Advances in photopharmacology: Fluorescent photoisomers for precision cancer theranostics

Photopharmacology, which utilizes photoswitches to reversibly modulate pharmacological activity upon light exposure, has emerged as a promising strategy in treating diseases. In contrast to conventional chemotherapeutic agents, photopharmacological approaches offer precise spatiotemporal control over drug activation, thereby reducing off-target toxicity, mitigating drug resistance, and minimizing overtreatment. Despite its transformative potential, the application of photopharmacology in cancer theranostics remains relatively underexplored. This review aims to consolidate recent advancements in the field, with a particular focus on the role of fluorescent properties in cancer theranostics. We systematically conclude key photoisomerizable scaffolds, including azobenzene, hemiindigoid, diarylethene, and spiropyran, highlighting their structural features, roles in precursor construction, bioimaging and function mechanisms. These scaffolds demonstrate significant advantages in cancer theranostics, span from real-time fluorescent imaging modalities to photoresponsive drug platforms. This review underscores the practical potential of photopharmacology in enabling precision medicine and light-guided therapeutic interventions. By emphasizing recent breakthroughs, we aim to stimulate further research, accelerate the adoption of innovative photopharmacological strategies in oncology and promote clinical practice.