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摘要: 乳腺癌作为全球女性发病率最高的癌症,一直威胁着全世界女性的健康。雌激素受体(estrogen receptor,ER)介导的信号通路在乳腺癌疾病发展中扮演着重要的角色,成为乳腺癌治疗的重要靶点之一,一直吸引着许多药企进行相关药物的研发。2002年,由阿斯利康开发的首个选择性雌激素受体下调剂(selective estrogen receptor down-regulators,SERDs)——氟维司群正式在美国上市。氟维司群通过下调ER水平,全面抑制ER信号通路,临床疗效优于其他内分泌治疗药物,使得SERDs受到越来越多药企的关注。然而,肌内注射限制了氟维司群的临床应用,表明SERDs的开发仍有很大提升空间。综述相关SERDs的研发现状,为进一步研究与应用提供参考。Abstract: As the cancer with the highest incidence in women worldwide, breast cancer has always been a big threat to the health of women around the world. Estrogen receptor(ER) signaling pathway plays an important role during the pathogenesis of breast cancer. As an important target for the treatment of breast cancer, ER has attracted many pharmaceutical companies to develop related drugs. In 2002, the first selective estrogen receptor down-regulators(SERDs) developed by AstraZeneca-fulvestrant was officially launched in the United States. By reducing ER levels, fulvestrant shows a full inhibition of ER signaling pathway and superior clinical effects to other endocrine drugs. This makes SERDs get more and more attention from pharmaceutical companies. However, the clinical application of fulvestrant bas been limited by intramuscular injection, leaving much room for the improvement of SERDs. This review introduces the development status of SERDs, so as to provide reference for further research and application.
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Keywords:
- estrogen receptor /
- down-regulator /
- breast cancer treatment
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