The quest for new functional nanomaterials is one of the defining purposes of nanoscience and nanotechnology. A large number of metal nanoparticles (NPs) are extensively exploited for biomedical applications. Metal NPs, in particular platinum NPs (PtNPs), possess remarkable properties that make them a potential candidate as a diagnostic or therapeutic agent. Due to potential technological interest over the last decade, PtNPs have attracted much attention in the field of anticancer research. PtNPs, when conjugated with many functionalizing agents such as polymers, ligands, drugs, peptides, and surfactants, exhibit improved targeting and reduced cytotoxic effects in various cancers. The PtNPs conjugated with folic acid, graphene oxide, and iron NPs are gained more attention due to their stability, large surface area, and reduced toxicity. To achieve this goal, PtNPs are co‐loaded with drugs or other modalities that offer an opportunity for multimodal activity in the frame of treating cancer types focusing on breast, blood, lung, ovarian, skin, liver, etc. However, a review of PtNPs’ function in diagnosis and treatment is still lacking. In this review, the effectiveness of PtNPs toward inducing and elevating death of the cancerous cells proving its delivery approaches and antitumor nature, concluding with future perspectives, are summarized.

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