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