1983
DOI: 10.1677/joe.0.0990447
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Comparison of the biological effects of tamoxifen and a new antioestrogen (LY 117018) on the immature rat uterus

Abstract: The uterotrophic and antiuterotrophic activities of tamoxifen and 6-hydroxy-2-(p-hydroxyphenyl)-benzo(b)thien-3-yl p- less than 2-(1-pyrrolidinyl) ethoxyphenyl ketone (LY 117018) in the immature rat uterus have been evaluated. The antioestrogens were administered alone, concurrently or sequentially with or without oestradiol. LY 117018 administered alone was less uterotrophic (oestrogenic) than tamoxifen. At high doses, when administered concurrently with oestradiol, LY 117018 was more antiuterotrophic (antioe… Show more

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Cited by 26 publications
(13 citation statements)
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“…This model contains high circulating levels of plasma estradiol over the dosing period of the study as a result of the estrogen pellets used to drive growth of the MCF-7 cells as a xenograft. With plasma levels between 750 and 1,000 pg/mL over day [21][22][23][24][25][26][27][28][29][30][31][32][33][34][35], this model is more representative of the premenopausal setting where estrogen levels can vary between 20 and 400 pg/mL (47). As the receptor binding data does not suggest a significant difference in affinity for the receptor between AZD9496 and fulvestrant, increased efficacy is likely due to the higher free drug levels of AZD9496 versus fulvestrant in this model.…”
Section: Discussionmentioning
confidence: 99%
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“…This model contains high circulating levels of plasma estradiol over the dosing period of the study as a result of the estrogen pellets used to drive growth of the MCF-7 cells as a xenograft. With plasma levels between 750 and 1,000 pg/mL over day [21][22][23][24][25][26][27][28][29][30][31][32][33][34][35], this model is more representative of the premenopausal setting where estrogen levels can vary between 20 and 400 pg/mL (47). As the receptor binding data does not suggest a significant difference in affinity for the receptor between AZD9496 and fulvestrant, increased efficacy is likely due to the higher free drug levels of AZD9496 versus fulvestrant in this model.…”
Section: Discussionmentioning
confidence: 99%
“…The rat uterine weight assay for the measurement of estrogenic activity was performed as described previously (31). Details of individual models, protein analysis of tumor fragments, and pharmacokinetic analysis of plasma samples are included in Supplementary Methods.…”
Section: Rat Uterine and Xenograft Studiesmentioning
confidence: 99%
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“…Tamoxifen shows both oestrogenic and antioestrogenic effects (Clark & Peck, 1979;Rochefort et al, 1983;Wakeling et al, 1983). The balance of these effects varies between tissues (Clark & Peck, 1979) and even within the same cell (Rochefort et al, 1983).…”
Section: Discussionmentioning
confidence: 99%
“…The balance of these effects varies between tissues (Clark & Peck, 1979) and even within the same cell (Rochefort et al, 1983). In the immature rat uterus tamoxifen shows greater oestrogenic activity in the presence of low concentrations of oestrogen (Wakeling et al, 1983) (Brodie et al, 1983).…”
Section: Discussionmentioning
confidence: 99%