The activation of anticancer molecules with visible light constitutes an elegant strategy to target tumors and to improve the selectivity of treatments. In this context, we report here a visible-light activatable bis-platinum complex (DHP-Pt2) incorporating an organic photo-switchable ligand based on the dimethyldihydropyrene moiety. Illumination of this metal complex with red light (660 nm) under air readily produces the corresponding endoperoxide form (CPDO2-Pt2). These two metal complexes exhibit different DNA binding properties and, more importantly, we show that only the photogenerated CPDO2-Pt2 is able to penetrate into cancer cell nuclei, where it is then capable of releasing cytotoxic singlet oxygen. This study represents the first proof-of-concept showing that dimethyldihydropyrene derivatives can be used to transport and deliver singlet oxygen into cancer cell nuclei upon visible-light activation