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[225Ac]Ac-A9-0642 is an investigational actinium-225 labeled radioligand therapy developed by Alpha-9 Oncology. It is designed to target the Gastrin-Releasing Peptide Receptor (GRPR), a G-protein coupled receptor that is highly expressed in several solid tumors, including prostate, breast, and colorectal cancers. By utilizing the alpha-emitting isotope Actinium-225, the drug delivers high-energy radiation over a very short range (micrometers), causing lethal double-stranded DNA breaks in cancer cells while minimizing exposure to adjacent healthy tissues. It is currently being evaluated in a Phase 1/1b clinical trial (NCT06422104) for the treatment of patients with GRPR-expressing advanced solid tumors.
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