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[225Ac]hu11B6-IgG3R435H is a preclinical-stage targeted alpha-particle radioimmunotherapy (TAT) agent developed by DiaProst AB. It consists of a humanized monoclonal antibody, hu11B6, engineered into an IgG3 subclass with an R435H Fc mutation designed to enhance binding to the neonatal Fc receptor (FcRn) and optimize its pharmacokinetic profile. The antibody is conjugated via a DOTA chelator to the alpha-emitting radionuclide Actinium-225 (225Ac). It specifically targets human kallikrein 2 (hK2/KLK2), a serine protease that is highly and almost exclusively expressed in prostate tissue and prostate cancer cells, including those in castration-resistant and androgen receptor-addicted states. Upon binding and internalization, the alpha radiation delivers high-energy particles that induce lethal double-strand DNA breaks in the tumor cells while minimizing damage to surrounding healthy tissue.
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