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对[52 Mn]Mn-DOTATATE和[52 Mn]Mn-DOTA-JR11进行PET成像

James M Omweri¹, Hailey A Houson¹, Shannon E Lynch¹

¹University of Alabama at Birmingham.

Research square

|August 16, 2024

概括

在临床前模型中,与DOTA-JR11相比,标有DOTATATE的-52显示出优异的瘤吸收和内部化. 这突出了使用52Mn-DOTATATE改善神经内分泌瘤成像的潜力.

科学领域:

核医学是一种核医学.
放射性药物化学放射性药物化学
在瘤学瘤学.

背景情况:

-52 (52Mn) 是PET成像的一个有前途的同位素.
索马托斯塔丁受体2 (SSTR2) 在神经内分泌瘤 (NETs) 中过度表达.
[68Ga]Ga-DOTATATE (激动剂) 显示内部化,而[68Ga]Ga-DOTA-JR11 (对抗剂) 的内部化有限,但药理动力学更好.

研究的目的:

在放射性标记DOTATATE和DOTA-JR11中,具有52Mn.
为了比较52Mn-DOTATATE和52Mn-DOTA-JR11的体外和体内性能.
评估它们对SSTR2阳性NET成像的潜力.

主要方法:

对DOTATATE和DOTA-JR11的放射性标记使用52Mn.
在小鼠血清中的体外稳定性测试.
在SSTR2+AR42J细胞中进行体外细胞吸收和内化研究.
在AR42J瘤携带小鼠中的体内生物分布和PET成像.

主要成果:

这两种辐射追踪剂都显示出对SSTR2.2的亲和力.
与52Mn-DOTA-JR11 (7.31%/mg和20.85%) 相比,52Mn-DOTATATE的细胞吸收率 (11.95%/mg) 和内化率 (53.13%) 更高.
在注射后4小时,PET成像显示52Mn-DOTATATE (11.16% ID/g) 与52Mn-DOTA-JR11 (2.11% ID/g) 的瘤吸收显著更高.

结论:

对于这两种52Mn辐射追踪剂,都实现了高的放射化学产量和纯度.
在SSTR2-向方面,52Mn-DOTATATE在体外和体内表现优越.
这些发现支持使用52Mn-DOTATATE进行增强的NET成像.

关键词:

在AR42JJ中.这是SSTR2的SSTR2.激进分子/对抗分子的作用.-52是一种.酸是一种酸.

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