MICROSPHERE-ENCAPSULATED 4OH-TAMOXIFEN: A NEW SUSTAINED RELEASE DELIVERY SYSTEM WITH ANTITUMOUR ACTIVITY AGAINST DMBA-INDUCED MAMMARY CARCINOMA IN SPRAGUE-DAWLEY RATS

Authors: P Auvray, F Bichat, G Griffon-Etienne, A Bataille, N Guilbaud, E Vuaridel, A Carrio, M. Bayssas, and P Genne
Oncodesign; Debiopharma

Abstract: Tamoxifen (TAM), a synthetic non-steroidal anti-estrogenic compound, is considered as the standard treatment of postmenopausal advanced breast cancer. 4-hydroxytamoxifen (4OH-TAM), one of its hydroxylated metabolites, may be responsible for a major part of the effects of TAM in vivo, with an affinity towards the estrogen receptor (ER) of 10- to 100-fold stronger (ref.1,2). Consequently, the use of 4OH-TAM would be of interest in women, but is limited by its inactivation in the liver when administered per os (PO) (ref.3).

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