The clinical application of Pt-based anticancer drugs has inspired the development of novel chemotherapeutic metallodrugs with improved efficacies. Pt(IV) prodrugs are one of the most promising successors of Pt(II) drugs and have displayed great anticancer performance. In particular, judicious modification of axial ligands endows Pt(IV) complexes with unique properties that enable them to overcome the limitations of conventional Pt(II) drugs. Herein, we summarize recent developments in Pt(IV) anticancer complexes, with a focus on their axial functionalization with other anticancer agents, immunotherapeutic agents, photosensitive ligands, peptides, and theranostic agents. We hope that this concise view of recently reported Pt(IV) coordination complexes will help researchers to design next-generation multi-functional anticancer agents based on a comprehensive Pt(IV) platform.
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