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分子成像可在活体状态下直观判断分子靶向药物靶位点存在状态,分子靶向药物与靶位点结合率及精确监测分子靶向药物的治疗疗效,为临床治疗方案的选择和调整提供依据。EGFR是多种恶性肿瘤的关键靶点。研究表明放射性核素标记的表皮生长因子酪氨酸激酶抑制剂是很有潜力的成像探针,其中尤以4-苯氨基-喹唑啉类研究最为广泛。本文简要介绍4-苯氨基-喹唑啉不同衍生物的结构及性质。阐述了18F标记4-苯氨基-喹唑啉类的主要方法:先用18F标记苯氨基,然后将18F标记化合物与喹唑啉或衍生物进行连接,和18F标记喹唑啉或其衍生物,然后与苯胺或其衍生物进行连接。并且进一步比较不同示踪剂在体外、动物和人体内生物分布、肿瘤摄取和代谢的异同。特别是对18F标记示踪剂与11C标记示踪剂在动物和人体分布进行比较。尤其是[18F]ML04肝脏摄取低,肿瘤-本底高,多数学者认为[18F]ML04是最有潜力成为18F标记表皮生长因子受体酪氨酸激酶抑制剂4-苯氨基-喹唑啉类示踪剂。
Molecular imaging can directly determine the presence of molecular target drug target site in vivo, the binding rate between molecular targeted drug and target site, and accurately monitor the therapeutic effect of molecular targeted drugs, thus providing the basis for the selection and adjustment of clinical treatment options . EGFR is a key target for a variety of malignancies. Studies have shown that radionuclide-labeled epidermal growth factor tyrosine kinase inhibitors are potential imaging probes, of which 4-anilino-quinazolines are the most widely studied. This article briefly introduces the structure and properties of different derivatives of 4-anilino-quinazoline. The main method of labeling 18-labeled 4-anilino-quinazolines is described as follows: the anilino group is first labeled with 18F and the 18F-labeled compound is then coupled with a quinazoline or derivative, and the 18F is labeled with a quinazoline or a derivative thereof, Then with aniline or its derivatives. And further comparison of different tracer in vitro, animal and human biodistribution, tumor uptake and metabolism of similarities and differences. In particular, animal and human distribution of 18F labeled tracer with 11C labeled tracer was compared. In particular, [18F] ML04 has low liver uptake and high tumor-to-background levels, and most scholars consider [18F] ML04 as the most promising 18F-labeled epidermal growth factor receptor tyrosine kinase inhibitor 4-anilino-quinazolines Tracer.