2025 Volume 48 Issue 9 Pages 1295-1318
In recent years, radiotheranostics, a theranostic approach utilizing radioisotopes, has been gaining significant attention, primarily in the field of oncology. The success of this technology relies on the design of probes that specifically target desired sites, making the development of effective diagnostic and therapeutic agents a crucial area of research. This review provides an overview of the fundamental concepts and recent advancements in probe design for radiotheranostics, with a particular focus on pharmacokinetics and subcellular localization. Key topics discussed include: (1) multimerization, (2) introduction of the albumin-binding moiety, (3) charge modification, (4) glycosylation, (5) conjugation of cell-penetrating peptides, (6) introduction of the covalent binding moiety, (7) targeting the nucleus, and (8) utilizing drug release properties to control pharmacokinetics and intracellular localization. Through these strategies, we review the optimization and novel design possibilities for probes in radiotheranostics.
