硼中子俘获治疗靶向硼携带剂4-硼-L-苯丙氨酸患者体内生物分布

Biological Distribution in Patients of Boron Agent 4-Borono-L-Phenylalanine for Boron Neutron Capture Therapy

摘要: 硼中子俘获治疗（boron neutron capture therapy, BNCT）是二元靶向放射治疗方法，中子并不直接提供肿瘤治疗剂量，而是利用肿瘤靶向¹⁰B携带剂将¹⁰B(n, α)⁷Li俘获反应产生的剂量沉积于肿瘤细胞。因此了解血液、肿瘤组织和正常组织中¹⁰B携带剂的生物分布对于BNCT临床治疗是必不可少的。目前国际上BNCT临床主要使用4-硼-L-苯丙氨酸（4-borono-L-phenylalanine, BPA）为硼携带剂。本文简要总结了BPA的结构、理化特性、细胞摄取机制以及人体生物分布等数据，目的是支持和促进基于BPA的BNCT临床试验准备。

Abstract: Boron neutron capture therapy(BNCT) is a binary targeted radiation therapy in which neutron does not directly provide tumor dose. The dose produced by the ¹⁰B(n, α)⁷Li capture reaction will be deposited in tumor cells by using targeted ¹⁰B agents. Therefore, understanding the biological distribution of ¹⁰B agents in the blood, tumor and normal tissue is essential for BNCT. 4-borono-L-phenylalanine(BPA) is the mainly used ¹⁰B agent in BNCT clinical trials worldwide. In order to support and facilitate the preparation of BPA-based BNCT clinical trials, information on the structure, physicochemical properties, cellular uptake mechanisms and human biological distribution of BPA are summarized in this paper.