11C-PD153035 PET显像对非小细胞肺癌EGFR-TKIs治疗敏感性预测的研究

At present, the epidermal growth factor receptor (EGFR) inhibitors are the most widely used targeted therapy for non-small cell lung cancer. The targeted therapy eveluation relies mainly on the genetic testing or rough clinical estimate.PET recepter imaging is high sensitive and specific technique. Combining domestic and foreign literature and our previous research foundation, We hypothesize that: The radioactive uptakes of epidermal growth factor receptor imaging agent 11C-PD153035 are related with EGFR-TKIs sensitivity of cell lines of non small cell lung cancer. 11C-PD153035 PET/CT imaging can predict whether non-small cell lung cancer will resoponse for EGFR - TKIs treatment. Accordingly, this research is centered on the early diagnosis, individualized drug screening and evaluation of therapic effect for non-small cell lung cancer, and create a molecular imaging technique from the lab to clinical application. The aim of this research is to solve early rapid diagnosis and the treatment of individuation of NSCLC, lower cancer diagnosis and treatment cost, improve the quality of life of cancer patients. Providing reliabel basis for the EGFR imaging agent 11C-pd153035 from experiment basis to clinical application.

表皮生长因子受体酪氨酸激酶抑制剂是非小细胞肺癌研究与应用最广泛的靶向药物。而其靶向治疗的疗效预测主要依靠有创性的基因检测方法或粗略的临床估计。PET 受体显像是集受体配体结合高特异性和放射性探测高敏感性于一体的显像技术。目前，以EGFR-TKIs为靶点的PET显像剂研究仍处于药物开发阶段。我们的前期工作已成功研制显像剂11C-PD153035，并初步证实其放射性摄取与NSCLC细胞EGFR-TKIs敏感性的相关性。据此，本课题围绕放射性标记PD153035靶向性显像机制，通过筛选的对EGFR-TKIs敏感性不同细胞及移植瘤的体外和体内实验，验证11C-PD153035放射性摄取与肿瘤EGFR-TKIs治疗敏感性的相关性，建立预测非小细胞肺癌EGFR-TKIs敏感性和继发耐药的PET显像阈值。为开发NSCLC个体化治疗中靶向药物疗效预测的无创性影像学方法提供从实验室到临床应用转化的科学依据。

表皮生长因子受体酪氨酸激酶抑制剂是非小细胞肺癌研究与应用最广泛的靶向药物。而其靶向治疗的疗效预测主要依靠有创性的基因检测方法或粗略的临床估计。PET 受体显像是集受体配体结合高特异性和放射性探测高敏感性于一体的显像技术。目前，以EGFR-TKIs为靶点的PET显像剂研究仍处于药物开发阶段。我们的前期工作已成功研制显像剂11C-PD153035，并初步证实其放射性摄取与NSCLC细胞EGFR-TKIs敏感性的相关性。据此，本课题围绕放射性标记PD153035靶向性显像机制，通过筛选的对EGFR-TKIs敏感性不同细胞及移植瘤的体外和体内实验，验证11C-PD153035放射性摄取与肿瘤EGFR-TKIs治疗敏感性的相关性，建立预测非小细胞肺癌EGFR-TKIs敏感性和继发耐药的PET显像阈值。为开发NSCLC个体化治疗中靶向药物疗效预测的无创性影像学方法提供从实验室到临床应用转化的科学依据。