Theranostic in Oncology: Precision Targeting with Radioligand Therapy

Abstract

The rapid evolution of theranostics in oncology necessitates a consolidated review to synthesize its foundational principles, current clinical applications, and future trajectory. This approach, which integrates diagnostic imaging with targeted radio nuclide therapy, represents a paradigm shift toward precision medicine but requires a clear elucidation of its mechanisms and positioning within the broader oncology landscape. This review aims to fulfill that need by providing a comprehensive overview of radioligand therapy, from its core concepts to its comparative value and emerging potential. This mini review details the fundamental ‘lock and key’ mechanism of theragnostic, explaining the synergy between targeting vectors and radioactive payloads. It explores the radiopharmaceutical toolkit, comparing vectors like peptides and small molecules and contrasting the properties of diagnostic and therapeutic radionuclides. The critical roles of patient selection via pre-therapeutic imaging and personalized dosimetry for safety and efficacy are examined. Furthermore, the biological and physical mechanisms of cytotoxicity, including the pivotal crossfire effect, are described. The review also analyzes the distinct safety profile of radioligand therapy and positions against other systemic and radiotherapeutic modalities, highlighting its unique value in treating disseminated disease. Looking forward, the field is poised for expansion through the investigation of novel targets, radionuclides, and combination strategies with immunotherapy. Ongoing clinical trials are expected to solidify the role of theranostics in earlier lines of treatment, moving beyond the current late-line standard. Ultimately, the continued integration of molecular profiling and nanotechnology promises to further refine these strategies, cementing theranostics as a cornerstone of personalized cancer management.