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首页> 外文期刊>Biochimica et biophysica acta. Molecular basis of disease: BBA >Exemestane, a new steroidal aromatase inhibitor of clinical relevance
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Exemestane, a new steroidal aromatase inhibitor of clinical relevance

机译：Exemestane，一种具有临床意义的新型甾体芳香酶抑制剂

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摘要

Breast cancer is the leading cause of death among women and the contribution of circulating oestrogens to the growth of some mammary tumours has been recognized. Consequently, suppression of oestrogen action by inhibition of their biosynthesis at the androstenedioneoestrone aromatization step, by means of selective inhibitors of the enzyme aromatase, has become an effective therapeutic option for the treatment of hormone-dependent breast cancer. Exemestane (6-methylenandrosta-1,4-diene-3,17-dione) is a novel steroidal irreversible aromatase inhibitor recently approved and introduced into the global market under the name Aromasin. The design, laboratory and viable syntheses of exemestane, starting from a variety of steroidal precursors, are presented and discussed. Data from biochemical and pharmacological studies as well as the clinical impact of the compound are briefly reviewed. The drug is an orally active and well-tolerated hormonal therapy for postmenopausal patients with advanced breast cancer that has become refractory to standard current hormonal therapies.
机译：乳腺癌是女性死亡的主要原因，循环雌激素对某些乳腺肿瘤生长的贡献已得到公认。因此，借助于酶芳香酶的选择性抑制剂，通过抑制雄烯二酮雌酮芳香化步骤的生物合成来抑制雌激素作用，已经成为治疗激素依赖性乳腺癌的有效治疗选择。 Exemestane（6-methylenandrosta-1,4-diene-3,17-dione）是一种新型甾体不可逆芳香化酶抑制剂，最近被批准并以Aromasin的名称引入全球市场。介绍和讨论了依西美坦的设计，实验室和可行的合成方法，它们是从多种甾体前体开始的。简要回顾了来自生化和药理研究的数据以及该化合物的临床影响。对于绝经后的晚期乳腺癌患者，该药物是一种口服活性良好且耐受性良好的激素疗法，该疗法已对目前的标准激素疗法产生了顽固性。

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