Elevating theranostics: The emergence and promise of radiopharmaceutical cell‐targeting heterodimers in human cancers

Abstract Optimal therapeutic and diagnostic efficacy is essential for healthcare's global mission of advancing oncologic drug development. Accurate diagnosis and detection are crucial prerequisites for effective risk stratification and personalized patient care in clinical oncology. A paradigm shift is emerging with the promise of multi‐receptor‐targeting compounds. While existing detection and staging methods have demonstrated some success, the traditional approach of monotherapy is being reevaluated to enhance therapeutic effectiveness. Heterodimeric site‐specific agents are a versatile solution by targeting two distinct biomarkers with a single theranostic agent. This review describes the innovation of dual‐targeting compounds, examining their design strategies, therapeutic implications, and the promising path they present for addressing complex diseases.