表皮生长因子受体分子显像与基因突变在非小细胞肺癌中的研究进展

摘要

In vivo epidermal growth factor receptor (EGFR) imaging has great potential to affect patient-specific treatment for NSCLC,applying a targeted therapy,and measuring molecular-specific effects of treatment.New PET/CT radiotracers,such as N-(4-bromo-2-fluorophenyl)-6-methoxy-7-[(1-methylpiperidin-4-yl) methoxy]quinazolin-4-amine (ZD6476),five 4-(anilino) quinazoline derivatives (ML01) and 4-[(3-iodophenyl) amino]-7-(2-[2-{ 2-(2-[2-{ 2-([18F]fluoroethoxy)-ethoxy {-ethoxy]-ethoxy)-ethoxy}-ethoxy]-quinazoline-6-yl-acrylamide) ([18F]F-PEG6-IPQA) are now available.But,11C labeled-4-N-(3-bromoanilino)-6,7-dimethoxyquinazoline (PD153035) is the only PET/CT radiotracer used for human clinical evaluation,primarily for EGFR imaging.Finally,the most important aspect of successful imaging is the identification and characterization of EGFR at the cellular or sub-cellular level with high specificity for the target.Considering the need for further development of such PET/CT tracers,EGFR molecular imaging will be presented along with an important examination of the progression that has been made thus far in the field.%表皮生长因子受体(EGFR)靶向药物的临床应用显著改善了EGFR突变的非小细胞肺癌患者的预后.但由于晚期肺癌患者较难获取组织标本,所以难以判断其敏感人群.PET显像可同时显示组织形态及功能代谢方面的信息,对EGFR分子状态的检测具有独特的优势.EGFR的PET显像包括抗体显像和小分子酪氨酸激酶抑制剂显像.其中抗体显像的EGFR特异性摄取较低,尚需要进一步的研究.而4-3-溴苯氨基-6,7双甲氧喹唑啉(PD153035)可竞争性地结合EGFR胞内区ATP结合位点,抑制酪氨酸激酶活性,直接反映肿瘤细胞EGFR的活性状态,是目前研究最为深入,也是最有希望取得成功的小分子酪氨酸激酶抑制剂.随着分子影像技术在临床中的应用,无创性检测患者体内EGFR突变状态,有望改变晚期患者的疗效监测方法,指导靶向治疗个体化方案的选择,从而进一步提高晚期患者的疗效和预后.