Platinum-based　drugs　cisplatin,　carboplatin,　and　oxaliplatin　are　widely　used　for　chemotherapeutic　eradication　of　cancer.　However,　the　side　effects　of　platinum　drugs,　such　as　lack　of　selectivity,　high　systemic　toxicity,　and　drug　resistance,　seriously　limit　their　clinical　application.　With　advancements　in　nanotechnology　and　chemical　synthesis,　Pt-based　anti-cancer　drugs　have　made　great　progress　in　cancer　therapy　in　recent　years.　Many　strategies　relied　on　the　anti-cancer　mechanism　similar　to　cisplatin　and　achieved　some　success　by　modifying　existing　platinum　drugs.　Pt-based　nanodrugs,　such　as　platinum　nanoclusters,　have　novel　anti-cancer　mechanisms　and　great　potential　in　tumor-targeted　therapy　and　have　shown　promising　results　in　clinical　application.　In　this　review,　we　systematically　explored　the　development　of　first-line　platinum　chemotherapy　drugs　in　the　clinic　and　their　anti-cancer　mechanisms.　We　also　summarize　the　progress　of　Pt-based　anti-cancer　drug　application　in　cancer　therapy,　emphasizing　their　modification　to　enhance　the　anti-tumor　effect.　Finally,　we　address　challenges　faced　by　platinum　chemotherapy　drugs,　especially　Pt　nanocluster-based　nanodrugs,　in　cancer　treatment.　The　new　platinum　drugs　and　their　targeted　modifications　undoubtedly　provide　a　promising　prospect　for　improving　the　current　anti-cancer　treatments.