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).