雄激素受体拮抗剂治疗前列腺癌新进展  

Androgen receptor antagonists in prostate cancer

作　　者：刘家舟 潘家骅[1] 薛蔚[1] LIU Jiazhou;PAN Jiahua;XUE Wei(Department of Urology,Renji Hospital,School of Medicine,Shanghai Jiaotong University,Shanghai 200127,China)

机构地区：[1]上海交通大学医学院附属仁济医院泌尿科,上海200127

出　　处：《现代泌尿外科杂志》2022年第3期268-272,274,共6页Journal of Modern Urology

基　　金：ELAVL3在神经内分泌型前列腺癌发生发展中的作用及分子机制(No.82072847)。

摘　　要：雄激素-受体轴及其下游信号传导通路在前列腺癌(PCa)发生发展中发挥重要作用,是传统雄激素剥夺治疗(ADT)的靶点。但PCa经过18~24个月的ADT后,将发展为去势抵抗性前列腺癌(CRPC),预后不良。近年来,直接作用于雄激素受体(AR)的新一代AR拮抗剂成为PCa药物治疗的热点。恩杂鲁胺、阿帕他胺、达络他胺先后进入临床,在基础研究中显示出对受体亲和力高、抗受体突变能力强等优势,在临床试验中也表现出对CRPC和激素敏感性PCa的疗效显著。本文就近年来新一代AR拮抗剂的研究进展进行总结综述。The androgen receptor(AR)axis plays a vital role in prostate cancer progression,which is the target of traditional androgen deprivation therapy(ADT).Unfortunately,after 18-24 months of ADT,prostate cancer is likely to progress despite the initial therapeutic effects and lead to poor prognosis.Such status is clinically termed castration-resistant prostate cancer.Re⁃cently,new-generation AR antagonists targeting androgen receptors have become the hotspot in prostate cancer treatment.Enzalutamide,apalutamide and darolutamide have been synthesized and put into practice.Preclinical studies have shown high po⁃tency and strong mutation resistance,while evidence in clinical trails indicates significant efficacy against castration-resistant and hormone-sensitive prostate cancer presented by these drugs.This review will summarize the latest study results on the new-generation AR antagonists.

关 键 词：前列腺肿瘤 雄激素受体拮抗剂 恩杂鲁胺 阿帕他胺 达络他胺 

分 类 号：R737[医药卫生—肿瘤]