Despite drug delivery nanoplatformsr eceivinge xtensive attention,d evelopment of as imple, effective, and multifunctional theranostics nanoplatform stillr emains a challenge. Herein, av ersatile nanoplatformb ased on az irconium framework (UiO-66-N 3 )w as synthesized, which demonstrated ac ombined photodynamic therapy (PDT), photothermal therapy (PTT), and chemotherapy (CT) for cancert reatment. AR u II polypyridyl alkynec omplex (Ra) as ap hotosensitizer was modified into an anoplatformb yc lick reactions for the first time. When exposed to suitable light irradiation, the as-preparedmultifunctional nanoplatform (UiO-Ra-DOX-CuS) not only demonstrated efficient 1 O 2 generation, but also exhibited excellent photothermal conversion ability.I n particular, the nanotherapeutic agentp resented ad ual-stimuli response;e ither acidic environment or NIR laser irradiation would trigger the drug release. The synergetic efficacy of UiO-Ra-DOX-CuS combinedP DT,P TT,a nd CT,w hich was evaluated by cell experiments. Moreover,t he designc ould promotet he development of Ru II polypyridyl alkyne complexesb ased multifunctional nanoparticles and multimodal cancert reatment.[a] Dr.Supporting information and the ORCID identification number(s) for the author(s) of this articlecan be found under: https://doi.