多靶点抗肿瘤新药crizotinib的研究进展

Crizotinib:a novel multi-targeted anti-tumor drug

Crizotinib是一种口服多激酶抑制药，针对c—Met和EML4-ALK融合基因为靶点，抑制肿瘤细胞增殖。I期临床试验的推荐剂量为250mg，每日二次。EML4-ALK融合基因的发生率约为4％～7％．I／Ⅱ期临床试验表明ALK阳性的患者在多程治疗后接受crizotinib治疗1年生存率可达77％，2年生存率为64％，且安全性良好。目前，crizotinibm期临床试验正在进行中，FDA已批准其用于ALK阳性的局部晚期和转移的非小细胞肺癌治疗。

Crizotinib is a novel oral multi-targeted tyrosine kinase inhibitor that inhibits c-Met and EML4- ALK fusion gene. Phase I clinical recommended the drug dose of 250 rag, twice daily. EML4-ALK is a fusion oncogene found in approximately 4% - 7% of patients with non- small- cell lung cancer. I/II clinical trial showed that the one year survival rate of patients who harbor ALK transIocation treated by crizotinib after several lines was 77%, and the two years survival rate was 64%. Currently, the crizotinib m clinical trial is ongoing, and the FDA has proved crizotinib for the treatment of patients with advanced non-small-cell lung cancer whose tumors are ALK-positive.