PSMA binder-1 is a ligand for PSMA and can be used to synthesize Ac-PSMA-trillium. Ac-PSMA-trillium is a suitable PSMA-targeting compound with improved PSMA binding properties and pharmacokinetic properties. PSMA ligands have different biological applications after being modified with different radioactive isotopes. If labeled with 111In, it can be used as DOTA chelating agent and imaging agent. Or it can be labeled with 225Ac (to obtain Actinium-225-PSMA-Trillium (BAY 3563254)), which has a radioactive killing effect; it can be used as a Macropa chelator for targeted radionuclide therapy (TRT) , has a strong inhibitory effect on metastatic castration-resistant prostate cancer (mCRPC).
References:
[1]. Sun M, et al. Prostate-Specific Membrane Antigen (PSMA)-Targeted Radionuclide Therapies for Prostate Cancer. Curr Oncol Rep. 2021 Mar 29;23(5):59.
[2]. Zitzmann-Kolbe S, et al., Preclinical evaluation of an actinium-225 labeled PSMA-targeting small molecule (225Ac-PSMA-Trillium (BAY 3563254)) for the treatment of metastatic castration resistant prostate cancer (mCRPC)[J]. Cancer Research, 2024, 84(6_Supplement): 6033-6033.