申请人:Memorial Sloan Kettering Cancer Center
公开号:US11135320B2
公开(公告)日:2021-10-05
Described herein are Tz/TCO-based pretargeting strategies using an Al[18F]-NOTA-labeled tetrazine radioligand. This imaging strategy enables delineation of cancer at earlier time points compared to other imaging strategies and further decreases the radiation dose to healthy tissues compared to directly labeled antibodies. Al-based 18F imaging of small molecules, such as tetrazine, has not been previously achieved due to the decomposition of tetrazine during radiofluorination. Radiofluorination is advantageous over other radiolabeling methods because, in addition to having a shorter half-life, 18F is more readily available to produce and therefore integrated into hospital workflows.
本文描述的是使用 Al[18F]-NOTA 标记的四嗪放射性配体的基于 Tz/TCO 的预靶向策略。与其他成像策略相比,这种成像策略能在更早的时间点对癌症进行分界,与直接标记的抗体相比,还能进一步降低对健康组织的辐射剂量。由于四嗪在放射性氟化过程中会分解,以前还没有实现过小分子(如四嗪)的铝基 18F 成像。与其他放射性标记方法相比,放射性氟化法的优势在于,除了半衰期较短之外,18F 更容易生产,因此可纳入医院工作流程。