Veterans Affairs Medical Centre and the Baylor College of Medicine, Houston, TX, USA.
Eur Urol. 2011 Aug;60(2):270-8. doi: 10.1016/j.eururo.2011.04.032. Epub 2011 Apr 29.
The development of agents targeting androgen signalling holds promise for men with castration-resistant prostate cancer (CRPC).
The emerging role of abiraterone acetate (AA), a novel, orally administered androgen synthesis inhibitor, is critically analysed.
Data were acquired from critically important original research published in peer-reviewed literature or presented at conferences conducted by the American Society of Clinical Oncology and the European Society of Medical Oncology.
The major findings are addressed in an evidence-based, objective, and balanced fashion.
AA specifically inhibits CYP17 and substantially reduces serum androgen levels without inducing significant adrenal insufficiency. A phase 3 trial reported a significant extension of survival in metastatic CRPC with AA plus prednisone compared to prednisone alone following docetaxel. The primary toxicity of mineralocorticoid excess is manageable. The addition of low-dose corticosteroids to AA may be necessary for controlling symptoms of mineralocorticoid excess.
针对雄激素信号的药物的发展为去势抵抗性前列腺癌（CRPC）患者带来了希望。
对新型口服雄激素合成抑制剂醋酸阿比特龙（AA）的新作用进行了批判性分析。
数据来源于在同行评议文献中发表的重要原始研究或在美国临床肿瘤学会和欧洲肿瘤内科学会会议上发表的研究。
主要发现以循证、客观和平衡的方式呈现。
AA 特异性抑制 CYP17，并显著降低血清雄激素水平，而不会引起明显的肾上腺功能不全。一项 3 期试验报告称，与单独使用泼尼松龙相比，AA 加泼尼松龙可显著延长转移性 CRPC 患者的生存期，这些患者在多西他赛治疗后。盐皮质激素过多的主要毒性是可以控制的。对于控制盐皮质激素过多的症状，可能需要将低剂量皮质类固醇添加到 AA 中。
