Radionuclide‐Activated Luminescence for Cancer Theranostics

Abstract

AbstractWithin dielectric media, charged particles emitted from medical radionuclides induce polarization of surrounding molecules, which subsequently generate Cerenkov luminescence (CL) upon returning to their ground state. This CL emission confers clinically approved radiotracers with distinctive potential for applications in phototheranostics. However, the utility of CL in vivo has been severely constrained by its ultraviolet‐weighted emission spectrum and extremely low photon flux, particularly in living imaging and triggering photodynamic therapy. Certain optical probes, encompassing fluorescent agents and nanoparticle scintillators, can be activated by radionuclides to generate red‐shifted emissions with amplified luminescence intensity compared to CL. This phenomenon, termed radionuclide‐activated luminescence (RL), represents a promising strategy for enhancing radionuclide‐induced tumor phototheranostic outcomes. This review systematically summarizes the advances in RL technology, highlighting the development of various RL probes and their innovative applications in laser‐free optical bioimaging and cancer phototherapy. It further delves into the confronting challenges and prospects of RL technology, aiming to provide a comprehensive overview and practical insights to advance the integration of radiotheranostics and phototheranostics in clinical practice.