Rhea L P, Mendez-Marti S, Aragon-Ching J B
Department of Internal Medicine, Inova Fairfax Hospital, Fairfax, Virginia, USA.
GU Medical Oncology, Inova Schar Cancer Institute, Fairfax, Virginia, USA.
Drugs Today (Barc). 2020 Mar;56(3):185-193. doi: 10.1358/dot.2020.56.3.3110574.
Darolutamide is a novel, nonsteroidal androgen receptor (AR)-signaling inhibitor. It serves as a second-generation antiandrogen and is currently indicated for the treatment of patients with nonmetastatic castration-resistant prostate cancer (nmCRPC). The product was approved by the United States Food and Drug Administration (FDA) in July 2019 and by the Japanese Ministry of Health, Labour and Welfare (MHLW) in January 2020 for the treatment of men with nmCRPC, and is awaiting approval in the E.U. for the same indication. This review will cover the background, preclinical development, safety, pharmacokinetics, pharmacodynamics and clinical studies that led to the approval of darolutamide. The key clinical data, ongoing trials and future directions for darolutamide are also discussed herein.
达洛鲁胺是一种新型非甾体雄激素受体（AR）信号抑制剂。它作为第二代抗雄激素药物，目前被用于治疗非转移性去势抵抗性前列腺癌（nmCRPC）患者。该产品于2019年7月获得美国食品药品监督管理局（FDA）批准，并于2020年1月获得日本厚生劳动省（MHLW）批准，用于治疗nmCRPC男性患者，目前正在等待欧盟对同一适应症的批准。本综述将涵盖达洛鲁胺获批背后的背景、临床前开发、安全性、药代动力学、药效学及临床研究。本文还讨论了达洛鲁胺的关键临床数据、正在进行的试验以及未来方向。
