Platinum(II)-based drugs are widely used for the treatment of solid tumors, especially in combination protocols. Severe side effects and occurrence of resistance are the major limitations to their clinical use. To overcome these drawbacks, a plethora of Pt(IV) derivatives, acting as anticancer prodrugs, have been designed, synthesized and preclinically (often only in vitro) tested. Here, we summarize the recent progress in the development and understanding of the chemical properties and biochemical features of these Pt(IV) prodrugs, especially those containing bioactive molecules as axial ligands, acting as multi-functional agents. Even though no such prodrugs have been yet approved for clinical use, many show encouraging pharmacological profiles. Thus, a better understanding of their features is a promising approach towards improving the available Pt-based anticancer agents.