The anticancer drug edelfosine is a potent inhibitor of neovascularization in vivo.

Edelfosine is an alkyl-lysophospholipid that acts as an anticancer agent in vivo. To test the hypothesis that part of its antineoplastic activity may be due to its ability to inhibit the neovascularization on which the progressive growth of all tumors depends, we evaluated edelfosine in vitro and in vivo for antiangiogenic activity. Edelfosine acted directly on cultured capillary endothelial cells, inhibiting their migration toward the angiogenic factor, basic fibroblastic growth factor (bFGF), at doses of 8-200 nM. When given systemically to rats (20 mg/kg i.p. twice daily), edelfosine was well tolerated and antiangiogenic. The majority of treated animals became unable to mount a corneal neovascular response to a pellet releasing bFGF, whereas vigorous vessel ingrowth was seen in untreated controls.