Anti-tumour/metastasis Effects of the Potassium-Sparing Diuretic Amiloride: An Orally Active Anti-Cancer Drug Waiting for Its Call-Of-Duty?

Int J Cancer. 2011 Nov 1;129(9):2051-61. doi: 10.1002/ijc.26156. Epub 2011 Aug 1.


Amiloride.HCl is clinically used as an oral potassium-sparing diuretic, but multiple studies in biochemical, cellular and animal models have shown that the drug also possesses anti-tumour and anti-metastasis activities. The additional effects appear to arise through inhibition of two discrete targets: (i) the sodium-hydrogen exchanger 1 (NHE1), a membrane protein responsible for the characteristically low extracellular pH of tumours and (ii) the urokinase-type plasminogen activator (uPA), a serine protease mediator of cell migration, invasion and metastasis and well-known marker of poor prognosis in cancer. This mini-review summarises for the first time the reported anti-tumour/metastasis effects of amiloride in experimental models, discusses the putative molecular mechanisms responsible for these effects and concludes by commenting on the pros and cons of trialling amiloride or one of its structural analogues as potential new anti-tumour/metastasis drugs.

Publication types

  • Review

MeSH terms

  • Administration, Oral
  • Amiloride / administration & dosage
  • Amiloride / pharmacology
  • Amiloride / therapeutic use*
  • Animals
  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use*
  • Disease Models, Animal
  • Humans
  • Neoplasm Metastasis / drug therapy*
  • Neoplasms / drug therapy*
  • Sodium Channel Blockers / administration & dosage
  • Sodium Channel Blockers / pharmacology
  • Sodium Channel Blockers / therapeutic use*
  • Sodium-Hydrogen Exchangers / antagonists & inhibitors
  • Urokinase-Type Plasminogen Activator / antagonists & inhibitors


  • Antineoplastic Agents
  • Sodium Channel Blockers
  • Sodium-Hydrogen Exchangers
  • Amiloride
  • Urokinase-Type Plasminogen Activator