Strategies to improve the efficacy of platinum compounds

Giacomo Cossa, Laura Gatti, Franco Zunino, Paola Perego

Research output: Contribution to journalArticlepeer-review


Platinum drugs are widely used in antitumour therapy and are a cornerstone of the treatment of different solid tumours. The pharmacological interest of cisplatin has led to the design of many analogues to broaden the spectrum of activity, reduce side effects, and overcome resistance. Although the cis configuration was initially identified as the only active one, trans-platinum complexes have shown significant antitumour activity in preclinical models. In addition to mononuclear platinum compounds, multinuclear platinum complexes have been generated that are characterised by a different mode of interaction with DNA. Since a major limitation to the clinical efficacy of platinum compounds is drug resistance, the most important feature of nonconventional platinum drugs should be the capability of overcoming cellular resistance. However, due to the multifactorial nature of clinical resistance, which also involves pharmacological factors, the optimisation of current platinum-based therapy also includes the development of drug delivery approaches. The present review focuses on recent studies on the molecular alterations of tumour cells that are associated with resistance to platinum drugs, the development of novel platinum drugs, and approaches that may contribute to improve the efficacy of platinum-based therapy.

Original languageEnglish
Pages (from-to)2355-2365
Number of pages11
JournalCurrent Medicinal Chemistry
Issue number19
Publication statusPublished - 2009


  • Cisplatin
  • Drug delivery
  • Drug resistance
  • Oxaliplatin
  • Polynuclear platinum compounds

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology


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