타우 PET영상을 위한 ¹⁸F-THK5351의 표지방법 개발

• 영문명: Development of Radiosynthetic Methods of ¹⁸F-THK5351 for tau PET Imaging
• 발행기관: 대한핵의학기술학회
• 저자명: 박준영(Jun-Young Park) 손정민(Jeong-Min Son) 전중현(Joong-Hyun Chun)
• 간행물 정보: 『핵의학기술』Vol.22 No.1, 51~54쪽, 전체 4쪽
• 주제분류: 의약학 > 방사선과학
• 파일형태: PDF
• 발행일자: 2018.05.30

영문 초록

Purpose ¹⁸F-THK5351 is the newly developed PET probe for tau imaging in alzheimer's disease. The purpose of study was to establish the automated production of ¹⁸F-THK5351 on a commercial module. Materials and Methods Two different approaches were evaluated for the synthesis of ¹⁸F-THK5351. The first approach (method I) included the nucleophilic ¹⁸F-fluorination of the tosylate precursor, subsequently followed by pre-HPLC purification of crude reaction mixture with SPE cartridge. In the second approach (method II), the crude reaction mixture was directly introduced to a semi-preparative HPLC without SPE purification. The radiosynthesis of ¹⁸F-THK5351 was performed on a commercial GE TRACERlab™ FX-{FN} module. Quality control of ¹⁸F-THK5351 was carried out to meet the criteria guidelined in USP for PET radiopharmaceuticals. Results The overall radiochemical yield of method I was 23.8±1.9% (n=4) as the decay-corrected yield (end of synthesis, EOS) and the total synthesis time was 75±3 min. The radiochemical yield of method II was 31.9±6.7% (decay-corrected, n=10) and the total preparation time was 70±2 min. The radiochemical purity was>98%. Conclusion This study shows that method II provides higher radiochemical yield and shorter production time compared to the pre-SPE purification described in method I. The ¹⁸F-THK5351 synthesis by method II will be ideal for routine clinical application, considering short physical half-life of fluorine-18 (t1/2=110 min).

목차

서론

실험대상 및 방법

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고찰 및 결론

요약

REFERENCES

키워드

Alzheimer’s Disease ¹⁸F-THK5351 tau PET Radiopharmaceutical