Yang Guangjian, Hu Jiaqi, Liu Runze, Li Pei, Yang Linke, Tang Xiaoyong, Wang Luokun
Department of Respiratory Medical Oncology, Shandong Cancer Hospital and Institute, Shandong First Medical University and Shandong Academy of Medical Sciences, Jinan, Shandong Province.
Department of Contract Research Organization Business Unit, PharmaBlock Sciences (Nanjing) Inc., Nanjing, Jiangsu Province.
Anticancer Drugs. 2025 Jun 1;36(5):432-437. doi: 10.1097/CAD.0000000000001695. Epub 2025 Feb 17.
The novel and highly selective anaplastic lymphoma kinase ( ALK ) inhibitor iruplinalkib showed potent activity and manageable safety profiles in patients with ALK -rearranged non-small cell lung cancer (NSCLC). However, the evidence of iruplinalkib for uncommon ALK double fusion and secondary G1202R resistance mutation is limited. Here, we report a case of a 36-year-old male with metastatic NSCLC harboring uncommon TTC7A - ALK and EML4 - ALK double fusion. Alectinib as first-line therapy showed partial response, with a progression-free survival (PFS) of 20 months. When his disease progressed, the ALK secondary G1202R resistance mutation was identified. His metastatic paraesophageal lymph node decreased during iruplinalkib treatment, achieving an ongoing PFS benefit for 10 months. Treatment-related adverse events of iruplinalkib were grade 1 hypercholesterolemia and hypertriglyceridemia. The modeling simulation revealed that the G1202R mutation exerted little effect on the binding of iruplinalkib. Iruplinalkib showed potency to G1202R because of its unique chemical structure and removal of steric clashes, which might be a promising option for ALK -rearranged NSCLC patients with G1202R resistance mutation.
新型高选择性间变性淋巴瘤激酶(ALK)抑制剂艾乐替尼在ALK重排的非小细胞肺癌(NSCLC)患者中显示出强大的活性和可控的安全性。然而,艾乐替尼针对罕见的ALK双重融合和继发性G1202R耐药突变的证据有限。在此,我们报告一例36岁男性转移性NSCLC患者,其携带罕见的TTC7A-ALK和EML4-ALK双重融合。阿来替尼作为一线治疗显示出部分缓解,无进展生存期(PFS)为20个月。当他的疾病进展时,发现了ALK继发性G1202R耐药突变。在艾乐替尼治疗期间,他的转移性食管旁淋巴结缩小,持续获得了10个月的PFS获益。艾乐替尼的治疗相关不良事件为1级高胆固醇血症和高甘油三酯血症。建模模拟显示,G1202R突变对艾乐替尼的结合影响很小。由于其独特的化学结构和消除了空间位阻冲突,艾乐替尼对G1202R显示出活性,这可能是ALK重排且具有G1202R耐药突变的NSCLC患者的一个有前景的选择。