Recently, targeted alpha-particle therapy (TAT) has garnered recognition for the treatment of various cancer types. The high linear energy transfer of emitted alpha-particles enables targeted cleavage of chemical bonds at proximal distances (micrometer range), leaving neighboring healthy tissues unharmed. We propose this strategy can be applied for the treatment of Alzheimer's disease using astatine-211 (At-211) as a covalently bound alpha-emitting radionuclide. Flutemetamol (X = F-18) is an FDA-approved radiopharmaceutical for positron-emission tomography (PET) imaging of beta-amyloid deposition, a diagnostic tool for Alzheimer's disease. The incorporation of astatine-211 onto the derivative thioflavin scaffold (X = At-211) could result in a novel theranostic agent (1) for the targeted obliteration of amyloid aggregates. Here, we report on the synthesis and characterization of flutemetamol I-127 and At-211 derivatives. (This abstract was updated from a previous submission to a 2020 symposium canceled due to the COVID-19 pandemic.)

At-211 labeled small molecule based on the flutemetamol scaffold: Potential theranostic for Alzheimer’s disease

ACS Spring Meeting 2021

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