Fosbretabulin (also known as combretastatin A-4 phosphate or CA4P) is a microtubule destabilizing experimental drug, a type of

vascular-targeting agent A vascular-targeting agent (VTA) or vascular disrupting agent (VDA) is a drug designed to damage the vasculature (blood vessels) of cancer tumors causing central necrosis. VTAs can be small-molecule or ligand-based. Small-molecule VTAs include: * ...

, a drug designed to damage the vasculature (blood vessels) of cancer tumours causing central necrosis. It is a derivative of combretastatin. It is formulated as the

salts In chemistry, a salt or ionic compound is a chemical compound consisting of an assembly of positively charged ions ( cations) and negatively charged ions (anions), which results in a compound with no net electric charge (electrically neutral). ...

fosbretabulin disodium and fosbretabulin tromethamine. Fosbretabulin is a

prodrug A prodrug is a pharmacologically inactive medication or compound that, after intake, is metabolized (i.e., converted within the body) into a pharmacologically active drug. Instead of administering a drug directly, a corresponding prodrug can be ...

. ''

In vivo Studies that are ''in vivo'' (Latin for "within the living"; often not italicized in English) are those in which the effects of various biological entities are tested on whole, living organisms or cells, usually animals, including humans, an ...

'', it is dephosphorylated to its

active metabolite An active metabolite, or pharmacologically active metabolite is a biologically active metabolite of a xenobiotic substance, such as a drug or environmental chemical. Active metabolites may produce therapeutic effects, as well as harmful effects. ...

combretastatin A-4 Combretastatin A-4 is a combretastatin and a stilbenoid. It can be isolated from ''Combretum afrum'', the Eastern Cape South African bushwillow tree or in '' Combretum leprosum'', the mofumbo, a species found in Brazil. Function Tubulin repres ...

. In July 2007, the pharmaceutical company OXiGENE initiated a 180-patient phase III clinical trial of fosbretabulin in combination with

carboplatin Carboplatin, sold under the brand name Paraplatin among others, is a chemotherapy medication used to treat a number of forms of cancer. This includes ovarian cancer, lung cancer, head and neck cancer, brain cancer, and neuroblastoma. It is a ...

for the treatment of

anaplastic thyroid cancer Anaplastic thyroid cancer (ATC), also known as anaplastic thyroid carcinoma, is an aggressive form of thyroid cancer characterized by uncontrolled growth of cells in the thyroid gland. This form of cancer generally carries a very poor prognosis d ...

. There is currently no fully FDA approved treatment for this form of cancer. By 2017, it had completed multiple clinical trials (e.g. for solid tumours, non-small cell lung cancer) with more in progress.

References

Prodrugs Experimental cancer drugs Phosphate esters {{antineoplastic-drug-stub

See also

References