Abstract Prostate-specific membrane antigen (PSMA) is a transmembrane glycoprotein highly expressed on prostate cancer cells, making it an ideal target for novel prostate cancer therapies. Currently, there are several actinium-225 (225Ac)-PSMA-targeting small molecules (SMOL) in clinical development for treating patients with metastatic castration-resistant prostate cancer. 225Ac-PSMA-Trillium (BAY 3563254), is a novel PSMA-targeting molecule which comprises a highly specific PSMA-binding motif, an albumin-binding domain to optimize tumor uptake and retention, and a Macropa™ chelator complexed with the alpha-emitter 225Ac. Here, we compared 225Ac-PSMA-Trillium with three other 225Ac-PSMA-SMOLs, i.e., 225Ac-PSMA-617, 225Ac-PSMA-R2 and 225Ac-PSMA-I Part 1 (Regular Abstracts); 2026 Apr 17-22; San Diego, CA. Philadelphia (PA): AACR; Cancer Res 2026;86(7 Suppl):Abstract nr 7202.
Hagemann et al. (Fri,) studied this question.