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Novel CYP11B-ligand [123/131I]IMAZA as promising theranostic tool for adrenocortical tumors: comprehensive preclinical characterization and first clinical experience by Britta Heinze; Andreas Schirbel; Lukas Nannen; David Michelmann; Philipp E. Hartrampf; Christina Bluemel; Magdalena Schneider; Ken Herrmann; Heribert Haenscheid; Martin Fassnacht; Andreas K. Buck; Stefanie Hahner is a Medicine article available to read on EtoBox.
What is Novel CYP11B-ligand [123/131I]IMAZA as promising theranostic tool for adrenocortical tumors: comprehensive preclinical characterization and first clinical experience about?
## Abstract ## Purpose Adrenal tumors represent a diagnostic and therapeutic challenge. Promising results have been obtained through targeting the cytochrome P450 enzymes CYP11B1 and CYP11B2 for molecular imaging, and [^123/131^I]iodometomidate ([^123/131^I]IMTO) has even been successfully introduced as a theranostic agent. As this radiopharmaceutical shows rapid metabolic inactivation, we aimed at developing new improved tracers. ## Methods Several IMTO derivatives were newly designed by replacing the unstable methyl ester by different carboxylic esters or amides. The inhibition of aldosterone and cortisol synthesis was tested in different adrenocortical cell lines. The corresponding radiolabeled compounds were assessed regarding their stability, in vitro cell uptake, in vivo biodistribution in mice, and their binding specificity to cryosections of human adrenocortical and non-adrenocortical tissue. Furthermore, a first investigation was performed in patients with known metastatic adrenal cancer using both [^123^I]IMTO and the most promising compound (R)-1-[1-(4-[^123^I]iodophenyl)ethyl]-1H-imidazole-5-carboxylic acid azetidinylamide ([^123^I]IMAZA) for scintigraphy. Subsequently,
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- Author
- Britta Heinze; Andreas Schirbel; Lukas Nannen; David Michelmann; Philipp E. Hartrampf; Christina Bluemel; Magdalena Schneider; Ken Herrmann; Heribert Haenscheid; Martin Fassnacht; Andreas K. Buck; Stefanie Hahner
- Publisher
- Springer Science and Business Media LLC
- Published
- 2021
- Language
- EN
- Field
- Medicine (Health Sciences)