中枢神经系统
表皮生长因子受体
酪氨酸激酶
药理学
癌症研究
化学
临床试验
受体
酪氨酸激酶抑制剂
表皮生长因子
医学
内科学
癌症
作者
Qingbei Zeng,Jiabing Wang,Ziqiang Cheng,Kan Chen,Peter Johnström,Katarina Varnäs,David Yunzhi Li,Zhen Yang,Xiaolin Zhang
标识
DOI:10.1021/acs.jmedchem.5b01073
摘要
Recent reports suggest that an increasing number of patients with lung cancer, especially those with activating mutations of the epidermal growth factor receptor (EGFR), also present with brain metastases and leptomeningeal metastases. These patients have poor prognosis as there are no approved drugs for these indications. Available agents have poor efficacy for these patients even at well above their standard dose. Herein, we report the discovery of (4-[(3-chloro-2-fluorophenyl)amino]-7-methoxyquinazolin-6-yl (2R)-2,4-dimethylpiperazine-1-carboxylate 1m (AZD3759), an investigational drug currently in Phase 1 clinical trial, which has excellent central nervous system penetration and which induces profound regression of brain metastases in a mouse model.
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