[225Ac]AJ210

[225Ac]AJ210 is an experimental radiopharmaceutical designed for targeted alpha-particle therapy (TAT) of pancreatic ductal adenocarcinoma (PDAC). It consists of a low molecular weight peptide, AJ210, which serves as a high-affinity ligand for the Ephrin type-A receptor 2 (EphA2), a cell surface protein frequently overexpressed in aggressive and treatment-resistant cancers. The peptide is conjugated to the alpha-emitting radioisotope Actinium-225 (225Ac) via a DOTA chelator. Upon administration, [225Ac]AJ210 specifically binds to EphA2-expressing tumor cells and is rapidly internalized, delivering potent, high-linear energy transfer (LET) alpha radiation directly to the cancer cells. This radiation induces lethal double-strand DNA breaks while minimizing damage to adjacent healthy tissues. [225Ac]AJ210 is typically developed as part of a theranostic pair alongside [68Ga]AJ210, which is used for non-invasive PET imaging to identify patients with high EphA2 expression who are most likely to benefit from the therapy.

Other names

Actinium-225 AJ210Actinium225 AJ210Actinium 225 AJ210225Ac-labeled EphA2-targeting peptide