第二阶段研究Poziotinib表皮生长因子受体(EGFR)患者肺腺癌有获得性耐药突变EGFR-Tyrosine激酶抑制剂。

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汉代司法院,李KH、金SW、Min YJ,曹E,李Y,李SH,金重,李门将,黑洞,汉族H,荣格J,李JS

第二阶段研究Poziotinib表皮生长因子受体(EGFR)患者肺腺癌有获得性耐药突变EGFR-Tyrosine激酶抑制剂。

Res治疗癌症。2017年1月,49 (1):10 - 19。doi: 10.4143 / crt.2016.058。2016年5月3日Epub。

PubMed ID

27188206 (在PubMed

]

文摘

目的:我们研究poziotinib的功效,第二代表皮生长因子受体(EGFR)酪氨酸激酶抑制剂(TKI)在肺腺癌患者激活表皮生长因子受体突变,谁开发获得抗病性EGFR-TKIs (AR)。材料和方法:单臂二期研究包括EGFR-mutant肺腺癌与AR基于杰克曼埃罗替尼、吉非替尼标准。患者接受poziotinib 16毫克口服每天一次在28天为一个周期。主要终点是无进展生存(PFS)。Prestudy肿瘤活组织检查和血液样本获得确定耐药机制。结果:39例患者治疗。肿瘤的基因决定37例;19 EGFR T790M突变和两个PIK3CA基因突变检测在prestudy肿瘤,和七个T790M突变检测等离子体分析。三个(8%;95%可信区间(CI), 2 - 21)和17 (44%; 95% CI, 28 to 60) patients had partial response and stable disease, respectively. The median PFS and overall survival were 2.7 months (95% CI, 1.8 to 3.7) and 15.0 months (95% CI, 9.5 to not estimable), respectively. A longer PFS was observed for patients without T790M or PIK3CA mutations in tumor or plasma compared to those with these mutations (5.5 months vs. 1.8 months, p=0.003). The most frequent grade 3 adverse events were rash (59%), mucosal inflammation (26%), and stomatitis (18%). Most patients required one (n=15) or two (n=15) dose reductions. CONCLUSION: Low activity of poziotinib was detected in patients with EGFR-mutant non-small cell lung cancer who developed AR to gefitinib or erlotinib, potentially because of severe-toxicityimposed dose limitation.

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药物靶点

药物	目标	类	生物	药理作用	行动
Poziotinib	表皮生长因子受体	蛋白质	人类	未知的	抑制剂 粘结剂	细节