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Reducing the renal retention of low- to moderate-molecular-weight radiopharmaceuticals

Tijdschriftbijdrage - Tijdschriftartikel

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.
Tijdschrift: Current Opinion in Chemical Biology
ISSN: 1367-5931
Volume: 63
Pagina's: 219-228
Aantal pagina's: 10
Jaar van publicatie:2021
Trefwoorden:Low to moderate radiopharmaceuticals, Radiohalogens, Molecular imaging, Radiometals, Albumin-bindingagents, Renal endocystic receptors, Renal reuptake, Cleavable linkers, Renal retention, Pretargeting, Targetedradionuclide therapy, Biochemie & -fysica en Moleculaire biologie