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A Permanently Charged Tamoxifen Derivative Displays Anticancer Activity and Improved Tissue Selectivity in Rodents¹

Pharmos, Ltd., Kiryat Weizmann, Rehovot 76326, Israel [A. B.]; Pharmos Corporation, Alachua, Florida 32615 [M. B., E. P.]; Departments of Biological Regulation [H. D.] and Molecular Genetics [A. M. K.], Weizmann Institute of Science, Rehovot 76100, Israel; and Endocrine Unit. Tel Aviv Medical Center, Tel Aviv 64381, Israel [D. S.]

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.

¹ Supported in part by a grant (to A. M. K.) from the Israel Cancer Association. A. M. K. is the Joseph Moss Professor of Molecular Endocrinology, Weizmann Institute of Science.

² To whom requests for reprints should be addressed. Phone: 00972-8-9409679; Fax: 00972-8-9409686.

Received 6/19/96. Accepted 8/14/96.

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