[225Ac]Ac-macropa-tusamitamab

[225Ac]Ac-macropa-tusamitamab is an experimental radiopharmaceutical designed for targeted alpha therapy (TAT). It consists of the humanized monoclonal antibody tusamitamab, which targets carcinoembryonic antigen-related cell adhesion molecule 5 (CEACAM5), conjugated to the alpha-emitting radioisotope actinium-225 via the macropa chelator. This agent is specifically being investigated for the treatment of metastatic castration-resistant prostate cancer (mCRPC), particularly in cases where tumors exhibit low or negative expression of the androgen receptor (AR) and prostate-specific membrane antigen (PSMA), but high expression of CEACAM5. Upon binding to CEACAM5 on the surface of cancer cells, the conjugate is internalized, and the actinium-225 decay chain releases high-energy alpha particles that induce lethal DNA double-strand breaks, leading to cell death while minimizing damage to adjacent healthy tissues due to the short range of alpha radiation.

Other names

225Ac-macropa-tusamitamabActinium-225 macropa-tusamitamabActinium225 macropa-tusamitamabActinium 225 macropa-tusamitamab225Ac-tusamitamab