Photodynamic therapy is a non-invasive medical approach that employs a source of light along with photosensitizer for the treatment of several diseases. Photodynamic therapy makes use of reactive oxygen species like cytotoxic singlet oxygen for the induction of apoptotic cell death in cancerous cells. Anticancer chemotherapeutic treatments use the cytotoxicity of metallodrugs, wherein all the cells (both cancer and normal cells) in a patient are subjected to similar cytotoxic effects, which results into severe undesirable side effects. During the last couple of decades, metal complexes based on transition metal ions/atoms have displayed exciting cytotoxicity as photodynamic therapeutic agents. Photodynamic therapy serves as an effective localized approach for cancer treatment; wherein metal complexes are employed as photosensitizers. In response to the growing investigations on the utility of metal complexes as photosensitizers in the photodynamic therapy of cancer, we have made attempts to review the recent advances made in the utilization of metal complexes in this field of research. Efforts are made to critically review the in vitro and in vivo studies pertaining to the development of metal complexes based on ruthenium, iridium, osmium, platinum, cobalt, zinc and rhenium, among others; as effective agents for the photodynamic therapy of cancer. Besides, the intervention of nanotechnology for enhancing the anticancer PDT profiles of metal complexes has been described. Importantly, the current status of metal complexes in clinical trials for the photodynamic therapy of cancer have been highlighted. Finally, existing challenges in the development of effective photoactive metallodrugs have been outlined, and future outlooks of research for the development of effective photoactive metallodrugs have been commented upon.

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