乳腺癌内分泌药物治疗的研究进展  

Research advances in new endocrine therapy drugs of breast cancer

作　　者：蒋维平 

机构地区：[1]常州方圆制药有限公司,常州213022

出　　处：《中国新药杂志》2013年第5期556-560,592,共6页Chinese Journal of New Drugs

摘　　要：乳腺癌是严重影响妇女身心健康甚至危及生命的恶性肿瘤之一。传统的乳腺癌内分泌治疗药物是作用于雌激素环节的雌激素受体调节剂、芳香化酶抑制剂,但芳香化酶抑制剂的选择性较差,有中度的治疗相关毒性,如高血脂、骨丢失、肝脂肪化等,因此需要开发具有组织选择性、高效低毒的芳香化酶抑制剂。此外,新型的甾体硫酸酯酶抑制剂也已成为有效的激素依赖性乳腺癌(HDBC)治疗药物,氨基磺酸酯基团被证实是这类药物中的药效团。本文综述了芳香化酶抑制剂和硫酸酯酶抑制剂的研究进展。Breast cancer is one of malignant tumors heahh and even cause death. The traditional endocrine therapy that seriously impact women＇s physical and mental drugs of breast cancer are estrogen receptor modulators and aromatase inhibitors that act on metabolic pathway of endogenous estrogenic steroids. The objective of the research on this class of drugs is to find new aromatase inhibitors with tissue selectivity, high efficacy and low toxicity. Novel steroid sulfatase inhibitors are effective hormone dependent breast cancer （HDBC） treatment drugs. Sul- famate moiety is confirmed to be the pharmacophore of these drugs. This article reviews research advances in aro- matase inhibitors and steroid sulfatase inhibitors.

关 键 词：乳腺癌 雌激素 芳香化酶抑制剂 甾体硫酸酯酶抑制剂 

分 类 号：R979.12[医药卫生—药品]