A vascular-targeting agent (VTA) or vascular disrupting agent (VDA) is a drug designed to damage the vasculature (

blood vessel Blood vessels are the tubular structures of a circulatory system that transport blood throughout many Animal, animals’ bodies. Blood vessels transport blood cells, nutrients, and oxygen to most of the Tissue (biology), tissues of a Body (bi ...

s) of

cancer Cancer is a group of diseases involving Cell growth#Disorders, abnormal cell growth with the potential to Invasion (cancer), invade or Metastasis, spread to other parts of the body. These contrast with benign tumors, which do not spread. Po ...

tumor A neoplasm () is a type of abnormal and excessive growth of tissue. The process that occurs to form or produce a neoplasm is called neoplasia. The growth of a neoplasm is uncoordinated with that of the normal surrounding tissue, and persists ...

s causing central

necrosis Necrosis () is a form of cell injury which results in the premature death of cells in living tissue by autolysis. The term "necrosis" came about in the mid-19th century and is commonly attributed to German pathologist Rudolf Virchow, who i ...

. VTAs can be small-molecule or

ligand In coordination chemistry, a ligand is an ion or molecule with a functional group that binds to a central metal atom to form a coordination complex. The bonding with the metal generally involves formal donation of one or more of the ligand's el ...

-based. Small-molecule VTAs include: *

microtubule Microtubules are polymers of tubulin that form part of the cytoskeleton and provide structure and shape to eukaryotic cells. Microtubules can be as long as 50 micrometres, as wide as 23 to 27 nanometer, nm and have an inner diameter bet ...

destabilizing drugs such as

combretastatin A-4 disodium phosphate Fosbretabulin (also known as combretastatin A-4 phosphate or CA4P) is a microtubule destabilizing experimental drug, a type of vascular-targeting agent, a drug designed to damage the vasculature (blood vessels) of cancer tumours causing central n ...

(CA4P),

ZD6126 ZD6126 is a vascular-targeting agent and a prodrug of N-acetylcolchinol, related to colchicine. It has shown promising results on tumors in mice. A phase I clinical trial identified gastrointestinal and cardiac effects as limiting dosing. Tw ...

AVE8062 Ombrabulin was an experimental drug candidate discovered by Ajinomoto and further developed by Sanofi-Aventis. Ombrabulin is a combretastatin A-4 derivative that exerts its antitumor effect by disrupting the formation of blood vessels needed for t ...

, Oxi 4503 *

vadimezan Vadimezan (also known as or ASA404 and dimethylxanthenone acetic acid or DMXAA) is a tumor- vascular disrupting agent (tumor-VDA) that attacks the blood supply of a cancerous tumor to cause tumor regression. Clinical trials Non-small cell lung ...

(ASA404)

Clinical trials

Phase II : ZD6126, CA4P,

plinabulin Plinabulin (provisional name BPI-2358, formerly NPI-2358) is a small molecule under development by BeyondSpring Pharmaceuticals, and has completed a world-wide Phase 3 clinical trial for non-small cell lung cancer. Plinabulin is being investigate ...

(NPI-2358) Phase III : DMXAA (ASA404).

References

{{antineoplastic-drug-stub Cancer treatments Drugs acting on the cardiovascular system