Platinum compounds, such as cisplatin, carboplatin and oxaliplatin are amongst the most useful drugs in the anticancer armamentarium. DNA is considered the biological target of platinum drugs but the overall efficacy is the sum of target binding, cellular uptake and metabolic deactivation. This contribution will summarize the medical uses and biological mechanisms of the currently used drugs. The status of new agents in development, especially those such as polynuclear platinum and mononuclear transplatinum compounds acting by different mechanisms to cisplatin and congeners, will be critically surveyed.