Ketoconazole is a nonselective steroid 17α-hydroxylase/17,20 lyase (CYP17A1) inhibitor that has been used, off-label, as a second-line therapy for castration-resistant prostate cancer (CRPC). The drug has shown clinical efficacy without survival benefit. Despite not improving survival, ketoconazole has beneficial characteristics, such as its low cost, a relatively favourable toxicity profile compared with chemotherapy, and its efficacy both before and after chemotherapy. The approval of several new, highly effective treatments, including abiraterone acetate, enzalutamide, and apalutamide, warrants re-evaluation of the role of ketoconazole and other classic agents in achieving the optimal timing and sequencing of available agents to prolong survival and maintain patients’ quality of life. In the current CRPC treatment landscape, we believe that ketoconazole can be considered in patients with nonmetastatic CRPC and in those with metastatic CRPC who do not respond to, tolerate, or have access to chemotherapy and other standard therapeutic options.

酮康唑是一种非选择性类固醇 17α-羟化酶/17,20 裂解酶 (CYP17A1) 抑制剂，已在标签外用作去势抵抗性前列腺癌 (CRPC) 的二线治疗。该药物已显示出临床疗效，但没有生存益处。尽管没有提高生存率，但酮康唑具有有益的特性，例如成本低、与化疗相比毒性相对有利，以及在化疗前后均有效。包括醋酸阿比特龙、恩杂鲁胺和阿帕鲁胺在内的几种新的高效治疗方法的批准，需要重新评估酮康唑和其他经典药物在实现可用药物的最佳时机和顺序以延长生存期和维持患者质量方面的作用的生活。在当前的 CRPC 治疗环境中，