Background: Intensive efforts have been implemented to improve the efficacy of platinum complexes
especially with emerging cisplatin resistance and elevated cancer deaths. Platinum(IV) agents show better pharmacokinetics
and decreased side effects compared to Platinum(II) agents.
Methods: This review aims to summarize and categorize the strategies being employed to improve the efficacy of
Platinum-based anticancer agents in recent years.
Results: Nanoparticles and nanoplatforms offer a vast variety of strategies in targeting specific tumor types and
delivering one or two lethal drugs simultaneously. Theranostic agents are being developed to achieve enhanced
imaging and provide further insight into the activity of platinum containing chemotherapy. Moreover, photoactivation
of Pt(IV) prodrugs specifically at the tumor site is gaining attention due to a controlled activity. A platinum
agent formulated as large multi-activity complex is the most common strategy being employed.
Conclusion: Platinum(IV) agents offer great potential in targeting, increasing efficacy, and decreasing toxicity of
Platinum-based anticancer agents. The strategies being employed are aiming to increase specificity and targeting
as well as provide more potent agents.