Synthetic Antiangiogenic Agents

Table 5.3 Examples of Angiogenesis-Related Conditions3

Synthetic Antiangiogenic Agents

Table 5.3 Examples of Angiogenesis-Related Conditions3

Malignant tumors



Hemophilic joints




Pyogenic granuloma


Atherosclerotic plaques

Diabetic retinopathy

Hypertrophic scars

Neovascular glaucoma

Retrolental fibroplasias

Macular degeneration


Vascular restenosis

Vascular adhesions

Corneal graft neovascularization


Arteriovenous malformations


Hemorrhagic telangiectasia

Rheumatoid arthritis

volved in regulating endothelial cell shape and division (49-52). Microtubules are composed of tubulin polymers (53). Drugs capable of interfering with tubulin polymerization would therefore be expected to be effective antiangiogenic agents (54).

Combretastatin A4 (Fig. 5.6) is a tubulin-binding compound that was initially isolated from the South African tree Combretan caffrum (55, 56). This lipophilic cis stilbene destabilizes microtubules, thus affecting the cytoskeleton of dividing endothelial cells, causing apoptosis and inhibiting angiogenesis (53,54, 56-58).

The solubility of combretastatin A4 was increased by attaching a phosphate moiety (59). The resulting compound, combretastatin A4 3-o-phosphate is a water-soluble prodrug whose phosphate moiety is cleaved in vivo by serum phosphatases to generate the active drug. This prodrug (developed by Oxigene is currently in phase I clinical trials to evaluate its effects on tumor vasculature (54, 60).

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