永久抑制EGFR新药ASP8273在美国进入1期临床

yyy666 · 发表于 2015-5-27 00:11:27

非常期待！！！

pigbubu · 发表于 2015-5-27 01:01:23

谢谢分享。
永久抑制就是不可逆抑制，共价结合突变的EGFR，covalently binds to and inhibits the activity of mutant forms of EGFR
看起来跟CO1686， AZD9291， EGF816差不多就是三代EGFR的一种，
能抑制T790M，副作用比一代二代小，最终也会产生耐药。
有效率也跟其他的差不多， 70%左右。

看看这个星期的ASCO有没有结果更新。

EGFR inhibitor ASP8273 An orally available, irreversible, third-generation, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity. Upon oral administration, ASP8273 covalently binds to and inhibits the activity of mutant forms of EGFR, including the T790M EGFR mutant, thereby preventing EGFR-mediated signaling. This may both induce cell death and inhibit tumor growth in EGFR-overexpressing tumor cells. EGFR, a receptor tyrosine kinase mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization. ASP8273 preferentially inhibits mutated forms of EGFR including T790M, a secondarily acquired resistance mutation, and may have therapeutic benefits in tumors with T790M-mediated resistance when compared to other EGFR tyrosine kinase inhibitors. As this agent is selective towards mutant forms of EGFR, its toxicity profile may be reduced as compared to non-selective EGFR inhibitors which also inhibit wild-type EGFR. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)