Abstract—Even after cisplatin was approved four decades ago, platinum-based medications continue to have a leading position in cancer treatment plans. The efficacy of these medications in treating many tumour types has been proven, however their ability to treat cancers is still restricted due to the onset of severe side effects and rising drug resistance. The development of platinum (IV) prodrugs with various inhibitors has resulted from our understanding of the mechanisms of action of platinum compounds in cancer treatment. These prodrugs are being studied for their potential to reverse the effects of platinum compounds through alternative biological pathways, such as immune stimulatory mechanisms. Pt-based anti-cancer medications have advanced significantly in cancer therapy in recent years thanks to developments in chemical synthesis and nanotechnology. Numerous tactics were based on the cisplatin-like anti-cancer mechanism, and they were somewhat successful by changing existing platinum drugs. Platinum-based nano-drugs, such platinum nanoclusters, have demonstrated encouraging outcomes in clinical application and offer unique anti-cancer mechanisms. They also have significant potential in tumor-targeted therapy. This study summarises the development of Pt-based anti-cancer drug application in cancer therapy, with a focus on how to modify the drugs to increase the anti-tumor efficacy.