| Summary: | “All in one” organic–inorganic nanocomposites with high biocompatibility and excellent physicochemical properties have recently attracted special attention in cancer imaging and therapy. Combination of organic and inorganic materials confers the nanocomposites with superior biocompatibility and biodegradability of organic materials, as well as magnetic, mechanical, and optical properties of inorganic materials. Increased endeavors have been made to produce diverse organic–inorganic nanocomposites and investigate their potential applications in cancer treatment. Thus, a systematic review of research progresses of diverse organic–inorganic nanocomposites in cancer imaging and therapy is indispensable. Following a brief overview of nanocomposites synthesis, classification, and functionalization, the current review is focused on comprehensively summarizing representatives of both organic–inorganic nanoscale nanocomposites (including organic-silica, organic-carbon, organic-quantum dots, organic-platinum family metals, organic-gold, organic metal oxides, and other nanocomposites) and organic–inorganic molecular nanocomposites (including metal-organic frameworks, organosilica nanoparticles, and amorphous metal coordination polymer particles), and further analyzing their working mechanism in cancer imaging and therapy. Finally, the challenges and future perspectives of organic–inorganic nanocomposites are addressed for promoting their developments and clinical application in cancer treatment.
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