Division of Hematology, Tisch Cancer Institute, Mount Sinai School of Medicine, New York, NY 10029, USA.
Br J Haematol. 2013 Apr;161(1):68-75. doi: 10.1111/bjh.12220. Epub 2013 Jan 21.
Panobinostat (LBH589), a novel histone deacetylase inhibitor (HDACi), was evaluated in a phase I study of patients with primary myelofibrosis (PMF) and post-essential thrombocythaemia/polycythaemia vera-related myelofibrosis (Post-ET/PV MF). Eighteen patients (PMF 56%; Post-PV MF 28%; Post-ET MF 17%) were treated in three cohorts at oral doses of (i) 20, (ii) 30, and (iii) 25 mg three times weekly consecutively. Reversible thrombocytopenia was the dose-limiting toxicity. Five patients (two in Dose Cohort 1, one in Dose Cohort 2 and two in Dose Cohort 3) received six or more cycles and were evaluable for response assessment. After the sixth cycle, three of these five patients achieved clinical improvement (CI) with 100% reduction in palpable splenomegaly from baseline, and two patients experienced stable disease. Panobinostat therapy was also associated with improvement in the degree of anaemia in two of the five patients. Of the three patients who achieved CI after six cycles, one patient achieved a near complete remission after 15 cycles of treatment and another patient had resolution of marrow fibrosis after 16 cycles. We conclude that panobinostat is a well-tolerated, clinically active treatment for MF patients, regardless of JAK2 V617F status, and most effective when given at low doses over long periods of time.
泊那替尼(LBH589)是一种新型组蛋白去乙酰化酶抑制剂(HDACi),在原发性骨髓纤维化(PMF)和原发性血小板增多症/真性红细胞增多症相关骨髓纤维化(Post-ET/PV MF)患者的 I 期研究中进行了评估。18 名患者(PMF 占 56%;Post-PV MF 占 28%;Post-ET MF 占 17%)分别在三个队列中接受口服剂量(i)20、(ii)30 和(iii)25mg,每周连续服用 3 次。可逆性血小板减少是剂量限制性毒性。5 名患者(剂量队列 1 中有 2 名,剂量队列 2 中有 1 名,剂量队列 3 中有 2 名)接受了 6 个或更多周期的治疗,可进行反应评估。在第六个周期后,这 5 名患者中的 3 名达到了临床改善(CI),从基线开始,可触及的脾肿大减少了 100%,2 名患者病情稳定。泊那替尼治疗还可改善 5 名患者中的 2 名患者的贫血程度。在 6 个周期后达到 CI 的 3 名患者中,1 名患者在 15 个周期的治疗后达到了接近完全缓解,另 1 名患者在 16 个周期后骨髓纤维化得到了缓解。我们得出结论,泊那替尼是一种耐受性良好、具有临床活性的 MF 患者治疗药物,与 JAK2 V617F 状态无关,并且在长时间内低剂量给药时效果最佳。