225Ac-PSMA-XT

225Ac-PSMA-XT is a next-generation radiopharmaceutical designed for the treatment of metastatic castration-resistant prostate cancer (mCRPC). It consists of a high-affinity targeting ligand directed against Prostate-Specific Membrane Antigen (PSMA), which is highly overexpressed on prostate cancer cells, conjugated to the alpha-emitting radioisotope Actinium-225 (225Ac). The 'XT' designation refers to the specific optimized ligand or linker technology utilized by the developer to enhance tumor retention and minimize off-target accumulation, particularly in the salivary glands and kidneys, which are common sites of toxicity for first-generation PSMA-targeted alpha therapies. By delivering high-linear energy transfer (LET) alpha particles directly to the tumor microenvironment, 225Ac-PSMA-XT induces complex double-strand DNA breaks that are difficult for cancer cells to repair, potentially overcoming resistance to beta-emitting therapies like 177Lu-PSMA-617.

Other names

Actinium-225 PSMA-XTActinium225 PSMA-XTActinium 225 PSMA-XT225Ac-labeled PSMA-XT