To facilitate multicentre clinical studies on targeted alpha
therapy, it is necessary to develop an automated, on-site procedure for conjugating rare, short-lived, alpha-emitting
radionuclides to biomolecules.
Astatine-211 is one of the few alpha-emitting nuclides with appropriate chemical and physical properties for use in targeted
therapies for
cancer. Due to the very short range of the emitted α-particles, this
therapy is particularly suited to treating occult, disseminated
cancers.
Astatine is not intrinsically tumour-specific; therefore, it requires an appropriate tumour-specific targeting vector, which can guide the radiation to the
cancer cells. Consequently, an appropriate method is required for coupling the nuclide to the vector. To increase the availability of
astatine-211 radiopharmaceuticals for targeted alpha
therapy, their production should be automated. Here, we present a method that combines dry distillation of
astatine-211 and a synthesis module for producing
radiopharmaceuticals into a process platform. This platform will standardize production of astatinated
radiopharmaceuticals, and hence, it will facilitate large clinical studies focused on this promising, but chemically challenging, alpha-emitting
radionuclide. In this work, we describe the process platform, and we demonstrate the production of both astaine-211, for preclinical use, and
astatine-211 labelled
antibodies.