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Pt(IV) antitumor prodrugs: dogmas, paradigms, and realities

Mauro Ravera1, Elisabetta Gabano1, Michael J McGlinchey2

  • 1Dipartimento di Scienze e Innovazione Tecnologica, Università del Piemonte Orientale, Viale Michel 11, Alessandria, Italy. domenico.osella@uniupo.it.

Dalton Transactions (Cambridge, England : 2003)
|January 11, 2022
PubMed

Insights

Platinum(IV) prodrugs offer a promising alternative to platinum(II) anticancer drugs by reducing side effects and overcoming resistance. Research into their chemical and biochemical properties aims to improve platinum-based cancer therapies.

Area of Science:

  • Oncology
  • Medicinal Chemistry
  • Drug Development

Background:

  • Platinum(II)-based drugs are mainstays in solid tumor treatment but face limitations like severe side effects and drug resistance.
  • Platinum(IV) prodrugs are being developed as advanced anticancer agents to circumvent these challenges.
  • Many Pt(IV) derivatives incorporate bioactive molecules as axial ligands, creating multi-functional therapeutic agents.

Purpose of the Study:

  • To review recent advancements in the development and chemical understanding of platinum(IV) prodrugs.
  • To highlight the biochemical features and therapeutic potential of Pt(IV) agents, particularly those with bioactive axial ligands.
  • To explore the promise of Pt(IV) prodrugs as next-generation platinum-based anticancer therapies.

Main Methods:

  • Literature review of recent preclinical studies on platinum(IV) prodrugs.
  • Analysis of chemical properties and synthesis strategies for Pt(IV) derivatives.
  • Evaluation of biochemical characteristics and pharmacological profiles of Pt(IV) anticancer agents.

Main Results:

  • Numerous Pt(IV) prodrugs have been designed and synthesized, showing potential in preclinical settings.
  • Pt(IV) prodrugs with bioactive axial ligands demonstrate multi-functional therapeutic capabilities.
  • While none are clinically approved, many Pt(IV) prodrugs exhibit encouraging pharmacological profiles.

Conclusions:

  • Platinum(IV) prodrugs represent a significant advancement over traditional platinum(II) agents.
  • Further understanding of Pt(IV) prodrug chemistry and biochemistry is crucial for clinical translation.
  • These agents hold promise for improving the efficacy and safety of platinum-based cancer treatment.

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