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Reducing the renal retention of low- to moderate-molecular-weight radiopharmaceuticals.
Current Opinion in Chemical Biology ( IF 6.9 ) Pub Date : 2021-07-26 , DOI: 10.1016/j.cbpa.2021.06.008
Dora Mugoli Chigoho 1 , Jessica Bridoux 1 , Sophie Hernot 1
Affiliation  

The field of nuclear imaging and therapy is rapidly progressing with the development of targeted radiopharmaceuticals that show rapid targeting and rapid clearance with minimal background. Unfortunately, they are often reabsorbed in the kidneys, leading to possible nephrotoxicity, limiting the therapeutic dose, and/or reducing imaging quality. The blocking of endocytic receptors has been extensively used as a strategy to reduce kidney radiation. Alternatively, the physicochemical properties of radiotracers can be modulated to either prevent their reuptake or promote the excretion of radiometabolites. Other interesting strategies focus on the insertion of a cleavable linker between the radiolabel and the targeting moiety or pretargeting approaches in which the targeting moiety and radiolabel are administered separately. In the context of this review, we will discuss the latest advances and insights on strategies used to reduce renal retention of low- to moderate-molecular-weight radiopharmaceuticals.

中文翻译:

减少低至中等分子量放射性药物的肾潴留。

随着靶向放射性药物的发展,核成像和治疗领域正在迅速发展,这些药物在最小背景下显示出快速靶向和快速清除。不幸的是,它们经常被肾脏重新吸收,导致可能的肾毒性、限制治疗剂量和/或降低成像质量。内吞受体的阻断已被广泛用作减少肾脏辐射的策略。或者,可以调节放射性示踪剂的理化特性,以防止其再摄取或促进放射性代谢物的排泄。其他有趣的策略集中在放射性标记和靶向部分之间插入可切割的接头或分别给予靶向部分和放射性标记的预靶向方法。
更新日期:2021-07-26
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