Molecular alterations in malignant disease result in the expression or upregulations of various targets that can be used for imaging and treatment with
radiopharmaceuticals. This
theranostic principle has acquired greater importance in
personalized medicine in recent years, particularly in oncology, where advanced
tumors can be treated effectively with low side effects. Since the pioneering use of 131I in differentiated
thyroid cancer in the 1940s, remarkable achievements in nuclear medicine endoradiotherapy have been demonstrated, mainly in the treatment of neuroendocrine
neoplasms by using 177Lu-labeled
somatostatin analogs or in the treatment of advanced
prostate cancer using prostate-specific membrane
antigen-directed
radionuclide therapy. Besides that, this review focuses on promising novel
radiopharmaceuticals and describes their preclinical and clinical status. Radiolabeled
antibodies, such as
131I-omburtamab directed against the B7-H3
protein on the surface of
neuroblastoma cells; HuMab-5B1, a 89Zr/177Lu-labeled antibody for the treatment of CA19-9-expressing
malignancies; and 177Lu-lilotomab, a CD37 antibody for the treatment of
B-cell lymphomas, are being highlighted. The
neurotensin receptor ligand 111In/177Lu-3B-227 has demonstrated high potential in imaging and
therapy for several
malignancies (e.g., pancreatic
adenocarcinomas). Targeting of the fibroblast activation
protein is currently being explored for different
tumor entities using PET imaging with the fibroblast activation
protein inhibitor (FAPI)
68Ga-FAPI-04, and the first therapeutic applications of 90Y-FAPI-04 have been applied. After 2 decades of rapid development in
theranostics, a variety of new targets are available for further clinical investigation.