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Existing and emerging endocrine therapies for breast cancer.

机译：现有和新兴的内分泌治疗乳腺癌的方法。

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Endocrine therapy is first-line therapy for patients with estrogen receptor-positive or progesterone receptor-positive metastatic breast cancer. Commonly used endocrine therapies are tamoxifen, megestrol acetate, and aromatase inhibitors. Although tamoxifen and megestrol acetate have a favorable therapeutic profile, there are risks associated with these agents. With tamoxifen, the partial agonist property can lead to thromboembolic events. An important adverse event of megestrol acetate is weight gain and fluid retention in some patients. The aromatase inhibitors are currently used as second-line therapy after tamoxifen failure. A recent study showed that anastrozole, an aromatase inhibitor, is as effective or even superior to tamoxifen when used as a first-line therapy. However, not all patients will respond to currently available therapies. A new class of drug, the estrogen receptor downregulators, has been developed. Fulvestrant, the first agent in this new class, not only induces the degradation ofthe estrogen receptor but also is an estrogen antagonist; further, its lack of agonist activity provides a better safety profile. Two phase III trials have proven that fulvestrant is at least as effective as anastrozole in postmenopausal women with advanced breast cancer. Fulvestrant is an effective and safe endocrine therapy for postmenopausal women who have failed prior endocrine therapy.
机译：内分泌治疗是雌激素受体阳性或孕激素受体阳性转移性乳腺癌患者的一线治疗。常用的内分泌疗法是他莫昔芬，醋酸孕甾酮和芳香酶抑制剂。尽管他莫昔芬和醋酸孕甾酮具有良好的治疗效果，但存在与这些药物相关的风险。使用他莫昔芬时，部分激动剂性质可能导致血栓栓塞事件。醋酸孕甾酮的一个重要不利事件是某些患者的体重增加和体液retention留。他莫昔芬失败后，芳香酶抑制剂目前被用作二线治疗。最近的一项研究表明，芳香酶抑制剂阿那曲唑在用作一线治疗时与他莫昔芬同样有效，甚至优于他莫昔芬。但是，并非所有患者都会对当前可用的疗法产生反应。已经开发出一类新的药物，雌激素受体下调剂。氟色农酯是这一新类中的第一种药物，它不仅诱导雌激素受体降解，而且还是雌激素拮抗剂。此外，其缺乏激动剂活性提供了更好的安全性。两项III期临床试验已证明，氟维司群对绝经后晚期乳腺癌妇女的疗效至少与阿那曲唑相同。 Fulvestrant是对内分泌治疗失败的绝经后妇女的一种有效且安全的内分泌治疗。

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