依西美坦

结论caspase-3调控异位内膜间质细胞的凋亡；依西美坦增加caspase-3的表达，促进异位内膜间质细胞凋亡。

Conclusions Caspase-3 regulates the apoptosis of ectopic endometrial stromal cells , exemestane enhances the expression of caspase-3 , and promotes the apoptosis of ectopic endometrial stromal cells .

反向添加雌激素可阻断依西美坦的作用。

The add - back of estrodiol could block the action of exemestane .

RP-HPLC法测定依西美坦片中依西美坦的含量及其有关物质

Determination of Exemestane and Its Related Compounds in Tablets by RP-HPLC

方法：以雄甾烯二酮为原料，经Mannich反应、溴化、脱溴等数步反应制得依西美坦。

METHOD : This compound was synthesized by steps of Mannich reaction , bromination , and debromination .

检测波长247nm。结果依西美坦在40～210.6μg/ml浓度范围内线性关系良好，平均回收率为99.97%，RSD为0.57%，最小检出浓度为0.4112μg/ml。

RESULTS Exemestane had a good linear relation in the range of 40 ~ 210.6 μ g / ml , the average recovery was 99.97 % , the RSD was 0.57 % and the limit concentration was 0.4112 μ g / ml.

依西美坦作用72h后，异位间质细胞雌激素合成减少，β-内啡肽的表达增加，凋亡率升高（P<0.05）；

72h after Exemestane reacted , the estrogen synthesized by the ectopic stromal cells was down regulated , the expression of β - endorphin was unregulated and the apoptosis rate was higher ( P < 0.05 ) .

传统的制备方法是以全化学工艺合成，而依西美坦合成最重要的一步C1,2位脱氢时要使用DDQ等大量有毒有害化学试剂，且产物较难分离。

Exemestane is traditionally synthesized by chemical method . But some toxic and hazardous chemicals such as DDQ are used in 1-dehydrogenation which is the most important step in the synthesis of exemestane . And it is very difficult to extract exemestane from the by-products .

目的：研究依西美坦胶囊与依西美坦片的生物等效性。

OBJECTIVE : To study the bioequivalence of exemestane capsule and exemestane tablet .

本文综述了依西美坦的化学合成、药理作用及临床应用。

The chemical synthesis , pharmacological action and clinical trial of exemestane were reviewed .

新型抗肿瘤药物依西美坦

Exemestane , a new anti-tumor drug

卵巢切除联合依西美坦治疗绝经前激素受体阳性晚期难治性乳腺癌

Of or relating to the menopause . Oophorectomy combined with exemestane treating advanced refractory breast cancer

依西美坦治疗晚期转移性乳腺癌195例多中心随机对照研究

Treatment of advanced metastatic breast cancer with exemestane , a multicenter randomized controlled study of 195 cases

依西美坦的有效率在不同的年龄、绝经时间、无病间期和受体来源于不同阶段病情的患者中，差异均无显著性（P>0.05）。

There was no significant difference in different ages , time of menopause , disease-free interval or receptor status ( P > 0.05 ) .

结果依西美坦是口服有效的芳香化酶灭活剂，其耐受性好、安全性高，在乳腺癌的辅助治疗、新辅助治疗及转移性乳腺癌的治疗中均取得较好疗效。

Results Exemestane is an effective steroidal aromatase inactivator with superior tolerability , safety and efficacy in the adjuvant , neo-adjuvant and metastatic therapy of breast cancer .

目的：探讨NO/ET与异位子宫内膜间质细胞凋亡的关系以及芳香化酶抑制剂依西美坦的作用。

Objective : To investigate the relationship between NO / ET and the apoptosis of ectopic uterine endometrial stromal cells , and the effect of aromatase inhibitor exemestane .

依西美坦为第三代甾体类芳香化酶抑制剂，临床上治疗绝经后妇女晚期乳腺癌，作用机制为与芳香化酶底物结合位点不可逆结合使芳香化酶失活。

Exemestane is a third-generation steroidal aromatase inhibitor which can cause inactivation of aromatase enzyme by binding irreversibly to the substrate binding site and can be used to treat advanced breast cancer in postmenopausal women .

结论：β-内啡肽与异位子宫内膜间质细胞的凋亡有关，依西美坦经降调β-内啡肽的表达而增加异位内膜间质细胞的凋亡，反加雌激素可以阻断这一作用。

Conclusion : There is relationship between the β - endorphin and apoptosis of ectopic uterine endometrial cells , Exemestane increased apoptosis rate of the ectopic stromal cells by down regulating the expression of β - endorphin , the add-back of estrodiol may block the action .