Metal complexes in cancer therapy have attracted much interest mainly because metals exhibit unique characteristics, such as redox activity, metal‐ligand interaction, structure and bonding, Lewis acid properties etc. In 1965, Barnett Rosenberg serendipitously discovered the metal‐based compound cisplatin, an outstanding breakthrough in the history of metal‐based anticancer complexes and led to a new area of anticancer drug discovery. Many metal‐based compounds have been studied for their potential anticancer properties. Some of these compounds have FDA approval for clinical use, while others are now undergoing clinical trials for cancer therapy and detection. In the present study, we have highlighted the primary mode of action of metallic complexes and all FDA‐approved/under clinical trial drugs with reference to cancer treatment. This review also focuses on recent progress on metal‐based complexes such as platinum, ruthenium, iron, etc. with potential anticancer activities.