[225Ac]Ac-DOTA-trastuzumab F(ab')2

[225Ac]Ac-DOTA-trastuzumab F(ab')2 is a preclinical radioimmunotherapy (RIT) agent developed by researchers at the University of Toronto. It consists of a bivalent antibody fragment, trastuzumab F(ab')2, conjugated to the macrocyclic chelator DOTA and radiolabeled with the alpha-particle-emitting radioisotope Actinium-225 (225Ac). The agent targets Human Epidermal Growth Factor Receptor 2 (HER2) on cancer cells, delivering highly localized and cytotoxic alpha radiation to induce DNA double-strand breaks and tumor cell death. In preclinical studies of HER2-positive breast cancer, [225Ac]Ac-DOTA-trastuzumab F(ab')2 demonstrated a superior therapeutic index compared to its full IgG and Fab counterparts, significantly increasing median survival in tumor-bearing mice while minimizing normal tissue toxicity.

Other names

225Ac-DOTA-trastuzumab F(ab')2actinium-225 DOTA-trastuzumab F(ab')2