Novel therapeutic applications of cardiac glycosides

Nat Rev Drug Discov. 2008 Nov;7(11):926-35. doi: 10.1038/nrd2682. Epub 2008 Oct 24.


Cardiac glycosides are a diverse family of naturally derived compounds that bind to and inhibit Na+/K+-ATPase. Members of this family have been in clinical use for many years for the treatment of heart failure and atrial arrhythmia, and the mechanism of their positive inotropic effect is well characterized. Exciting recent findings have suggested additional signalling modes of action of Na+/K+-ATPase, implicating cardiac glycosides in the regulation of several important cellular processes and highlighting potential new therapeutic roles for these compounds in various diseases. Perhaps most notably, the increased susceptibility of cancer cells to these compounds supports their potential use as cancer therapies, and the first generation of glycoside-based anticancer drugs are currently in clinical trials.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use*
  • Apoptosis / drug effects
  • Cardiac Glycosides / chemistry
  • Cardiac Glycosides / pharmacology
  • Cardiac Glycosides / therapeutic use*
  • Cell Proliferation / drug effects
  • Clinical Trials as Topic
  • Heart Diseases / drug therapy
  • Humans
  • Molecular Structure
  • Neoplasms / drug therapy*
  • Neoplasms / enzymology
  • Sodium-Potassium-Exchanging ATPase / antagonists & inhibitors*
  • Tumor Cells, Cultured


  • Antineoplastic Agents
  • Cardiac Glycosides
  • Sodium-Potassium-Exchanging ATPase