Drug transporters of platinum-based anticancer agents and their clinical significance

Drug Resist Updat. 2011 Feb;14(1):22-34. doi: 10.1016/j.drup.2010.12.002. Epub 2011 Jan 20.


Platinum-based drugs are among the most active anticancer agents and are successfully used in a wide variety of human malignancies. However, acquired and/or intrinsic resistance still represent a major limitation. Lately, in particular mechanisms leading to impaired uptake and/or decreased cellular accumulation of platinum compounds have attracted attention. In this review, we focus on the role of active platinum uptake and efflux systems as determinants of platinum sensitivity and -resistance and their contribution to platinum pharmacokinetics (PK) and pharmacodynamics (PD). First, the three mostly used platinum-based anticancer agents as well as the most promising novel platinum compounds in development are put into clinical perspective. Next, we describe the presently known potential platinum transporters--with special emphasis on organic cation transporters (OCTs)--and discuss their role on clinical outcome (i.e. efficacy and adverse events) of platinum-based chemotherapy. In addition, transporter-mediated tumour resistance, the impact of potential platinum transporter-mediated drug-drug interactions, and the role of drug transporters in the renal elimination of platinum compounds are discussed.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacokinetics*
  • Antineoplastic Agents / pharmacology
  • Biological Transport
  • Carboplatin / pharmacokinetics
  • Carboplatin / pharmacology
  • Cisplatin / pharmacokinetics
  • Cisplatin / pharmacology
  • Drug Interactions
  • Drug Resistance, Neoplasm
  • Humans
  • Organic Cation Transport Proteins / metabolism*
  • Organoplatinum Compounds / pharmacokinetics*
  • Organoplatinum Compounds / pharmacology
  • Oxaliplatin


  • Antineoplastic Agents
  • Organic Cation Transport Proteins
  • Organoplatinum Compounds
  • Oxaliplatin
  • Carboplatin
  • Cisplatin