[225Ac]-anti-EGFRvIII

[225Ac]-anti-EGFRvIII (also known as FPI-1792) is an investigational targeted alpha therapy (TAT) developed by Fusion Pharmaceuticals (now a subsidiary of AstraZeneca) in collaboration with the National Research Council Canada. It is designed for the treatment of glioblastoma multiforme (GBM), an aggressive and lethal primary brain tumor. The drug consists of a humanized monoclonal antibody that specifically targets the epidermal growth factor receptor variant III (EGFRvIII), a tumor-specific mutation frequently expressed in GBM but absent in normal tissues. This antibody is conjugated to the alpha-emitting radioisotope actinium-225 (225Ac) via a proprietary bifunctional chelate. Upon binding to EGFRvIII-expressing cells, the actinium-225 delivers high-energy alpha particles that induce complex double-strand DNA breaks, leading to selective cell death while sparing surrounding healthy brain tissue. Preclinical studies have demonstrated significant therapeutic efficacy and survival benefits in orthotopic GBM models, both as a monotherapy and in combination with standard-of-care treatments like external beam radiation and temozolomide.

Other names

Actinium-225 anti-EGFRvIIIActinium225 anti-EGFRvIIIActinium 225 anti-EGFRvIII225Ac-EGFRvIII TAT