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Targeted alpha therapy (TAT) is a rapidly advancing class of radiotherapeutics that can effectively deliver potent and local radiation to cancer cells while sparing the surrounding normal cells. TATs hold great promise for treatment-resistant tumors such as glioblastoma multiforme (GBM) due to the extensive DNA damage and cell death induced by alpha particles. GBM is an aggressive and lethal primary adult brain tumor that is highly resistant to external beam radiation and chemotherapy. Herein, we present the preclinical evaluation of a novel TAT for treatment of GBM targeting the most common tumour-specific mutant, epidermal growth factor receptor variant 3 (EGFRvIII). Our EGFRvIII TAT consists of a humanized EGFRvIII monoclonal antibody, a proprietary bifunctional chelate, and the alpha-emitting radionuclide, actinium-225 (²²⁵Ac). In vivo biodistribution and efficacy of our EGFRvIII TAT was evaluated in two …