Target intelligence / Profile preview

Combretastatin A4 phosphate (CA4P)

Target
CA4P
Molecular classification
Other (small organic molecule; prodrug of combretastatin A-4), Antimitotic agent, Vascular disrupting agent
01

Overview

Combretastatin A4 phosphate is a water-soluble prodrug of combretastatin A-4, a natural stilbene derivative originally isolated from the African bushwillow tree (*Combretum afrum*). As a microtubule inhibitor, it acts by binding to the colchicine site of tubulin, halting mitosis and resulting in rapid disruption of the tumor vasculature. Its effectiveness in inducing central necrosis of tumors makes it a promising candidate for anti-cancer therapy, commonly used as a vascular disrupting agent especially in combination with chemotherapy. CA4P is delivered as a phosphate salt to improve solubility and is converted to the active form (combretastatin A-4) in the body

Other names
FosbretabulinCombretastatin A-4 phosphateCA4PCA4PDfosbretabulin disodiumfosbretabulin tromethamineCRC 8709
02

Mechanism of action

Prodrug rapidly converted to combretastatin A-4 in vivo; CA-4 binds to the colchicine site on tubulin, inhibits tubulin polymerization, destabilizes microtubules, disrupts tumor vasculature, and induces tumor necrosis

03

Biological functions

Anti-angiogenesisTumor vascular disruptionInduction of central necrosis in tumors
04

Disease associations

Cancer (notably anaplastic thyroid cancer, non-small cell lung cancer, solid tumors)
05

Safety considerations

Extensive tumor necrosis may lead to secondary tissue effects (e.g., inflammation)Potential off-target vascular effectsCardiovascular riskPoor water solubility of CA-4 (parent compound)
06

Interacting drugs

carboplatin

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