Recent Advances in Pretargeted Strategy for Cancer Theranostics

Abstract In nuclear medicine, theranostic probes that combine nuclear imaging capabilities with therapeutic functions have shown promise for the diagnosis and treatment of cancers. Nevertheless, the development of theranostic probes may be constrained by two principal factors: (1) the discrepancy between the slow accumulation time of the probes in the tumours and the short‐lived radionuclides, and (2) the suboptimal imaging/treatment effect and high radioactive toxicity caused by long‐lived radionuclides. In recent years, pretargeted strategy has been proposed as a potential solution to solve these problems. In the pretargeted strategy, two components consisting of a tumour‐targeting vector (e. g., antibody) and a radionuclide are injected separately, which can then couple in the tumour tissues to trap radionuclides for nuclear imaging and/or therapy. This two‐step process allows for the independent optimization of the pharmacokinetics of them in vivo, benefiting to improve nuclear imaging and/or therapy of tumours in vivo. In this concept, we will discuss the principle of the pretargeted strategy, with a focus on the discussion of different tumour‐targeting vectors, including antibody‐mediated delivery, nanoparticle‐mediated delivery, metabolic glycan labeling‐mediated accumulation, and enzyme‐triggered in situ self‐assembly‐mediated retention. Finally, we will discuss the current challenges and perspectives on their applications for cancer theranostics in clinics.