4-Borono-2-18F-氟-L-苯丙氨酸PET用于硼中子俘获疗法的诊断：四分之一世纪的研究概述。,Annals of Nuclear Medicine

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4-Borono-2-18F-氟-L-苯丙氨酸PET用于硼中子俘获疗法的诊断：四分之一世纪的研究概述。
Annals of Nuclear Medicine ( IF 2.5 ) Pub Date : 2019-03-02 , DOI: 10.1007/s12149-019-01347-8
Kiichi Ishiwata _{1,

2}

Affiliation

开发了4-10B-Borono-2-18F-氟-L-苯丙氨酸（18F-FBPA）来监测用于硼中子俘获治疗（BNCT）的4-10B-borono-L-苯丙氨酸（10B-BPA）的药代动力学正电子发射断层扫描（PET）。在各种动物模型中均证实了18F-FBPA的肿瘤成像潜能。在动物模型和细胞培养物中，黑色素瘤中18F-FBPA的积累高于非黑色素瘤。在体外和体内模型中，将18F-FBPA掺入主要由L型氨基酸转运蛋白介导的肿瘤中。18F-FBPA的肿瘤分布主要与DNA合成的活性有关。18F-FBPA在代谢上稳定，但以非酶方式并入黑色素生成。18F-FBPA的这些体外和体内特征与10B-BPA的特征非常吻合。核磁共振和其他使用非放射性19F-10 / 11B-FBPA的研究也有助于表征。通过比较18F-FBPA和10B-BPA的药代动力学以及使用不同剂量的两种探针直接测量肿瘤中18F和10B的含量，证实了18 / 19F-FBPA作为10B-BPA体内探针的有效性和可靠性。通过不同的途径和方法进行管理。在临床上，基于动态18F-FBPA PET的动力学参数，连续输注10B-BPA的肿瘤中估计的10B浓度类似于直接在手术标本中测量的浓度。验证了18F-FBPA PET对10B浓度估算和BNCT规划的意义。后来18F-FBPA PET参与了患有顽固性肿瘤（例如恶性脑瘤）的患者的10B-BPA BNCT，头颈部肿瘤和黑色素瘤。通常，静态PET扫描用于筛查患者的BNCT，预测10B-BPA的分布和积累以及评估BNCT后的治疗。在某些临床试验中，BNCT的纳入标准是肿瘤与正常组织之比18F-FBPA> 2.5。除BNCT以外，18F-FBPA被证明是在核医学中用于肿瘤诊断的有用PET探针：与11C-蛋氨酸相比，肿瘤与正常脑部的对比更好，放射治疗后复发性和放射性坏死的分化，以及黑色素瘤优先摄取。18F-FBPA研究的进一步进展有望为成功的10B-BPA BNCT和放射性合成18F-FBPA提供更高的18F活性量和更高的摩尔活性，从而更详尽地评估肿瘤和正常组织中10B的浓度。

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4-Borono-2-18F-fluoro-L-phenylalanine PET for boron neutron capture therapy-oriented diagnosis: overview of a quarter century of research.

4-10B-Borono-2-18F-fluoro-L-phenylalanine (18F-FBPA) was developed for monitoring the pharmacokinetics of 4-10B-borono-L-phenylalanine (10B-BPA) used in boron neutron capture therapy (BNCT) with positron emission tomography (PET). The tumor-imaging potential of 18F-FBPA was demonstrated in various animal models. Accumulation of 18F-FBPA was higher in melanomas than in non-melanoma tumors in animal models and cell cultures. 18F-FBPA was incorporated into tumors mediated mainly by L-type amino acid transporters in in vitro and in vivo models. Tumoral distribution of 18F-FBPA was primarily related to the activity of DNA synthesis. 18F-FBPA is metabolically stable but is incorporated into melanogenesis non-enzymatically. These in vitro and in vivo characteristics of 18F-FBPA corresponded well to those of 10B-BPA. Nuclear magnetic resonance and other studies using non-radioactive 19F-10/11B-FBPA also contributed to characterization. The validity and reliability of 18/19F-FBPA as an in vivo probe of 10B-BPA were confirmed by comparison of the pharmacokinetics of 18F-FBPA and 10B-BPA and direct measurement of both 18F and 10B in tumors with various doses of both probes administered by different routes and methods. Clinically, based on the kinetic parameters of dynamic 18F-FBPA PET, the estimated 10B-concentrations in tumors with continuous 10B-BPA infusion were similar to those measured directly in surgical specimens. The significance of 18F-FBPA PET was verified for the estimation of 10B-concentration and planning of BNCT. Later 18F-FBPA PET has been involved in 10B-BPA BNCT of patients with intractable tumors such as malignant brain tumors, head and neck tumors, and melanoma. Usually a static PET scan is used for screening patients for BNCT, prediction of the distribution and accumulation of 10B-BPA, and evaluation of treatment after BNCT. In some clinical trials, a tumor-to-normal tissue ratio of 18F-FBPA > 2.5 was an inclusion criterion for BNCT. Apart from BNCT, 18F-FBPA was demonstrated to be a useful PET probe for tumor diagnosis in nuclear medicine: better tumor-to-normal brain contrast compared with 11C-methionine, differentiation of recurrent and radiation necrosis after radiotherapy, and melanoma-preferential uptake. Further progress in 18F-FBPA studies is expected for more elaborate evaluation of 10B-concentrations in tumors and normal tissues for successful 10B-BPA BNCT and for radiosynthesis of 18F-FBPA to enable higher 18F-activity amounts and higher molar activities.

更新日期：2019-11-01

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