Department of Pathology, The Ohio State University, 4132 Graves Hall, 333 W. 10th Ave, Columbus, OH, 43210, USA.
Department of Radiology, Center for Medical Imaging, State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University and Collaborative Innovation Center for Biotherapy, Chengdu, Sichuan, 610041, P. R. China.
Cancer Commun (Lond). 2018 Jun 19;38(1):35. doi: 10.1186/s40880-018-0299-7.
Boron neutron capture therapy (BNCT) is a binary radiotherapeutic modality based on the nuclear capture and fission reactions that occur when the stable isotope, boron-10, is irradiated with neutrons to produce high energy alpha particles. This review will focus on tumor-targeting boron delivery agents that are an essential component of this binary system. Two low molecular weight boron-containing drugs currently are being used clinically, boronophenylalanine (BPA) and sodium borocaptate (BSH). Although they are far from being ideal, their therapeutic efficacy has been demonstrated in patients with high grade gliomas, recurrent tumors of the head and neck region, and a much smaller number with cutaneous and extra-cutaneous melanomas. Because of their limitations, great effort has been expended over the past 40 years to develop new boron delivery agents that have more favorable biodistribution and uptake for clinical use. These include boron-containing porphyrins, amino acids, polyamines, nucleosides, peptides, monoclonal antibodies, liposomes, nanoparticles of various types, boron cluster compounds and co-polymers. Currently, however, none of these have reached the stage where there is enough convincing data to warrant clinical biodistribution studies. Therefore, at present the best way to further improve the clinical efficacy of BNCT would be to optimize the dosing paradigms and delivery of BPA and BSH, either alone or in combination, with the hope that future research will identify new and better boron delivery agents for clinical use.
硼中子俘获治疗（BNCT）是一种基于核俘获和裂变反应的二元放射治疗方式，当稳定同位素硼-10 被中子辐照时，会产生高能阿尔法粒子。本文将重点介绍硼中子俘获治疗的肿瘤靶向硼递药系统，这是该二元系统的一个重要组成部分。目前有两种低分子量含硼药物正在临床上使用，分别是硼苯丙氨酸（BPA）和硼替佐米（BSH）。尽管它们远非理想药物，但它们的疗效已在高级别胶质瘤、头颈部复发性肿瘤以及数量较少的皮肤和皮肤外黑色素瘤患者中得到了证实。由于它们的局限性，过去 40 年来，人们一直在努力开发新的硼递药系统，以提高其临床应用的生物分布和摄取率。这些药物包括含硼卟啉、氨基酸、多胺、核苷、肽、单克隆抗体、脂质体、各种类型的纳米颗粒、硼簇化合物和共聚物。然而，目前这些药物都没有达到有足够令人信服的数据来支持临床生物分布研究的阶段。因此，目前进一步提高 BNCT 临床疗效的最佳方法是优化 BPA 和 BSH 的剂量方案和给药方式，无论是单独使用还是联合使用，希望未来的研究能够为临床应用找到新的更好的硼递药系统。
