225Ac-LNC1011

225Ac-LNC1011 (also known as Dan-PSMA) is a novel radiopharmaceutical designed for targeted alpha therapy (TAT) in the treatment of prostate cancer. It consists of a prostate-specific membrane antigen (PSMA)-binding ligand conjugated to a dansylphenylalanine moiety and a DOTA chelator, radiolabeled with the alpha-emitting isotope Actinium-225 (225Ac). The addition of the dansylated amino acid is intended to optimize the drug's pharmacokinetic profile by increasing albumin binding, which leads to enhanced tumor uptake and prolonged retention within PSMA-positive lesions compared to earlier generation radioligands like PSMA-617. By delivering high-energy alpha particles directly to the tumor site, 225Ac-LNC1011 induces lethal double-strand DNA breaks in cancer cells while minimizing radiation exposure to surrounding healthy tissues. The drug is primarily being developed for metastatic castration-resistant prostate cancer (mCRPC).

Other names

Dan-PSMA[225Ac]-LNC1011注射液225Ac-labeled PSMA-targeted radioligand