Department of Haematology, Leeds Teaching Hospitals NHS Trust, Level 3 Bexley Wing, St James's University Hospital, Leeds LS9 7TF, UK.
Dana-Farber Cancer Institute, Boston, MA 02215, USA.
Future Oncol. 2020 Apr;16(10):517-523. doi: 10.2217/fon-2019-0844. Epub 2020 Mar 24.
Treatment standards for chronic lymphocytic leukemia (CLL) have been transformed with the advent of effective inhibitors of B-cell receptor signaling such as ibrutinib - a first-in-class inhibitor of BTK. Off-target kinase inhibitions by ibrutinib are thought to contribute to its adverse events. Zanubrutinib is a next-generation BTK inhibitor with minimal off-target effects, sustained BTK occupancy in peripheral blood mononuclear cells and lymph nodes from patients with B-cell malignancies and promising responses in patients with CLL. Described here is a head-to-head Phase III study comparing the efficacy and safety of zanubrutinib with those of ibrutinib in patients with CLL/small lymphocytic lymphoma in the relapsed/refractory setting.
慢性淋巴细胞白血病 (CLL) 的治疗标准随着 B 细胞受体信号有效抑制剂（如伊布替尼）的出现而发生了转变——伊布替尼是首个 BTK 抑制剂。伊布替尼的非靶点激酶抑制作用被认为是其不良事件的原因。泽布替尼是一种下一代 BTK 抑制剂，具有最小的非靶点作用，可在 B 细胞恶性肿瘤患者的外周血单核细胞和淋巴结中持续占据 BTK，并在 CLL 患者中产生有前景的反应。这里描述的是一项头对头的 III 期研究，比较了泽布替尼与伊布替尼在复发/难治性 CLL/小淋巴细胞淋巴瘤患者中的疗效和安全性。
