[225Ac]Macropa-PEG4-7065

[225Ac]Macropa-PEG4-7065 is an experimental alpha-particle radioimmunotherapy (RIT) developed for the treatment of Acute Myeloid Leukemia (AML). It comprises the monoclonal antibody clone 7065, which specifically targets the active conformation of integrin-β2 (aITGB2)—a tumor-selective epitope widely expressed on AML blasts and leukemic stem cells but absent on normal hematopoietic progenitors. The antibody is conjugated to the alpha-emitter Actinium-225 ($^{225}$Ac) using a Macropa chelator and a PEG4 linker. This design allows for the delivery of high-linear energy transfer (LET) radiation directly to the leukemia cells, causing lethal double-strand DNA breaks. Preclinical data indicate that [225Ac]Macropa-PEG4-7065 provides significant survival benefits and reduced bone marrow toxicity compared to traditional CD33-targeted therapies, making it a promising candidate for clinical translation in relapsed or refractory AML.

Other names

[225Ac]Macropa-7065