芳香酶抑制剂治疗乳腺癌的研究进展  

Aromatase inhibitors in the treatment of breast cancer

作　　者：安富荣[1] 程华丰[1] 张楠森[1] 

机构地区：[1]上海第二医科大学仁济医院临床药学药理研究室,上海,200001

出　　处：《药学服务与研究》2001年第1期52-56,共5页Pharmaceutical Care and Research

摘　　要：芳香酶抑制剂通过阻断绝经后妇女内源性雌激素的合成,降低体内循环雌激素水平,达到有效阻滞乳腺癌生长.甚至导致癌细胞死亡的效应。第三代芳香酶抑制剂-来曲唑（letrozole）、阿那曲唑（anastrozole）、vorozole（非甾体型,Ⅱ型）和伊西美坦（exemestane）（甾体型,Ⅰ型）,用于二线治疗绝经后雌激素受体阳性的乳腺癌Ⅲ期临床试验结果表明,与常规治疗相比具有明显的优越性。最近,一线治疗转移性乳腺癌的初步试验结果表明,芳香酶抑制剂有可能取代他莫昔芬（tamoxifen）作为一线治疗药物。新一代芳香酶抑制剂的选择性高,耐受性好,目前在临床上得到广泛的应用。本文主要对芳香酶抑制剂的研究进展、药理作用机理、临床应用和可能的应用前景等做一综述。In postmenopausal women, aromatase inhibitors can prevent the synthesis of estrogens and significantly reduce plasma estrogen levels, and this has been associated with tumour regression in patients with estrogen-dependent breast cancer. The third-generation aromatase inhibitors- letrozole, anastrozole, vorozole (nonsteroidal, type II ) and exemestane (steroidal. type I ) have now been tested in phase III trials as second-line treatment of postmenopausal hormone-dependent breast cancer. They have shown clear superiority compared with the conventional therapies and are therefore considered established second-line hormonal agents. Currently, they are being tested as first-line therapy in the metastatic settings, and preliminary results suggest that the inhibitors might displace tamoxifen as first-line treatment. The new aromatase inhibitors are highly selective and very well tolerated by patients clinically. In this paper, the development, mechanism of action, the current clinical status and possible future applications of the aromatase inhibitors are reviewed.

关 键 词：芳香酶抑制剂 乳腺肿瘤 药理学 临床 药物疗法 

分 类 号：R737.9[医药卫生—肿瘤] R979.1[医药卫生—临床医学]