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氟维司群是一种雌激素受体下调剂,其降低细胞更新指数的效果比他莫昔芬更显著。

Fulvestrant, an estrogen receptor downregulator, reduces cell turnover index more effectively than tamoxifen.

作者信息

Bundred Nigel J, Anderson Elizabeth, Nicholson Robert I, Dowsett Mitchell, Dixon Michael, Robertson John F

机构信息

Department of Surgery, South Manchester University Hospital Education and Research Centre, UK.

出版信息

Anticancer Res. 2002 Jul-Aug;22(4):2317-9.


DOI:
PMID:12174920
Abstract

BACKGROUND: This study was performed to determine whether drug action on breast tumours could also be analysed using a cell turnover index (CTI), a composite measurement of both proliferation and apoptosis. MATERIALS AND METHODS: Data were obtained from a randomized, placebo-controlled trial comparing three single doses (50, 125 and 250 mg) of intramuscular fulvestrant (Faslodex, previously known as ICI 182,780) with oral tamoxifen 20 mg/day for 14-21 days in women with early, operable, ER-positive breast cancer. CTI was calculated as the ratio of the proliferation index to the apoptotic index. RESULTS: Fulvestrant 250 mg significantly reduced CTI compared with both placebo (p = 0.0003) and tamoxifen (p = 0.026). The effect on CTI with tamoxifen was not significantly different from that with placebo. CONCLUSION: This study suggests that CTI may be a useful indicator of drug action on breast tumour growth. A significant reduction in growth was found with fulvestrant 250 mg compared with tamoxifen.

摘要

背景:本研究旨在确定是否也可以使用细胞更新指数(CTI)来分析药物对乳腺肿瘤的作用,CTI是增殖和凋亡的综合测量指标。 材料与方法:数据来自一项随机、安慰剂对照试验,该试验比较了三种单剂量(50、125和250mg)的肌肉注射氟维司群(芙仕得,先前称为ICI 182,780)与口服他莫昔芬20mg/天,持续14 - 21天,用于早期、可手术、雌激素受体阳性乳腺癌女性。CTI计算为增殖指数与凋亡指数之比。 结果:与安慰剂(p = 0.0003)和他莫昔芬(p = 0.026)相比,250mg氟维司群显著降低了CTI。他莫昔芬对CTI的影响与安慰剂无显著差异。 结论:本研究表明CTI可能是药物对乳腺肿瘤生长作用的有用指标。与他莫昔芬相比,250mg氟维司群使肿瘤生长显著降低。

相似文献

[1]
Fulvestrant, an estrogen receptor downregulator, reduces cell turnover index more effectively than tamoxifen.

Anticancer Res. 2002

[2]
Comparison of the short-term biological effects of 7alpha-[9-(4,4,5,5,5-pentafluoropentylsulfinyl)-nonyl]estra-1,3,5, (10)-triene-3,17beta-diol (Faslodex) versus tamoxifen in postmenopausal women with primary breast cancer.

Cancer Res. 2001-9-15

[3]
Estrogen induces death of tamoxifen-resistant MCF-7 cells: contrasting effect of the estrogen receptor downregulator fulvestrant.

J Steroid Biochem Mol Biol. 2006-3

[4]
Combination treatment with fulvestrant and various cytotoxic agents (doxorubicin, paclitaxel, docetaxel, vinorelbine, and 5-fluorouracil) has a synergistic effect in estrogen receptor-positive breast cancer.

Cancer Sci. 2011-9-1

[5]
Tamoxifen inhibits nerve growth factor-induced proliferation of the human breast cancerous cell line MCF-7.

Cancer Res. 2001-4-1

[6]
Oestrogen receptor-mediated modulation of the EGFR/MAPK pathway in tamoxifen-resistant MCF-7 cells.

Breast Cancer Res Treat. 2003-9

[7]
Faslodex (ICI 182, 780), a novel estrogen receptor downregulator--future possibilities in breast cancer.

J Steroid Biochem Mol Biol. 2001-12

[8]
Effects of CH4893237, a new orally active estrogen receptor downregulator, on breast cancer xenograft models with low serum estrogen levels.

Oncol Rep. 2009-3

[9]
Effects of a pure antiestrogen on apoptosis and proliferation within human breast ductal carcinoma in situ.

Cancer Res. 2000-8-1

[10]
Antiproliferative effects of idoxifene in a placebo-controlled trial in primary human breast cancer.

Clin Cancer Res. 2000-6

引用本文的文献

[1]
Estradiol (E2) concentration shapes the chromatin binding landscape of estrogen receptor alpha.

J Biol Chem. 2025-4-9

[2]
Fulvestrant: A Review in Advanced Breast Cancer Not Previously Treated with Endocrine Therapy.

Drugs. 2018-1

[3]
Nuclear receptors and their selective pharmacologic modulators.

Pharmacol Rev. 2013-3-1

[4]
Activation of the mTOR pathway by low levels of xenoestrogens in breast epithelial cells from high-risk women.

Carcinogenesis. 2011-9-1

[5]
Fulvestrant: a review of its use in the management of hormone receptor-positive metastatic breast cancer in postmenopausal women.

Drugs. 2011-2-12

[6]
Fulvestrant: an oestrogen receptor antagonist with a novel mechanism of action.

Br J Cancer. 2004-3

[7]
Fulvestrant: a review of its use in hormone receptor-positive metastatic breast cancer in postmenopausal women with disease progression following antiestrogen therapy.

Drugs. 2004

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