A permanently charged tamoxifen derivative displays anticancer activity and improved tissue selectivity in rodents
Biegon, A.; Brewster, M.; Degani, H.; Pop, E.; Somjen, D.; Kaye, A.M.
Cancer Research 56(19): 4328-4331
1996
ISSN/ISBN: 0008-5472 PMID: 8813117 Document Number: 457259
A quaternized form of tamoxifen (TAM), tamoxifen methiodide (TMI), was shown to demonstrate very low brain uptake compared to TAM and, unexpectedly, was considerably less estrogenic than TAM in the uterus. The agonist activity of TMI in the bone was similar to that of TAM. TMI manifested significant dose-dependent tumoricidal activity with a rapid onset of action against MCF-7 human breast cancer implants in nude mice and a mean reduction in tumor size of 60% over six weeks.