Emerging Therapeutic Radiopharmaceuticals and Their Theranostic Pairs

Nuclear medicine is a rapidly evolving multidisciplinary research field that has been intensively investigated in the past decades. The successful clinical application of various metal-based radiopharmaceuticals for cancer imaging and therapy is based on the modular assembly of the drug complex through the popular bifunctional chelate (BFC) strategy. In targeted radionuclide therapy (TRT), potent radiation is selectively delivered to the cancer cells using radiopharmaceuticals that incorporate therapeutic radiometals which emit α-particles, β⁻-particles, or Meitner–Auger electrons (MAEs). Radiotheranostics is an emerging concept that connects nuclear imaging (via positron emission tomography (PET) or single-photon emission computed tomography (SPECT)) and therapy for personalized cancer diagnosis and treatment. This article outlines the fundamentals of radiopharmaceutical design and radiotheranostics and presents a general description of the therapeutic emissions accompanied by literature examples of the most promising radionuclides; ²¹²Pb, ²¹³Bi, ²²⁵Ac, ²²⁷Th, and ¹⁴⁹Tb for α therapy; ⁴⁷Sc, ⁶⁷Cu, ⁷⁷As, and ¹⁶¹Tb for β⁻ therapy; and ¹¹⁹Sb, ¹³⁵La, and ^197m/gHg for MAE therapy. A comparison of the currently used or proposed theranostic pairs of each radiometal is presented.

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