Platinum(IV) Prodrugs – A Step Closer to Ehrlich's Vision?

The concept of the “magic bullet”, a medicine designed to hit a specific biological target, was pioneered by Paul Ehrlich, the father of chemotherapy, some 100 years ago. Building on Ehrlich's vision, we have endeavoured to showcase not only how targeted PtIV prodrugs may be exploited to reduce systemic toxicities associated with modern‐day chemotherapeutics, including classical PtII drugs, but also how these prodrugs may overcome resistance issues that have plagued many chemotherapeutic regimes. A summary of advances in this field over the past decade is provided, with an emphasis on PtIV prodrugs that target not only DNA but also enzymes, proteins, peptides and hormones. Synthetic strategies for accessing PtIV chemistry are also provided. A summary of advances in the rational design and development of targeted PtIV prodrugs over the past decade is provided with an emphasis on derivatives that target not only DNA but also enzymes, proteins, peptides and hormones.