Antivascular therapy of cancer: DMXAA

Lancet Oncol. 2003 Mar;4(3):141-8. doi: 10.1016/s1470-2045(03)01018-0.


The vascular endothelium of tumour tissue, which differs in several ways from that of normal tissues, is a potential target for selective anticancer therapy. By contrast with antiangiogenic agents, antivascular agents target the endothelial cells of existing tumour blood vessels, causing distortion or damage and consequently decreasing tumour blood flow. DMXAA (5,6-dimethylxanthenone-4-acetic acid), a low-molecular-weight drug, has a striking antivascular and in some cases curative effect in experimental tumours. Its action on vascular endothelial cells seems to involve a cascade of events leading to induction of tumour haemorrhagic necrosis. These events include both direct and indirect effects, the latter involving the release of further vasoactive agents, such as serotonin, tumour necrosis factor, other cytokines, and nitric oxide from host cells. Phase I clinical trials of DMXAA have been completed and the next challenge to face is how the antivascular effect of this drug should be exploited for the treatment of human cancer.

Publication types

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

MeSH terms

  • Antineoplastic Agents / pharmacology*
  • Antineoplastic Agents / therapeutic use
  • Drug Design
  • Drugs, Investigational*
  • Endothelium, Vascular / drug effects
  • Humans
  • Microcirculation / drug effects
  • NF-kappa B / drug effects
  • Neoplasms / blood supply
  • Neoplasms / drug therapy*
  • Xanthenes / pharmacology*
  • Xanthenes / therapeutic use
  • Xanthones*


  • Antineoplastic Agents
  • Drugs, Investigational
  • NF-kappa B
  • Xanthenes
  • Xanthones
  • vadimezan