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[芳香化酶抑制剂:药理学方面]

[Aromatase inhibitors: pharmacological aspects].

作者信息

de Crémoux P

机构信息

Laboratoire de physiopathologie et de pharmacologie, Institut Curie, 26, rue d'Ulm, 75248 Paris Cedex 05, France.

出版信息

Bull Cancer. 2000 Dec;87 Spec No:23-29.

Abstract

Selective new aromatase inhibitors are a new class of agents that are of considerable interest in the treatment of hormone-dependent breast cancer in postmenopausal women. Aromatase is an enzymic complex that catalyses the conversion of the adrenal androgens androstenedione and testosterone to estrone. In postmenopausal women, the process of peripheral aromatisation accounts for the majority of circulating estrogens. The selective inhibition of estrogen production by aromatase inhibitors is an efficient strategy for breast cancer treatment. These compounds are classified as irreversible inhibitors of aromatase (type I), and comprise steroidal compounds. Reversible inhibitors of aromatase, which comprises non-steroidal compounds are type II aromatase inhibitors. Second and third generation aromatase inhibitors are considerably more potent and more specific in their ability to inhibit aromatase, as compared with first generation compounds (aminoglutethimide).

摘要

选择性新型芳香化酶抑制剂是一类新型药物,在治疗绝经后女性激素依赖性乳腺癌方面备受关注。芳香化酶是一种酶复合物,可催化肾上腺雄激素雄烯二酮和睾酮转化为雌酮。在绝经后女性中,外周芳香化过程是循环雌激素的主要来源。芳香化酶抑制剂选择性抑制雌激素生成是治疗乳腺癌的有效策略。这些化合物被归类为芳香化酶的不可逆抑制剂(I型),包括甾体化合物。由非甾体化合物组成的芳香化酶可逆抑制剂是II型芳香化酶抑制剂。与第一代化合物(氨鲁米特)相比,第二代和第三代芳香化酶抑制剂在抑制芳香化酶的能力上更强且更具特异性。

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