Cerium/Lanthanum-134 as a PET Imaging Theranostic Pair

Theranostics, at the intersection of imaging and therapy, offers personalized approaches to combat diseases like cancer. Actinium-225, has proven highly effective in targeted alpha therapies but poses challenges due to limited imaging options with its half-life and chemistry. Our research introduces a promising solution by developing a robust 134Ce radiolabeling method using chelators Macropa and DOTA. We applied this optimized method to prostate cancer targeting agents PSMA-617 and antibody YS5. Encouragingly, 134Ce/225Ac-Macropa-PEG4-YS5 demonstrated nearly identical distribution in most tissues and tumors, except for the liver and spleen. This study represents the first comprehensive examination of Ce-134 and Ac-225 chemistry and localization, from chelators to tumor-targeting agents. The findings endorse the potential use of 134Ce-radiopharmaceuticals for cancer imaging, offering valuable companion diagnostics to alpha particle radiotherapeutics.

research diagram

Figure: 134Ce/225Ac-based radiopharmaceuticals are promising for prostate cancer imaging and therapy. We utilize prostate cancer targeting agents PSMA-617 and antibody YS5 to radiolabel 134Ce/134La or 225Ac with DOTA/Macropa chelator ligands for evaluation with microPET/CT imaging.

For more information, refer to our published work:

  1. Bobba KN, Bidkar AP, Meher N, Fong C, Wadhwa A, Dhrona S, Sorlin A, Bidlingmaier S, Shuere B, He J, Wilson DM, Liu B, Seo Y, VanBrocklin HF, Flavell RR. Evaluation of 134Ce/134La as a PET Imaging Theranostic Pair for 225Ac α-Radiotherapeutics. J Nucl Med. 2023 Jul;64(7):1076-1082. doi: 10.2967/jnumed.122.265355. Epub 2023 May 18. PMID: 37201957; PMCID: PMC10315697.
  2. Bobba KN, Bidkar AP, Wadhwa A, Meher N, Drona S, Sorlin AM, Bidlingmaier S, Zhang L, Wilson DM, Chan E, Greenland NY, Aggarwal R, VanBrocklin HF, He J, Chou J, Seo Y, Liu B, Flavell RR. Development of CD46 targeted alpha theranostics in prostate cancer using 134Ce/225Ac-Macropa-PEG4-YS5. Theranostics. 2024 Jan 27;14(4):1344-1360. doi: 10.7150/thno.92742. PMID: 38389832; PMCID: PMC10879874.