A PERMANENTLY CHARGED TAMOXIFEN DERIVATIVE DISPLAYS ANTICANCER ACTIVITY AND IMPROVED TISSUE SELECTIVITY IN RODENTS

A quaternized form of tamoxifen (TAM), tamoxifen methiodide (TMI), was shown to demonstrate very low brain uptake compared to TAM and, unexp ectedly, was considerably less estrogenic than TAM in the uterus. The agonist activity of TMI in the bone was similar to that of TAM. TMI ma nifested significant dose-dependent tumoricidal activity with a rapid onset of action against MCF-7 human breast cancer implants in nude mic e and a mean reduction in tumor size of 60% over six weeks.