RU-58-668, A NEW PURE ANTIESTROGEN INDUCING A REGRESSION OF HUMAN MAMMARY-CARCINOMA IMPLANTED IN NUDE-MICE

被引:99
作者
VANDEVELDE, P
NIQUE, F
BOUCHOUX, F
BREMAUD, J
HAMEAU, MC
LUCAS, D
MORATILLE, C
VIET, S
PHILIBERT, D
TEUTSCH, G
机构
[1] Centre de Recherches Roussel UCLAF
关键词
D O I
10.1016/0960-0760(94)90144-9
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
RU 58 668, a new steroidal antiestrogen, has been synthesized. Its in vitro and in vivo pharmacological activities have been compared to those of tamoxifen and ICI 182,780. In vitro, it displayed affinities for human and murine estrogen receptors equivalent to those of 4-hydroxy-tamoxifen, along with moderate affinities for progestin and glucocorticoid receptors. RU 58 668 proved to be a potent antiproliferative agent on MCF-7 cells stimulated by estradiol, or by exogenous or endogenous growth factors (IC50, 0.01 nM). It also inhibited the growth of the insulin-stimulated T47D cell line. In vivo, RU 58 668 displayed a total antiuterotrophic activity in mice or rats without exhibiting any agonistic effect. Moreover, RU 58 668 was the only antiestrogenic compound tested so far to be able to induce a long term regression of human mammary MCF-7 tumors implanted in nude mice, suggesting its potential use for the treatment of advanced breast cancer.
引用
收藏
页码:187 / 196
页数:10
相关论文
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