靶向叶酸受体放射性药物研究进展

Research progress on radiopharmaceuticals targeting folate receptor

叶酸受体(FR)在正常组织中低表达,而在多种恶性肿瘤及炎症疾病中呈过度表达。FR的表达量与疾病严重程度、疗效预后呈正相关,因此FR是肿瘤和炎症疾病诊疗的重要靶点。靶向FR的放射性药物有PET显像剂、SPECT显像剂以及多种治疗药物,目前部分药物实现了临床转化。就靶向α和β亚型FR(FR-α、FR-β)放射性药物及其临床转化的研究进展进行综述。

Folate receptor(FR)is overexpressed in various malignant tumor and inflammatory diseases,while being lowly expressed in normal tissues.The expression of FR is positively correlated with disease severity,treatment and prognosis effciency.Therefore,FR is an important target for diagnosis and therapy of tumors and inflammatory diseases.Radiopharmaceuticals targeting FR include PET imaging agents,SPECT imaging agents,and therapeutic agents,and some of them have achieved clinical translation currently.This review focuses on the research progress of radiopharmaceuticals targeting alpha and beta subtypes of FR(FR-α,FR-β)and their clinical translation.