Tesmilifene, an analog of tamoxifen, acts as a chemopotentiator and antineoplastic agent and was developed for the treatment of breast cancer but never marketed.1 It binds with high affinity to the anti-estrogen binding site (AEBS) in rat liver microsomes but does not bind to the estrogen receptor (at or below 10 µM) .2 Displaces histamine from AEBS, an activity which correlates with its cytotoxic effects on breast cancer cells.2 Enhances the cytotoxicity of taxol, epirubicin, doxorubicin and vinorelbine in multidrug resistance cell lines.3 It has been shown to increase the permeability of the blood-brain and blood-glioma barrier in culture and animal models by modifying brain endothelial functions.4
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