225Ac-PRIT

**225Ac-PRIT** is a pretargeted radioimmunotherapy (PRIT) approach using the alpha-emitting radionuclide actinium-225 (^225Ac), typically linked to a DOTA-based hapten (proteus-DOTA), for the targeted delivery of high-energy alpha radiation to tumor cells[2][3]. The modality leverages a bispecific antibody (BsAb) system: one arm recognizes a tumor antigen (e.g., GPA33, HER2, GD2) and the other binds to the DOTA-hapten carrying ^225Ac. This enables precise tumor targeting, rapid renal clearance, minimal normal tissue retention, and an improved safety profile compared to conventional antibody-based radioimmunotherapy[2]. The high linear energy transfer (LET) of ^225Ac alpha particles induces complex DNA double-strand breaks, resulting in potent cytotoxicity and potential cures in animal models of colorectal cancer, breast cancer, and neuroblastoma[2][3]. PRIT technology is designed to address the limitations of long-lived antibody carriers and off-target toxicity in alpha therapy, with applications expanding to solid and hematologic tumors.

Other names

proteus-DOTAPr-PRITα-based pretargeted radioimmunotherapy