靶向表皮生长因子受体小分子类PET显像剂研究进展

PET imaging agents of small molecules inhibitors targeting EGFR

表皮生长因子受体（EGFR）在多种癌症的发生发展中起着重要作用，目前已有多种EGFR靶向药物被美国食品与药品管理局批准用于临床，但因个体敏感程度不同，总体疗效偏低。研究表明EGFR高表达或突变患者对靶向药物敏感，因此明确EGFR表达水平和突变状态对临床用药有重要指导意义。PET成像技术能实现分子水平无创显像，并能通过SUV进行半定量研究，使得在体内无创明确EGFR表达、突变情况，指导靶向药物的精准治疗成为可能。笔者综述了靶向EGFR的小分子类PET显像剂，以期为新的探针研发及其临床应用提供一定帮助。

Epithelial growth factor receptor（EGFR） plays an important role in numerous cancers and many types of targeting EGFR drugs have been approved by the Food and Drug Administration. However, the individual sensitivity and efficiency rates of these targeting EGFR medicines are low. Many studies have shown that patients with high EGFR expression or mutation are responsive to targeting drugs. Therefore, clearing the EGFR expression and mutation status is significant for clinical medication. PET is a noninvasive in vivo imaging technique that enables the visualization and quantification of the distribution of molecules labeled with positron-emitting isotopes at a picomolar level. PET can guide the precision medicine for these targeting EGFR drugs. This review summarizes the small-molecule PET probes for targeting EGFR.