This review summarized the progression of AIEgen-based photo-driven theranostics emphasizing on design strategies for efficient photosensitization, photothermal conversion and multimodal functionalities by adjusting the excited energy dissipation.

Synergistic photothermal immunotherapy has captured great attention owing to the mutually strengthening therapeutic outcomes towards both original tumors and abscopal tumors. Herein, a versatile theranostic agent displaying aggregation‐induced emission, namely TPA‐BT‐DPTQ, was designed and prepared based on benzo[c]thiophene unit as a building block; it can be used for simultaneous fluorescence imaging (FLI) in the second near‐infrared (NIR‐II) window, photoacoustic imaging (PAI), photothermal imaging (PTI), and thermal eradication of tumors. Further experiments validate that photothermal therapy (PTT) mediated by TPA‐BT‐DPTQ nanoparticles not only destroys the primary tumor but also enhances immunogenicity for further suppressing the growth of tumors at distant sites. Furthermore, PTT combining a programmed death‐ligand 1 (PD‐L1) antibody prevents the metastasis and recurrence of cancer by potentiating the effect of immunotherapy.

Owing to their versatile functionality and tunable energy dissipation, aggregation-induced emission luminogens (AIEgens) have emerged as ap otential platform for multimodal theranostics.N evertheless,t he construction of AIEactive phototheranostic agents in the second near-infrared window (NIR-II, 1000-1700 nm), which allows superior resolution and minimized photodamage,i ss till af ormidable challenge.H erein, benzo[c]thiophene serves as an electronrich and bulky donor (D)/p-bridge,w hich can enlarge the conjugation length and distort the backbone of an AIEgen. By precise D/p-bridge engineering,h ighly stable NIR-II AIEgen DPBTA-DPTQ nanoparticles are obtained with acceptable NIR-II fluorescence quantum yield and excellent photothermal conversion efficiency.Inaddition, the spatial conformation of DPBTA-DPTQ is determined for the first time by X-ray single crystal diffraction and theoretical simulations.DPBTA-DPTQ NPs have good biocompatibility and show efficient photothermal therapeutic effects in in vitro tests.F urthermore, DPBTA-DPTQ NPs were used in fluorescence-photoacoustic-photothermal trimodal imaging-guided photothermal eradication of tumors in HepG2 and B16-F10 tumor-xenografted mice.