Article
SKLB1206, a novel orally available multikinase inhibitor targeting EGFR activating and T790M mutants, ErbB2, ErbB4, and VEGFR2, displays potent antitumor activity both in vitro and in vivo.
Molecular cancer therapeutics - 1 Apr 2012
Pan Youli, Xu Yong, Feng Shan, Luo Shidong, Zheng Renlin, Yang Jiao, Wang Lijiao, Zhong Lei, Yang Han-Yu, Wang Bing-Lin, Yu Yang, Liu Jingjing, Cao Zhixing, Wang Xiaoyan, Ji Pan, Wang Zerong, Chen Xin, Zhang Shuang, Wei Yu-Quan, Yang Sheng-Yong
Abstract excerpt
Anti-epidermal growth factor receptor (EGFR) treatment has been successfully applied in clinical cancer therapy. However, the clinical efficacy of first-generation reversible EGFR inhibitors, such as gefitinib and erlotinib, is limited by the development of drug-resistant mutations, including the gatekeeper T790M mutation and upregulation of alternative signaling pathways. Second-generation irreversible EGFR...
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