PSMA-TO-1

PSMA-TO-1 (also known as PSMA-71 or Tumor-Optimized-1) is a novel prostate-specific membrane antigen (PSMA) targeting ligand developed by researchers at the Technische Universität München. Designed with an extended linker containing additional naphthyl groups, PSMA-TO-1 exhibits increased lipophilicity and enhanced binding to serum albumin, which prolongs its blood circulation time and increases tumor accumulation compared to standard PSMA ligands like PSMA-617. PSMA-TO-1 can be radiolabeled with diagnostic isotopes such as gallium-68 (68Ga) for PET imaging or therapeutic isotopes such as lutetium-177 (177Lu) and actinium-225 (225Ac) for targeted radionuclide therapy. Preclinical studies in prostate cancer models have demonstrated significant survival benefits with 225Ac-PSMA-TO-1, although it is associated with higher off-target radiation doses to the kidneys, salivary glands, and bone marrow.

Other names

Tumor-Optimized-1Tumor-Optimized1Tumor-Optimized 1