Vascular disrupting agents

Bioorg Med Chem. 2007 Jan 15;15(2):605-15. doi: 10.1016/j.bmc.2006.10.020. Epub 2006 Oct 27.


A clear definition for vascular targeting agents (VTAs) and vascular disrupting agents (VDAs) has separated the two as distinct methods of cancer treatment. VDAs differ from VTAs (antiangiogenesis drugs) in their mechanism of action. VTAs attempt to keep new blood vessels from forming and do not act on blood vessels that already feed existing tumors. In contrast, VDAs cause the vascular structure inside a solid tumor to collapse, depriving the tumor of blood and oxygen it needs to survive. Therefore, VDAs are an attractive way to approach the cancer problem by combating developed tumors. The following review discusses six small molecule VDAs, namely DMXAA, ZD6126, TZT1027, CA4P, AVE8062, and Oxi4503, their synthesis, biological mechanism of action, and current clinical status.

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology*
  • Blood Vessels / drug effects*
  • Cardiovascular Agents / pharmacology*
  • Flavonoids / pharmacology
  • Humans
  • Neoplasms / blood supply*
  • Neoplasms / drug therapy*
  • Terminology as Topic
  • Tubulin / metabolism


  • Antineoplastic Agents
  • Cardiovascular Agents
  • Flavonoids
  • Tubulin