非小细胞肺癌EGFR-TKIs治疗及PET分子成像的研究进展

表皮生长因子受体(epithelial growth factor receptor,EGFR)信号转导通路在非小细胞肺癌(Non-Small Cell Lung Cancer,NSCLC)中发挥重要作用,尤其胞内酪氨酸激酶结构域的突变状态决定了目前NSCLC的靶向治疗。针对EGFR突变的分子靶向药物表皮生长因子受体酪氨酸激酶抑制剂(epithelial growth factor receptor tyrosine kinase inhibitors,EGFR-TKIs)已开发并应用于NSCLC的治疗。在治疗过程中,EGFR的突变状态随时间发生动态变化,因此精准掌握EGFR的突变状态是靶向治疗方案制定、优化的关键。PET分子成像可在细胞和分子水平,对在体生物活动的发生、发展过程进行实时成像,使实时、在体揭示EGFR的突变状态成为可能。因此,多种以TKIs为前体标记放射性核素作为靶向肿瘤突变EGFR胞内段分子成像探针的研究逐渐增多。本文就EGFR-TKIs在NSCLC治疗及相关PET分子成像方面的研究进展进行综述。

Advances in the Treatment of EGFR-TKIs and PET Molecular Imaging in NSCLC

ABSTRACT: Epidermal growth factor receptor (EGFR) signal transduction pathway plays an important role in non-small Cell Lung Cancer (NSCLC), especially the state structure of intracellular tyrosine kinase domain mutations determines the targeted therapy of NSCLC. Molecular targeted drugs for EGFR mutations in the epidermal growth factor receptor tyrosine kinase inhibitors(EGFR TKIs) has been developed and applied to the treatment of NSCLC. In the treatment process, the mutation state of EGFR changes dynamically with time, so it is the key to formulate and optimize the mutation state of EGFR. PET molecular imaging can be used in real-time imaging of the occurrence and development of biological activities in the cell and molecular level, making it possible to reveal the mutation status of EGFR in real time. Therefore, a number of studies have been conducted on the molecular imaging probes of the tumor mutant EGFR with TKIs as precursors. This paper reviews the progress of EGFR-TKIs in the treatment of NSCLC and related PET molecular imaging.