[225Ac]Ac-Macropa-MUC-16

[225Ac]Ac-Macropa-MUC-16 is a targeted alpha-particle therapy (TAT) radioimmunoconjugate designed to treat cancers overexpressing Mucin-16 (MUC-16), also known as CA125. The agent comprises a fully human monoclonal antibody specific for MUC-16, conjugated via the macrocyclic bifunctional chelator Macropa-NCS to the alpha-emitting radioisotope Actinium-225 ([225Ac]). MUC-16 is highly expressed in approximately 80% of epithelial ovarian cancers (EOC) and 65% of pancreatic ductal adenocarcinomas (PDAC), making it a viable target for selective radiation delivery. Upon binding to the target, the conjugate delivers potent alpha radiation, which has a short range and high linear energy transfer, leading to complex DNA damage and cell death in tumor cells while sparing adjacent healthy tissue. Preclinical studies in cell-derived and patient-derived xenograft models have demonstrated significant tumor growth inhibition and complete remissions, particularly in high MUC-16 expressing tumors.

Other names

[225Ac]Ac-Macropa-anti-MUC-16225Ac-Macropa-MUC-16Actinium-225 labeled anti-MUC-16 radioimmunoconjugateActinium225 labeled anti-MUC-16 radioimmunoconjugateActinium 225 labeled anti-MUC-16 radioimmunoconjugate