Springer, Private Bag 65901, Mairangi Bay, Auckland, 0754, New Zealand.
Drugs. 2018 Apr;78(6):699-705. doi: 10.1007/s40265-018-0900-z.
Apalutamide (Erleada) is a next-generation oral androgen receptor (AR) inhibitor that is being developed by Janssen for the treatment of prostate cancer (PC). It binds directly to the ligand-binding domain of the AR and blocks the effects of androgens. In February 2018, apalutamide received its first global approval in the USA for the treatment of non-metastatic castration-resistant PC (nmCRPC). Apalutamide is undergoing phase III investigation in chemotherapy-naive patients with metastatic CRPC (in combination with abiraterone acetate plus prednisone), patients with high-risk localized or locally advanced PC receiving primary radiation therapy, and in patients with metastatic hormone-sensitive PC and biochemically-relapsed PC. This article summarizes the milestones in the development of apalutamide leading to this first approval in nmCRPC.
阿帕鲁胺（Erleada）是一种新一代的口服雄激素受体（AR）抑制剂，由杨森（Janssen）公司开发用于治疗前列腺癌（PC）。它直接与 AR 的配体结合域结合，并阻断雄激素的作用。2018 年 2 月，阿帕鲁胺在美国首次获得全球批准，用于治疗非转移性去势抵抗性 PC（nmCRPC）。阿帕鲁胺正在接受 III 期研究，用于化疗初治的转移性 CRPC 患者（与醋酸阿比特龙联合泼尼松）、接受原发放射治疗的高危局限性或局部进展性 PC 患者，以及转移性激素敏感性 PC 和生化复发的 PC 患者。本文总结了导致阿帕鲁胺在 nmCRPC 中首次获批的开发里程碑。
