Zhang Ling, Li Yunxia, Zhang Shaohong, Gao Chen, Nie Keke, Ji Youxin
Department of Oncology, Qingdao Cancer Hospital, Qingdao 266042, China.
Department of Medicine, Laixi Meihuashan Hospital, Qingdao 266600, China.
Cancer Biol Med. 2018 May;15(2):178-181. doi: 10.20892/j.issn.2095-3941.2018.0003.
Crizotinib, a small molecular tyrosine kinase inhibitor, manifests dramatic responses in patients with non-small cell lung cancer with echinoderm microtubule associated protein like 4-anaplastic lymphoma kinase (EML4-ALK) rearrangements. ALK gene point mutation is the primary mechanism of acquired crizotinib resistance; however, the intrinsic mechanism is not fully understood. Here, we report a patient with a low mutant allele fraction (MAF) of EML4-ALK rearrangement, who experienced primary resistance to crizotinib treatment. The patient was a 66-year-old Chinese man, who had a history of metastatic lung cancer and was treated with first- and third-generation epidermal growth factor receptor tyrosine kinase inhibitors (EGFR TKIs). After 14 months of osimertinib treatment, his disease progressed, and next-generation sequencing was performed from a liquid biopsy of the patient's blood. An EML4-ALK rearrangement was found and crizotinib was administered. The patient's lung lesions continued to progress after one month of crizotinib treatment, and pemetrexed-bevacizumab was initiated. After two cycles of chemotherapy, the metastatic cancers shrunk, and the patient maintained stable disease at his last follow-up. EML4-ALK rearrangements can happen in patients with EGFR-positive NSCLC, after acquired resistance to EGFR TKI treatment. The EGFR T790M and C797G mutations occur in cis is a critical mechanism of resistance to osimertinib therapy. The MAF of EML4-ALK rearrangements in cancer cells might be a predictive factor for crizotinib treatment.
克唑替尼是一种小分子酪氨酸激酶抑制剂,对棘皮动物微管相关蛋白样4-间变性淋巴瘤激酶(EML4-ALK)重排的非小细胞肺癌患者表现出显著疗效。ALK基因点突变是获得性克唑替尼耐药的主要机制;然而,其内在机制尚未完全明确。在此,我们报告1例EML4-ALK重排突变等位基因分数(MAF)较低的患者,其对克唑替尼治疗产生原发性耐药。该患者为一名66岁的中国男性,有转移性肺癌病史,曾接受第一代和第三代表皮生长因子受体酪氨酸激酶抑制剂(EGFR TKIs)治疗。在接受奥希替尼治疗14个月后,其病情进展,遂对患者血液进行液体活检并进行二代测序。结果发现EML4-ALK重排,随后给予克唑替尼治疗。克唑替尼治疗1个月后,患者肺部病灶持续进展,遂开始使用培美曲塞-贝伐单抗治疗。经过两个周期的化疗,转移癌缩小,患者在末次随访时病情保持稳定。EML4-ALK重排在EGFR阳性非小细胞肺癌患者中,可在获得性EGFR TKI治疗耐药后发生。EGFR T790M和C797G突变顺式发生是奥希替尼治疗耐药的关键机制。癌细胞中EML4-ALK重排的MAF可能是克唑替尼治疗的一个预测因素。