still a limitation for GIST treatment. Here we explored the KIT inhibitory activity of axitinib in preclinical models and describe initial characterization of its activity in GIST patient-derived primary cells...
2019: Therapeutic Advances in Medical Oncology