大剂量EGFR-TKI治疗非小细胞肺癌脑转移的研究进展

非小细胞肺癌(non-small cell lung cancer,NSCLC)患者发生脑转移在肺癌中常见,预后较差,除了标准的全脑放射治疗,化疗在NSCLC脑转移患者中的治疗作用有限.表皮生长因子受体(epidermal growth factor receptor,EGFR)-酪氨酸激酶抑制剂(tyrosine kinase inhibitor,TKI)由于脑脊液药物浓度低,疗效不佳.近来个案报道大剂量EGFR-TKI为存在EGFR突变的NSCLC脑转移患者带来了很大获益.本文对NSCLC脑转移治疗现状、EGFR-TKI应用于NSCLC脑转移与存在的困惑、大剂量TKI治疗NSCLC脑转移药代动力学基础以及安全性和有效性进行综述.

Research process on high-dose EGFR-TKI therapy for brain metastasis of non-small cell lung cancer

Brain metastasis of non-small cell lung cancer (NSCLC),which has poor prognosis,is common in lung cancer patients.Except for standard whole brain radiation therapy,chemotherapy has limited therapeutic effect on brain metastasis of NSCLC.Epidermal growth factor receptor (EGFR)-tyrosine kinase inhibitor (TKI) has poor efficacy due to low drug concentration in cerebrospinal fluid.Recently,some case reports have claimed that NSCLC patients with EGFR mutation and brain metastasis benefited a lot from high-dose EGFR-TKI therapy.This paper reviews current status of therapy for brain metastasis of NSCLC,use of EGFR-TKI in treating brain metastasis of NSCLC and the confusion,foundations of pharmacokinetics of high-dose TKI in treating brain metastasis of NSCLC as well as its safety and efficacy.