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恩杂鲁胺:一种新型抗雄激素药物,可延长 CRPC 患者的生存率。

Enzalutamide: a novel anti-androgen with prolonged survival rate in CRPC patients.

机构信息

Department of Pharmaceutical Chemistry, ISF College of Pharmacy, Ferozepur Road, Moga-142 001, India.

出版信息

Mini Rev Med Chem. 2013 Aug;13(10):1475-86. doi: 10.2174/13895575113139990003.

Abstract

Prostate cancer is the most common malignancy among men found to be the second leading cause of male cancer-related mortality due to development of resistance against androgen deprivation therapy (ADT). With the advancement in understanding of prostate cancer, numbers of agents have been emerged to target Androgen-Receptor (AR) signaling for the treatment of castration resistant prostate cancer (CRPC). Food and Drug Administration (FDA) has recently approved enzalutamide (XTANDI) for the treatment of CRPC. Androgen receptor promotes the prostate cancer progression after transformation. Androgen receptor signaling leads to CRPC when cellular nucleus binds to DNA and increases pro cancer gene expression. In phase ΙΙΙ clinical trial, enzalutamide showed that 160 mg once daily oral administration is well tolerated and significantly enhanced overall survival in men with CRPC after chemotherapy, demonstrated by reduction in the serum prostate specific antigen (PSA) level and increased survival rate by 4.8 months.

摘要

前列腺癌是男性中最常见的恶性肿瘤,由于对雄激素剥夺疗法 (ADT) 的耐药性的发展,它已成为男性癌症相关死亡的第二大主要原因。随着对前列腺癌认识的提高,已经出现了许多针对雄激素受体 (AR) 信号的药物来治疗去势抵抗性前列腺癌 (CRPC)。美国食品和药物管理局 (FDA) 最近批准恩杂鲁胺 (XTANDI) 用于治疗 CRPC。雄激素受体在转化后促进前列腺癌的进展。当细胞核与 DNA 结合并增加致癌基因的表达时,雄激素受体信号导致 CRPC。在 III 期临床试验中,恩杂鲁胺显示,每日一次口服 160mg 剂量可耐受良好,并显著提高了化疗后 CRPC 男性的总生存率,表现为血清前列腺特异性抗原 (PSA) 水平降低和生存率提高 4.8 个月。

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