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Development of an automated one-step radiolabeling procedure for a PSMA-targeted radiotherapeutic for prostate cancer
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DOI：10.1016/j.nucmedbio.2026.109607.png)
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Abstract
En 中文
CTT1403 (177Lu-CTT2001), an irreversible phosphoramidate PSMA inhibitor developed by Cancer Targeted Technology, was initially synthesized using a two-step radiolabeling method and has previously been evaluated in first-in-human studies. This two-step approach protected the phosphoramidate pharmacophore—containing a temperature- and pH-labile PN bond—from the harsh conditions required for lutetium-177 (177Lu) chelation. Although the final chemical structure of CTT1403 is identical regardless of the radiolabeling route, it was not clear that CTT2001 could tolerate one-step labeling conditions while preserving PSMA-binding integrity. Therefore, the aim of the study was to develop, optimize, and automate a one-step radiolabeling method for CTT1403 and to confirm that the resulting product is biologically equivalent and exhibits comparable in vitro and in vivo behavior to CTT1403 produced by the original two-step process.
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