阿帕他胺（ARN-509）治疗前列腺癌的研究进展

Updated progress of Apalutamide(ARN-509) in the treatment of prostate cancer

雄激素受体(AR)是治疗前列腺癌的重要靶点。然而,随着传统AR靶向药物治疗时间的延长,前列腺癌患者会出现治疗效果降低的现象。目前,研发针对AR的新型药物已成为前列腺癌治疗领域的研究热点;其中,随着对AR结构及其生物学功能的进一步了解,新一代强效AR拮抗剂-阿帕他胺(ARN-509)被成功合成,并且已在临床上表现出良好的疗效及安全性。为此,本文将历数新型AR靶向药物—阿帕他胺的研发历程,并对目前进行中/即将开展的ARN-509治疗前列腺癌相关Ⅲ期临床研究进行详细阐述。

The androgen receptor(AR)is an important target for the treatment of prostate cancer.However,with the prolongation of treatment with traditional AR-targeted drugs,the therapeutic effect is often reduced.At present,developing novel AR-targeted drugs has become a research hotspot in the field of prostate cancer treatment.With further understanding of AR structure and its biological functions,a novel and potent AR antagonist-Apaludamide(ARN-509)has been successfully synthesized and has shown good efficacy and safety in clinical practice.This article will review the development of Apalutamide,and elaborate the ongoing or upcoming phaseⅢclinical studies on the treatment of prostate cancer with Apalutamide.