Platinum(II) complexes are widely as chemotherapeutic agents worldwide. Despite their application, these compounds are associated with severe side effects and lack of tumor selectivity. To address these issues, researchers have explored platinum(IV) prodrugs that remain stable and inactive in the body, but can be rapidly converted into active analogs using specific triggers. This article critically reviews the mechanisms of chemical and photophysical triggers for activating platinum(IV) prodrugs.

Abstract

Platinum(II) complexes are used in approximately 50% of chemotherapeutic treatments worldwide. Despite their undoubtful clinical success, these compounds are associated with severe side effects and poor tumor selectivity. To overcome these drawbacks, the development of platinum(IV) molecular prodrugs and nanoparticle formulations that remain stable and therapeutically inactive in a biological environment, but could be quickly reduced into the therapeutically active analogs through a specific trigger have been thought. Within this article, the mechanisms for chemical and photophysical triggers for the activation of platinum(IV) prodrugs have been critically reviewed.