[225Ac]Ac-AG1001

`[225Ac]Ac-AG1001` is an investigational, next-generation somatostatin receptor subtype 2 (SSTR2) antagonist radiolabeled with the alpha-emitting radionuclide actinium-225 (225Ac). Developed by AlphaGen Therapeutics, the drug is designed to target SSTR2-expressing tumors, such as neuroendocrine tumors (NETs) and small cell lung cancer (SCLC). Unlike traditional SSTR2 agonists (e.g., DOTATATE) that trigger receptor internalization, AG1001 acts as an antagonist, binding to SSTR2 without activating it, which can potentially recognize a larger population of available receptor-binding sites and enhance tumor uptake. The actinium-225 payload delivers high-energy alpha radiation over short distances, causing localized double-stranded DNA breaks in tumor cells while minimizing damage to surrounding healthy tissues. In preclinical models, `[225Ac]Ac-AG1001` demonstrated nanomolar binding affinity, rapid tumor accumulation, fast renal clearance, and superior antitumor efficacy compared to `[225Ac]Ac-DOTATATE`.

Other names

225Ac-AG1001[225Ac]-AG1001