面向个性化医疗:一种可用于图像和治疗的-177和-225的化剂
Patrick Cieslik1, Manja Kubeil2, Kristof Zarschler2
1Universität Heidelberg, Anorganisch-Chemisches Institut, INF 270, 69120 Heidelberg, Germany.
Journal of the American Chemical Society
|November 16, 2022
概括
一种新型的双皮丁化剂可同时用-177和-225等放射性核酸进行成像和处理. 这种放射性药物具有很高的稳定性和快速复合性.
科学领域:
- 放射性药物化学
- 协调化学
- 核医学
背景情况:
- 使用放射性核素进行治疗和诊断.
- 开发多种放射性核素的稳定化剂是一项挑战.
- 双联体具有很高的热力学和运动稳定性的潜力.
研究的目的:
- 开发一种非状双基化剂,用于化放射性核素.
- 评估基于双的放射性金属复合物的稳定性和复合性.
- 评估针对 somatostatin 2 型受体的双联的疗效.
主要方法:
- 一种非牙的双联体的合成.
- -111,-177和动-225的复合物.
- 在SSTR2阳性细胞系的体外研究 (BON-SSTR2+,MPC).
- 在携带MPC瘤的小鼠中进行了体内生物分布和瘤积累研究.
主要成果:
- 在温和的条件下 (pH 6,<40°C) 结合 bispidine 化剂.
- 复合物在人体血清中表现出高热力学稳定性和惰性,与DOTA复合物相当.
- 标记为Lu和Ac的177和225合物在体内对SSTR2阳性细胞和瘤积累具有特定的结合作用.
结论:
- 无牙双连接物对发明放射性药物具有前景.
- 开发的化剂促进了医学成像和治疗的快速复杂化和高稳定性.
- 优化的配体设计,包括度和供体组,对于高效的放射性金属复合至关重要.
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