A permanently charged tamoxifen derivative displays anticancer activity and improved tissue selectivity in rodents

Anat Biegon; Marcus Brewster; Hadassa Degani; Emil Pop; Dalia Somjen; Alvin M. Kaye

A permanently charged tamoxifen derivative displays anticancer activity and improved tissue selectivity in rodents

Anat Biegon^*, Marcus Brewster, Hadassa Degani, Emil Pop, Dalia Somjen, Alvin M. Kaye

^*Corresponding author for this work

Research output: Contribution to journal › Article › peer-review

Abstract

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.

Original language	English
Pages (from-to)	4328-4331
Number of pages	4
Journal	Cancer Research
Volume	56
Issue number	19
State	Published - 1 Oct 1996
Externally published	Yes

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abstract = "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.",

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year = "1996",

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AU - Biegon, Anat

AU - Brewster, Marcus

AU - Degani, Hadassa

AU - Pop, Emil

AU - Somjen, Dalia

AU - Kaye, Alvin M.

PY - 1996/10/1

Y1 - 1996/10/1

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AB - 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.

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JO - Cancer Research

JF - Cancer Research

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ER -

A permanently charged tamoxifen derivative displays anticancer activity and improved tissue selectivity in rodents

Abstract

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