ALK ALK FUSION I1171

多病例报告表明，alk重排的非小细胞肺癌（NSCLC）中的I1171T错义突变对环唑替尼和阿来西尼具有抵抗力，但对铈替尼治疗敏感。这些结果已在体外得到验证。体外证据表明，这种突变干扰了阿来西尼与ALK活性位点的结合，并可能解释了其对结构上不同的ALK抑制剂西替尼的敏感性。
Multiple case reports indicate that the I1171T missense mutation in ALK-rearranged non-small cell lung cancer (NSCLC) confers resistance to crizotinib and alectinib but is sensitive to ceritinib treatment. These results have been validated in vitro. In vitro evidence indicates this mutation interferes with alectinib binding the active site of ALK and may explain the sensitivity to the structurally distinct ALK inhibitor ceritinib.