Journal of Radiopharmaceuticals and Molecular Probes (대한방사성의약품학회지)

Korean Society of Radiopharmaceuticals and Molecular Probes (대한방사성의약품학회)
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Development of Benzothiazole-Based Boron and Fluorine Complex for Boron Neutron Capture Therapy

  • Soyeon Kim (Leading Research Center of Total Solution for Osteoporosis Treatment, Chonnam National University) ;
  • Iqra Bibi (Division of Applied RI, Korea Institute of Radiological & Medical Sciences (KIRAMS)) ;
  • Jung Young Kim (Division of Applied RI, Korea Institute of Radiological & Medical Sciences (KIRAMS)) ;
  • Ji-Ae Park (Division of Applied RI, Korea Institute of Radiological & Medical Sciences (KIRAMS))
  • Received : 2024.04.17
  • Accepted : 2024.05.10
  • Published : 2024.06.30
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Abstract

Boron neutron capture therapy (BNCT) represents a cutting-edge approach in cancer treatment, offering a promising avenue to enhance cure rates for patients resistant to conventional therapies. A critical factor for successful BNCT is the development of boron drugs with exceptional tumor selectivity. In this study, we synthesized a novel benzothiazole derivative, potassium (4-(benzo[d]thiazol-2-yl)-2,6-difluorophenyl) trifluoroborate (B13), incorporating boron and fluorine. Following its synthesis, we radiolabeled the drug with 18F via a 19F/18F isotope exchange reaction, producing 18F-B13 with good radiochemical purity and yield. Notably, the radiotracer demonstrated significant uptake in U87MG tumors, as evidenced by PET imaging. Biodistribution analysis revealed a substantial accumulation of boron (4 ppm) in U87MG tumors 1h post-intravenous injection. Moreover, it showcased significant tumor/muscle ratios (2.04) 2 h post-injection. While the tumor selectivity of B13 did not meet the stringent standards for BNCT, its potential as a BNCT tracer remains promising. Notably, the tumor/muscle ratio remained elevated up to two hours post-injection, suggesting future avenues for optimization and clinical translation.

Keywords

Acknowledgement

이 논문은 한국연구재단 학문후속세대양성 지원사업(2021R1A6A3A01086709)과 과학기술정보통신부 한국원자력의학원 연구 운영비 지원사업(50462-2024)의 지원에 의하여 이루어졌으며 다른 이해 관계는 없음을 밝힙니다.

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