α核素肿瘤靶向治疗药物研究的进展与挑战

Progress ofα-Emitters for Tumor Targeted Radiotherapy

与目前常用于肿瘤内放射治疗研究的β核素相比,α核素具有射线能量高、射程短、放射生物学效应和细胞毒性作用强等特点,对散在性癌和微转移癌的内放射治疗具有良好的应用前景。本文介绍了近年来211 At、213Bi、212Bi、225Ac和223 Ra等α核素肿瘤靶向治疗研究的最新进展,并结合本课题组的工作对211 At肿瘤靶向治疗药物的研究现状进行重点评述。同时,对目前α核素肿瘤靶向治疗药物研究中面临的问题及临床应用前景进行分析与展望。

Compared withβ-emitters commonly used in radioimmunotherapy,α-emitters have advantages in high linear energy transfer with a short particle range in tissue resulting in high relative biological effectiveness(RBE)and cytotoxicity.Due to these properties,targetedα-therapy(TAT)is expected to be an effective treatment for disseminate and micrometastatic tumor.In this paper,the recent developments,problems and prospect of 211 At,213 Bi,212Bi,225 Ac,and 223 Ra are discussed.