Presentation Targeted Imaging and Therapy of Cancer with Molecular Probes Labeled with Copper Radioisotopes

Saga, Tsuneo

At present, various copper radioisotopes are produced by cyclotrons for targeted imaging and treatment of cancer. Among various copper radioisotopes, 64Cu, a positron emitter with relatively long physical half-life (12.70 h) that can be produced by small cyclotrons installed in many PET facilities, is most widely applied for PET imaging. We have labeled a tetramer of cyclic RGD peptide with 64Cu and evaluated its potential for PET imaging of cancer and neo-angiogenesis in preclinical models. In addition, 64Cu-labeled Fab fragment of anti-c-kit antibody successfully visualized human small cell lung cancer xenograft in mice. 62Cu, a positron emitter with short physical half-life (9.74 min), is not directly produced by cyclotron, but is eluted from 62Zn/62Cu generator. Our institution has produced 62Zn/62Cu generators using our large cyclotron and delivered them to several institutions in Japan. In each institution, they elute 62Cu from the generator and label 62Cu-ATSM, a PET probe for hypoxia, and performed clinical study of hypoxia PET imaging for patients with various types of cancers. In addition to imaging application, radioisotopes that emit cytotoxic particles can be applied for internal radiotherapy. 64Cu emits not only positrons but also -rays and Auger electrons, and can be regarded as a “theranostic” radioisotope. We have proved the potential of 64Cu-ATSM as an internal radiotherapy agent targeting hypoxic microenvironment. We have also applied 64Cu-labeled cyclic RGD tetramer for experimental internal radiotherapy and obtained promising results. 67Cu, a -ray emitter with long physical half-life (61.83 h), is also a promising therapeutic radionuclide. We are now trying to optimize the cyclotron production of 67Cu for internal radiotherapy. In this conference, I would like to introduce our research results aiming for the theranostic application of cancer targeting probes labeled with various copper radioisotopes.
The 11th Hangzhou International Molecular Imaging Conference (HIMIC)

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