[225Ac]Ac-DOTA-YS5

[225Ac]Ac-DOTA-YS5 is a novel CD46-targeted radiopharmaceutical consisting of the fully human monoclonal antibody YS5 conjugated with the chelator DOTA and labeled with actinium-225, an alpha-emitting radioisotope. YS5 binds with high affinity to CD46, which is overexpressed on prostate cancer cells, including forms of castration-resistant prostate cancer (CRPC) and treatment-emergent neuroendocrine prostate cancer (t-NEPC), with minimal expression in normal tissue. When administered, the antibody selectively binds to CD46-expressing cells, delivering alpha radiation intracellularly via actinium-225 decay, which generates double-strand DNA breaks and results in targeted cytotoxicity. The approach leverages the short range and high linear energy transfer of alpha particles to achieve potent tumor killing while sparing healthy tissues. [225Ac]Ac-DOTA-YS5 is primarily being developed for advanced metastatic prostate cancer, particularly in patient populations where other targets (e.g., PSMA) may be downregulated or absent[1][3][4][5][8][9][10].

Other names

[225Ac]DOTA-YS5Ac-225-DOTA-YS5Ac225-DOTA-YS5Ac 225-DOTA-YS5Actinium-225 DOTA-YS5Actinium225 DOTA-YS5Actinium 225 DOTA-YS5