三种新型雄激素受体抑制剂的研究进展  

Research progress of three new androgen receptor inhibitors

作　　者：何芳 郝俊旭 陈立江[1] HE Fang;HAO Jun-xu;CHEN Li-jiang(School of Pharmacy,Liaoning University,Shenyang LIAONING 110036,China)

机构地区：[1]辽宁大学药学院,辽宁沈阳110036

出　　处：《中国新药与临床杂志》2021年第6期411-416,共6页Chinese Journal of New Drugs and Clinical Remedies

摘　　要：雄激素受体(AR)在前列腺癌(PC)的发展过程中发挥着重要的作用,通过抑制AR进入细胞核来治疗PC逐渐成为研究热点,并以此为基础研发出一系列的AR抑制剂类药物。由于患者长时间使用第一代AR抑制剂药物产生了一系列不良反应,新型无激动剂活性的AR抑制剂药物恩扎卢胺、阿帕他胺和达罗他胺相继被研发上市。鉴于新型AR抑制剂的治疗价值,国内企业也加大了对新型AR抑制剂的自主研发。Androgen receptor(AR) plays an important role in the development of prostate cancer(PC). The treatment of PC by inhibiting the entry of AR into the nucleus has gradually become a research hotspot, so a series of AR inhibitors have been developed on the base. Due to a series of adverse reactions caused by long-term use of the firstgeneration AR inhibitors, new AR inhibitors with no agonist activity, such as enzalutamide, apalutamide and darolutamide, have been developed and marketed. In view of the therapeutic value of new AR inhibitors, domestic enterprises have also increased the independent research and development of new AR inhibitors.

关 键 词：前列腺肿瘤 受体 雄激素 雄激素受体拮抗剂 恩扎卢胺 阿帕他胺 达罗他胺 

分 类 号：R961[医药卫生—药理学] R977[医药卫生—药学]