基于 86Y 的正电子放射性药物：放射化学与生物学应用。
86Y based PET radiopharmaceuticals: radiochemistry and biological applications.
机构信息
Imaging Sciences, Translational Research Sciences, Pharma Research and Early Development, F. Hoffmann-La Roche Ltd., Basel, Switzerland.
出版信息
Med Chem. 2011 Sep;7(5):380-8. doi: 10.2174/157340611796799249.
Abstract
Development of targeted radionuclide therapy with (90)Y labeled antibodies and peptides has gained momentum in the past decade due to the successes of (90)Y-ibritumomab tiuxetan and (90)Y-DOTA-Phe(1)-Tyr(3)-octreotide in treatment of cancer. (90)Y is a pure β(-)-emitter and cannot be imaged for patient-specific dosimetry which is essential for pre-therapeutic treatment planning and accurate absorbed dose estimation in individual patients to mitigate radiation related risks. This review article describes the utility of (86)Y, a positron emitter (33%) with a 14.7-h half-life that can be imaged by positron emission tomography and used as an isotopically matched surrogate radionuclide for (90)Y radiation doses estimations. This review discusses various aspects involved in the development of (86)Y labeled radiopharmaceuticals with the specific emphasis on the radiochemistry and biological applications with antibodies and peptides.
摘要
过去十年中，由于（90）Y-ibritumomab tiuxetan 和（90）Y-DOTA-Phe（1）-Tyr（3）-octreotide 在癌症治疗中的成功，用（90）Y 标记的抗体和肽的靶向放射性核素治疗得到了迅猛发展。（90）Y 是一种纯 β（-）发射体，无法进行患者特异性剂量测定，这对于治疗前治疗计划和在个体患者中准确估计吸收剂量以减轻辐射相关风险至关重要。本文综述了正电子发射体（86）Y 的应用，（86）Y 的半衰期为 14.7 小时，半衰期为 33%，可用正电子发射断层扫描成像，并可用作（90）Y 辐射剂量估计的同位素匹配替代放射性核素。本文综述了开发（86）Y 标记放射性药物的各个方面，特别强调了抗体和肽的放射化学和生物学应用。
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