Photoactive monofunctional Pt(ii)–cyanine complex for nucleus and mitochondria dual-targeted antitumor therapy

) of photoactivated Pt-CDPEN is over 16-fold lower than that of cisplatin. Pt-CDPEN exhibited the lysosomal escape property, enabling dual targeting of the cellular nucleus and mitochondria, thus helping to mitigate the chemotherapeutic resistance of Pt drugs. After systemic administration, PEGylated Pt-CDPEN (named as LET-9) exhibited high tumor accumulation, efficient antitumor therapy, and good biocompatibility. This Pt(ii)-cyanine monofunctional complex provides a new platform for dual-targeted antitumor therapy, through simultaneously improving the efficacy and safety of Pt-based therapies.