Fluoropharmacology: intrinsic AIE antibiotics as theranostic photosensitizers against resistance and systemic toxicity.

Fluoropharmacology integrates pharmacokinetics/pharmacodynamics with real-time visualization by employing intrinsically fluorescent drugs that combine therapy and luminescence in a single entity. Herein, we report the systematic characterization that clinically approved quinolone antibiotics exhibit intrinsic aggregation-induced emission (AIE) characteristics. Mechanistic studies reveal that the AIE behavior originates from restricted intramolecular motion, thereby establishing the "drug-probe unity" principle that a single molecular architecture inherently encodes pharmacological activity, fluorescence emission, and photosensitizing capability. Exploiting this intrinsic property, we strategically repurpose the historically problematic phototoxicity of quinolones into a theranostic advantage by developing them as photosensitizers for localized antimicrobial therapy. This approach enables visualized pharmacokinetics/pharmacodynamics, synergistic antibacterial efficacy combining intrinsic antibiotic action with photodynamic effects against resistance and systemic toxicity through confined topical application. Beyond elucidating the AIE mechanisms of quinolones, this work proposes Fluoropharmacology as a promising framework that could potentially reshape drug discovery and utilization. By revealing that countless existing and future fluorescent drugs possess untapped visualization capabilities, Fluoropharmacology transforms conventional pharmacopeia into intelligent, image-guided theranostic agents, enabling observation of molecular events within living systems, illuminating the once-invisible journey of drugs from administration to action, and ultimately advancing personalized precision medicine that safeguards human health, where every fluorescent molecule narrates its own healing story.