[211At]PSMA-5

**[211At]PSMA-5** is a targeted alpha therapy radiopharmaceutical consisting of the alpha-emitting isotope astatine-211 (211At, half-life 7.2 hours) conjugated to a prostate-specific membrane antigen (PSMA) ligand. It selectively binds to PSMA, which is highly expressed on prostate cancer cells, particularly in metastatic castration-resistant prostate cancer (mCRPC), delivering cytotoxic alpha particles to induce DNA double-strand breaks and tumor cell death with minimal range in tissue. Developed by researchers at Osaka University, it demonstrates high tumor accumulation, low off-target uptake, and favorable pharmacokinetics; preclinical studies confirmed antitumor efficacy and safety, leading to a first-in-human investigator-initiated clinical trial (NCT06441994) in Japan for mCRPC patients, with administration to nine patients showing lesion-specific uptake.[1][2][3]

Other names

[At-211]PSMA-5af-002af002af 002