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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。
Aromatase inhibitors block the synthesis of endogenous estrogens in postmenopausal women and reduce circulating estrogen levels in the body, effectively blocking the growth of breast cancer and even leading to the death of cancer cells. Third-generation aromatase inhibitors - letrozole, anastrozole, vorozole (non-steroidal, type II) and exemestane (steroid type, type I) for second-line treatment Postmenopausal estrogen receptor-positive breast cancer Phase III clinical trial results show that compared with conventional treatment has obvious advantages. Recently, preliminary results of first-line treatment of metastatic breast cancer have shown that aromatase inhibitors may replace tamoxifen as first-line therapy. The new generation of aromatase inhibitors is highly selective and well tolerated, and is currently widely used clinically. This article mainly reviews the progress of aromatase inhibitors, pharmacological mechanism, clinical application and possible application prospects.