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[177Lu]Lu-DTPA-pivekimab is an investigational radioimmunotherapy agent being developed for the treatment of Acute Myeloid Leukemia (AML). It consists of pivekimab, a monoclonal antibody that targets CD123 (the interleukin-3 receptor alpha chain), conjugated with the bifunctional chelator Bz-DTPA and radiolabeled with the beta-emitting radionuclide lutetium-177 (177Lu). CD123 is highly expressed on AML blasts and leukemic stem cells but has limited expression on normal hematopoietic counterparts, making it a suitable target for selective therapy. The mechanism of action involves the targeted delivery of beta radiation to CD123-expressing cells, inducing DNA damage and cell death through both direct irradiation and cross-fire effects. This agent is part of a radiotheranostic platform that pairs therapeutic [177Lu]Lu-DTPA-pivekimab with diagnostic [89Zr]Zr-DFO-pivekimab for PET imaging to assess target expression and monitor treatment response.
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