Abstract
Trophoblast cell surface antigen 2 (TROP2) represents an ideal target in cancer diagnosis and therapy, particularly in antibody-drug conjugate (ADC) treatments. Several TROP2-targeted ADCs have been used for the treatment of end-stage metastatic cancers, demonstrating promising therapeutic efficacy. Research has shown that the efficacy of TROP2-ADCs is closely correlated with TROP2 expression levels, highlighting the potential of TROP2 expression as a key factor for patient stratification and selection, which could significantly predict the therapy response and therefore enhance treatment outcomes. Currently, immunohistochemistry (IHC) is the gold standard for detecting TROP2 expression, although it has certain limitations. Non-invasive molecular imaging techniques offer the potential to overcome these limitations, providing valuable guidance for subsequent treatment strategies. The development of immuno-Positron Emission Tomography (immunoPET) technologies, including radiolabeled monoclonal antibodies, nanobodies, peptides and small molecules, have made the non-invasive measurement of TROP2 expression feasible. TROP2-targeted molecular imaging represents a promising frontier for precision oncology, despite existing challenges in clinical translation. This review systematically summarizes the research progress in TROP2-targeted molecular imaging for tumor diagnosis and therapy, while discussing innovative approaches to overcome current technical limitations and accelerate clinical implementation.