走进曙色的冷门方向:硼携带剂发展历程简述  

Development history of boron delivery agents

作　　者：李纪元 涂智宇 刘志博 Jiyuan Li;Zhiyu Tu;Zhibo Liu(College of Chemistry and Molecular Engineering,Peking University,Beijing 100871,China;Peking University-Tsinghua University Center for Life Sciences,Beijing 100871,China)

机构地区：[1]北京大学化学与分子工程学院,北京100871 [2]北京大学-清华大学生命科学联合中心,北京100871

出　　处：《中国科学：化学》2020年第10期1296-1319,共24页SCIENTIA SINICA Chimica

基　　金：国家自然科学基金(编号:U186720011)资助项目。

摘　　要：本文简要回顾了20世纪50年代至今用于硼中子俘获治疗的硼携带剂数十年的发展历程,并对蓬勃发展的第三代硼携带剂进行了重点介绍.自20世纪50年代起,硼携带剂逐渐经历了三代的发展:第一代硼酸类似物因缺乏肿瘤特异性而退出历史舞台;第二代4-二羟基硼基-L型苯丙氨酸(BPA)和十一氢巯基十二硼化钠(BSH)经过历史的考验,成为仅有的两种目前应用于临床的硼携带剂,在黑色素瘤、神经胶质瘤和复发性头颈癌等局部侵袭性恶性肿瘤的治疗中发挥着重要作用;第三代硼携带剂正以百花齐放的姿态不断向BPA和BSH发起挑战,旨在追求更好的治疗效果,向着诊疗一体、多元化方向不断探索的新型硼携带剂,将为硼中子俘获治疗创造新的可能.This article briefly reviews the development of boron delivery agents used in boron neutron capture therapy from the 1950s to the present, and highlights the booming third-generation boron delivery agents. Since the 1950s, boron delivery agents has gradually experienced three generations of development. The first generation of boric acid analogs withdrew from the historical stage due to lack of tumor specificity;the second generation of BPA and BSH have passed the historical test and become the only two currently used in clinics, playing an important role in the treatment of locally invasive malignant tumors such as melanoma, gliomas, and recurrent head and neck cancer;the third generation of boron delivery agents are constantly challenging BPA and BSH in a blooming manner. In pursuit of better treatment effects, the new boron carrier agent that is constantly exploring in the direction of integration of diagnosis and treatment and diversification will create new possibilities for boron neutron capture therapy.

关 键 词：硼中子俘获治疗 硼携带剂 诊疗一体化 

分 类 号：TQ460.1[化学工程—制药化工]