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 Pt-IV prodrugs may be exploited to reduce systemic toxicities associated with modern-day chemotherapeutics, including classical Pt-II 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 Pt-IV prodrugs that target not only DNA but also enzymes, proteins, peptides and hormones. Synthetic strategies for accessing Pt-IV chemistry are also provided.