Antibody radiolabeling with diagnostic Cu-64 and therapeutic Lu-177 radiometal

초록

With the development of monoclonal antibodies, therapeutic or diagnostic radioisotope has been successfully delivered at tumor sites with high selectivity for antigens. Different approaches have been applied to improve the tumor-to-normal ratio by considering the in vivo stability of radioimmunoconjugates as a prerequisite. Various stable and inert antibody radiolabeling techniques for radioimmunoconjugate preparation have been extensively evaluated to enhance in vivo stability. Antibody radiolabeling techniques should be rapid and easy; they should not disrupt the immunoreactivity and in vivo behavior of antibodies, which are coupled with a bifunctional chelator (BFC) to stably coordinate with a radiometal. For the design of BFCs, radiometal coordination properties must be considered. However, various diagnostic radionuclides, such as 89Zr, 64Cu, 68Ga, 111In, and 99mTc, or therapeutic radionuclides, such as 177Lu, 67Cu, 90Y, and 225Ac, have been increasingly used for antibody radiolabeling. In addition to useful radionuclides, 64Cu and 177Lu with the most accessible or the highest production rates in many countries should be considered. In this review, we mainly discussed antibody radiolabeling techniques and conditions that involve 64Cu and 177Lu radiometals.

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