Weaver A N, Jimeno A
Department of Medicine, Internal Medicine Residency Training Program, University of Alabama at Birmingham, Birmingham, Alabama, USA.
Department of Medicine, Division of Medical Oncology and Developmental Therapeutics Program, University of Colorado Cancer Center, Aurora, Colorado, USA.
Drugs Today (Barc). 2020 Aug;56(8):531-539. doi: 10.1358/dot.2020.56.8.3158047.
Mantle cell lymphoma (MCL) has historically been an aggressive disease with poor long-term survival. In the last decade, Bruton tyrosine kinase (BTK) inhibition has emerged as a new treatment strategy for MCL, especially in the relapsed/refractory (r/r) setting. Zanubrutinib, a second-generation BTK inhibitor, was approved by the U.S. Food and Drug Administration (FDA) in late 2019 for r/r MCL on the basis of combined overall response rate of 84% in a total of 118 patients from two multicenter clinical trials, BGB-3111-AU-003 and BGB-3111-206. Duration of response was 14-18 months. Although 57% of patients developed grade 3 and 4 adverse side effects including anemia, pneumonia and neutropenia, only 8% discontinued treatment suggesting zanubrutinib monotherapy was fairly well tolerated. As compared to first-generation ibrutinib, zanubrutinib has higher BTK selectivity which may result in fewer off-target effects and improved potential for combination with other targeted therapies. In addition to a confirmatory phase III trial, there are multiple ongoing studies evaluating zanubrutinib as part of two- and three-drug regimens in MCL and other B-cell malignancies. These current results and areas of further interest indicate an exciting future for zanubrutinib in the treatment of MCL.
套细胞淋巴瘤(MCL)一直以来都是一种侵袭性疾病,长期生存率较低。在过去十年中,布鲁顿酪氨酸激酶(BTK)抑制已成为MCL的一种新治疗策略,尤其是在复发/难治性(r/r)情况下。泽布替尼是一种第二代BTK抑制剂,于2019年末被美国食品药品监督管理局(FDA)批准用于r/r MCL,这是基于两项多中心临床试验BGB-3111-AU-003和BGB-3111-206中总共118例患者84%的综合总缓解率。缓解持续时间为14至18个月。尽管57%的患者出现了3级和4级不良反应,包括贫血、肺炎和中性粒细胞减少,但只有8%的患者停止治疗,这表明泽布替尼单药治疗耐受性相当良好。与第一代伊布替尼相比,泽布替尼具有更高的BTK选择性,这可能导致脱靶效应更少,并提高与其他靶向疗法联合使用的潜力。除了一项确证性III期试验外,还有多项正在进行的研究在评估泽布替尼作为MCL和其他B细胞恶性肿瘤两药和三药方案的一部分。这些当前结果和进一步关注的领域表明泽布替尼在治疗MCL方面有着令人兴奋的前景。