[225Ac]Ac-DOTA-PKU525

[225Ac]Ac-DOTA-PKU525 is a targeted alpha therapy (TAT) radiopharmaceutical consisting of the fibroblast activation protein (FAP)-targeting antibody PKU525 conjugated to the alpha-emitting radionuclide actinium-225 (225Ac) via a DOTA chelator. Developed by researchers at Peking University, this agent is designed to selectively deliver high-energy alpha radiation to FAP-expressing cells within the tumor stroma, such as cancer-associated fibroblasts (CAFs). Unlike small-molecule FAP inhibitors (FAPIs) which often exhibit rapid clearance from the tumor, the antibody-based PKU525 provides prolonged tumor retention, enhancing the therapeutic window for the 10-day half-life of 225Ac. Preclinical studies in mouse models have demonstrated significant tumor growth inhibition with minimal systemic toxicity, suggesting potential for clinical translation in treating various FAP-positive solid tumors.

Other names

225Ac-DOTA-PKU525225Ac-labeled PKU525