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阿帕鲁胺用于治疗去势抵抗性前列腺癌患者。

Apalutamide for the treatment of patients with castration-resistant prostate cancer.

作者信息

Hauke R

机构信息

Nebraska Cancer Specialists, Omaha, Nebraska, USA.

出版信息

Drugs Today (Barc). 2018 Oct;54(10):585-590. doi: 10.1358/dot.2018.54.10.2885880.

Abstract

Patients with recurrent, nonmetastatic prostate cancer after curative intent therapy can experience a heterogeneous clinical course ranging from indolent disease that can be observed for years to a rapidly progressive disease that is metastatic in a relatively short time. Patients with short prostate-specific antigen (PSA) doubling times are at risk for early development of metastatic disease and are frequently placed on androgen deprivation therapy. Although castration-resistant disease inevitably occurs in these patients, most therapies for castration-resistant disease have shown benefit in the metastatic setting. Apalutamide is a nonsteroidal antiandrogen agent that binds directly to the ligand-binding domain of the androgen receptor, preventing androgen receptor translocation, DNA binding and androgen receptor-mediated transcription. Apalutamide showed improved metastasis-free survival and prolonged time to symptomatic progression in men with nonmetastatic castration-resistant prostate cancer with a short PSA doubling time.

摘要

接受根治性治疗后复发的非转移性前列腺癌患者可能经历异质性的临床病程,从可观察数年的惰性疾病到在相对短时间内发生转移的快速进展性疾病。前列腺特异性抗原(PSA)倍增时间短的患者有早期发生转移性疾病的风险,常接受雄激素剥夺治疗。尽管这些患者不可避免地会出现去势抵抗性疾病,但大多数去势抵抗性疾病的治疗在转移性情况下已显示出益处。阿帕他胺是一种非甾体类抗雄激素药物,它直接与雄激素受体的配体结合域结合,阻止雄激素受体易位、DNA结合以及雄激素受体介导的转录。对于PSA倍增时间短的非转移性去势抵抗性前列腺癌男性患者,阿帕他胺显示出无转移生存期改善和有症状进展时间延长。

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