In recent years, BODIPY-based theranostics have increasingly been used in cancer therapy and have achieved significant success. According to photochemical theories, the optical imaging (e.g., fluorescence [FLI]/photoacoustic [PAI]/photothermal imaging [PTI]) and phototherapy properties (photodynamic ther-apy [PDT] and photothermal therapy [PTT]) of BODIPY-based dyes can be well-tuned and balanced by chemical structural modifications. Furthermore, with the benefits of molecular/nanoparticle engineering, BODIPY-based theranostics can be endowed with versatile functionalities, including other cutting-edge therapeutic modalities, commendable tumor-targeting ability, and a delicate balance between imaging and therapy performance in a molecular/nano-entity, further enhancing its synergetic therapeutic potency and minimizing the undesirable side effects. In this review, we focus on BODIPY-based theranos-tics for tumor therapy and describe and discuss BODIPY-based FLI-guided chemotherapy, FLI-guided PDT, FLI-guided phototherapies, FLI-guided multi-modal therapies, and PAI-guided phototherapies, as well as multi-modal imaging-guided multi-modal therapies, particularly those that have become available in the last 3 years. The progress and bottlenecks of recent BODIPY-based theranostics are also itemized and dis-cussed, describing the general design principles of BODIPY-based theranostics, with the aim of promoting the use of the theranostics in the clinical transformation of cancer therapy. (c) 2022 Elsevier B.V. All rights reserved.
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