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芳香化酶抑制剂盐酸法倔唑预防雌性大鼠自发性肿瘤

Prevention of spontaneous tumours in female rats by fadrozole hydrochloride, an aromatase inhibitor.

作者信息

Gunson D E, Steele R E, Chau R Y

机构信息

Division of Preclinical Safety, Ciba-Geigy Corporation, Summit, New Jersey 07901, USA.

出版信息

Br J Cancer. 1995 Jul;72(1):72-5. doi: 10.1038/bjc.1995.279.

DOI:10.1038/bjc.1995.279
PMID:7639848
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2034132/
Abstract

Mammary tumours are oestrogen dependent in female Sprague-Dawley rats and in a significant proportion of women, so pharmacological treatment to inhibit oestrogen production is a valuable therapeutic measure to prevent or slow the progression of disease. Here we show that a non-steroidal aromatase inhibitor, which competitively inhibits the conversion of androstenedione to oestrone, prevents the development of both benign and malignant spontaneous mammary neoplasms in female Sprague-Dawley ats. It also slows the spontaneous development of pituitary pars distalis adenomas in female rats, and reduces the incidence of spontaneous hepatocellular tumours in male and female rats.

摘要

乳腺肿瘤在雌性斯普拉格-道利大鼠以及相当一部分女性中对雌激素依赖,因此抑制雌激素生成的药物治疗是预防或减缓疾病进展的一项重要治疗措施。在此我们表明,一种非甾体芳香化酶抑制剂,它竞争性抑制雄烯二酮向雌酮的转化,可预防雌性斯普拉格-道利大鼠良性和恶性自发性乳腺肿瘤的发生。它还能减缓雌性大鼠垂体远侧部腺瘤的自然发生,并降低雄性和雌性大鼠自发性肝细胞肿瘤的发生率。

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Prevention of spontaneous tumours in female rats by fadrozole hydrochloride, an aromatase inhibitor.芳香化酶抑制剂盐酸法倔唑预防雌性大鼠自发性肿瘤
Br J Cancer. 1995 Jul;72(1):72-5. doi: 10.1038/bjc.1995.279.
2
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本文引用的文献

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Antitumor and endocrine effects of an aromatase inhibitor (CGS 16949A) on DMBA-induced rat mammary tumor.一种芳香化酶抑制剂(CGS 16949A)对二甲基苯并蒽诱导的大鼠乳腺肿瘤的抗肿瘤和内分泌作用。
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The triphenylethylene drug tamoxifen is a strong liver carcinogen in the rat.三苯乙烯类药物他莫昔芬在大鼠中是一种强效肝脏致癌物。
Carcinogenesis. 1993 Feb;14(2):315-7. doi: 10.1093/carcin/14.2.315.
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5
Breast cancer in men. Clinical features, hormone receptor status, and response to therapy.男性乳腺癌。临床特征、激素受体状态及对治疗的反应。
Cancer. 1987 Sep 15;60(6):1337-40. doi: 10.1002/1097-0142(19870915)60:6<1337::aid-cncr2820600629>3.0.co;2-c.
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In vitro and in vivo studies demonstrating potent and selective estrogen inhibition with the nonsteroidal aromatase inhibitor CGS 16949A.体外和体内研究表明,非甾体芳香化酶抑制剂CGS 16949A具有强效和选择性雌激素抑制作用。
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CGS 16949A, a new nonsteroidal aromatase inhibitor: effects on hormone-dependent and -independent tumors in vivo.新型非甾体芳香化酶抑制剂CGS 16949A:对体内激素依赖性和非依赖性肿瘤的影响
Cancer Res. 1988 Feb 15;48(4):834-8.
8
Recent developments in aromatase inhibition as a potential treatment for oestrogen-dependent breast cancer.芳香化酶抑制作为雌激素依赖性乳腺癌潜在治疗方法的最新进展。
Prog Med Chem. 1989;26:253-98. doi: 10.1016/s0079-6468(08)70242-x.
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Inhibition of aromatase with CGS 16949A in postmenopausal women.使用CGS 16949A抑制绝经后女性的芳香化酶。
J Clin Endocrinol Metab. 1989 Jan;68(1):99-106. doi: 10.1210/jcem-68-1-99.
10
Development of antiestrogens and their use in breast cancer: eighth Cain memorial award lecture.抗雌激素药物的研发及其在乳腺癌治疗中的应用:第八届凯恩纪念奖讲座
Cancer Res. 1990 Jul 15;50(14):4177-89.