Pardanani A, Tefferi A
Division of Hematology, Department of Medicine, Mayo Clinic, Rochester, MN, USA.
Blood Cancer J. 2014 Dec 12;4(12):e268. doi: 10.1038/bcj.2014.84.
Ruxolitinib, a Janus kinase (JAK)-1 and JAK-2 inhibitor, is the first-in-class drug to be licensed in the United States for the treatment of high- and intermediate-risk myelofibrosis (MF). Several other JAK inhibitors are in development with some currently undergoing phase-3 clinical trial testing. None of the currently available JAK inhibitors are specific to mutant JAK2; their mechanism of action involves attenuation of JAK-STAT signaling with downregulation of proinflammatory cytokines, rather than selective suppression of the disease clone. Accordingly, while ruxolitinib and other JAK inhibitors are effective in controlling splenomegaly and alleviating constitutional symptoms, their benefit in terms of reversing bone marrow fibrosis or inducing complete or partial remissions appears to be limited. The experience to date with ruxolitinib shows that despite its salutary effects on quality of life, over half of the patients discontinue treatment within 2-3 years. In the current perspective, we examine the incidence and causes of ruxolitinib 'treatment failure' in MF patients based on our personal experience as well as a review of the published literature. We also discuss the challenges in defining and classifying ruxolitinib failure, and within the context of several clinical scenarios, we provide recommendations for the post-ruxolitinib management of MF patients.
芦可替尼是一种Janus激酶(JAK)-1和JAK-2抑制剂,是美国首个获批用于治疗高危和中危骨髓纤维化(MF)的同类药物。其他几种JAK抑制剂也在研发中,其中一些目前正在进行3期临床试验。目前可用的JAK抑制剂均对突变型JAK2无特异性;它们的作用机制是通过下调促炎细胞因子来减弱JAK-STAT信号传导,而不是选择性抑制疾病克隆。因此,虽然芦可替尼和其他JAK抑制剂在控制脾肿大和缓解全身症状方面有效,但它们在逆转骨髓纤维化或诱导完全或部分缓解方面的益处似乎有限。迄今为止,芦可替尼的使用经验表明,尽管它对生活质量有有益影响,但超过一半的患者在2至3年内停止治疗。在当前的观点中,我们根据个人经验以及对已发表文献的回顾,研究MF患者中芦可替尼“治疗失败”的发生率和原因。我们还讨论了定义和分类芦可替尼治疗失败的挑战,并在几种临床场景的背景下,为MF患者芦可替尼治疗后的管理提供建议。