Cardiac glycosides in cancer therapy: from preclinical investigations towards clinical trials

Invest New Drugs. 2013 Aug;31(4):1087-94. doi: 10.1007/s10637-013-9984-1. Epub 2013 Jun 10.


Cardiac glycosides have a long history in the treatment of cardiac disease. However, several preclinical studies as well as two phase I studies have shown that cardenolides may also possess anticancer effects. The mechanisms of these anticancer effects may include intracellular decrease of K(+) and increase of Na(+) and Ca(2+); intracellular acidification; inhibition of IL-8 production and of the TNF-α/NF-κB pathway; inhibition of DNA topoisomerase II and activation of the Src kinase pathway. To date three cardiac glycosides have been developed for treatment of cancer and were tested in a phase 1 clinical trial to determine dose limiting toxicities and maximum tolerated dose. Future studies of this novel class of anticancer drugs are warranted to determine their possible role in cancer treatment.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use
  • Cardiac Glycosides / chemistry
  • Cardiac Glycosides / pharmacology
  • Cardiac Glycosides / therapeutic use*
  • Cell Death / drug effects
  • Clinical Trials as Topic*
  • Drug Screening Assays, Antitumor
  • Humans
  • Neoplasms / drug therapy*


  • Antineoplastic Agents
  • Cardiac Glycosides