Presentation Theranostic application of cancer targeting probes labeled with various copper radioisotopes

Saga, Tsuneo

At present, various copper radioisotopes can be produced by cyclotrons and many molecular imagingprobes labeled with positron-emitting copper radioisotopes are utilized for PET imaging of cancer. Our institution hasproduced 62Zn/62Cu generators and delivered them to several institutions in Japan. In each institution, they eluted 62Cu from the generator and label 62Cu-ATSM, a PET probe for hypoxia, and performed clinical studies of hypoxiaimaging for patients with brain tumor, head and neck cancer and lung cancer patients. We have also developed 64Culabeledtetramer of cyclic RGD peptide, targeting αvβ3 integrins expressed on various cancer cells and activatedendothelial cells during angiogenesis, for the PET imaging of cancer and monitoring of anti-angiogenesis therapy. Inaddition to PET imaging, copper radioisotopes that emit β-rays and Auger electrons can be applied for treatment, socalledinternal radiotherapy. For example, 64Cu emits not only positrons but also β-rays and Auger electrons, and canbe regarded as a “theranostic” radioisotope. We have proved the potential of 64Cu-ATSM as an internal radiotherapyagent targeting hypoxic microenvironment, which is rich in cancer stem cells. We have also applied the tetramer ofcyclic RGD peptide labeled with 64Cu for experimental internal radiotherapy and obtained promising results. Recently,we are trying to optimize the cyclotron production of 67Cu that emits β-rays for possible application for internalradiotherapy. In this symposium, I would like to introduce our research results aiming for the theranostic application ofcancer targeting probes labeled with various copper radioisotopes.
The International Chemical Congress of Pacific Basin Societies 2015

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