Gale Rosemary E, Hills Robert, Pizzey Arnold R, Kottaridis Panagiotis D, Swirsky David, Gilkes Amanda F, Nugent Elizabeth, Mills Kenneth I, Wheatley Keith, Solomon Ellen, Burnett Alan K, Linch David C, Grimwade David
Department of Haematology, University College London Hospitals, United Kingdom.
Blood. 2005 Dec 1;106(12):3768-76. doi: 10.1182/blood-2005-04-1746. Epub 2005 Aug 16.
The prognostic significance of FLT3 mutations in acute promyelocytic leukemia (APL) is not firmly established and is of particular interest given the opportunities for targeted therapies using FLT3 inhibitors. We studied 203 patients with PML-RARA-positive APL; 43% of the patients had an FLT3 mutation (65 internal tandem duplications [ITDs], 19 D835/I836, 4 ITD+D835/I836). Both mutations were associated with higher white blood cell (WBC) count at presentation; 75% of the patients with WBC counts of 10 x 10(9)/L or greater had mutant FLT3. FLT3/ITDs were correlated with M3v subtype (P < .001), bcr3 PML breakpoint (P < .001), and expression of reciprocal RARA-PML transcripts (P = .01). Microarray analysis revealed differences in expression profiles among patients with FLT3/ITD, D835/I836, and wild-type FLT3. Patients with mutant FLT3 had a higher rate of induction death (19% vs 9%; P = .04, but no significant difference in relapse risk (28% vs 23%; P = .5) or overall survival (59% vs 67%; P = .2) at 5 years. In in vitro differentiation assays using primary APL blasts (n = 6), the FLT3 inhibitor CEP-701 had a greater effect on cell survival/proliferation in FLT3/ITD+ cells, but this inhibition was reduced in the presence of ATRA. Furthermore, in the presence of CEP-701, ATRA-induced differentiation was reduced in FLT3/ITD+ cells. These data carry implications for the use of FLT3 inhibitors as frontline therapy for APL.
急性早幼粒细胞白血病(APL)中FLT3突变的预后意义尚未明确确立,鉴于使用FLT3抑制剂进行靶向治疗的可能性,这一问题尤其受到关注。我们研究了203例PML-RARA阳性的APL患者;43%的患者存在FLT3突变(65例内部串联重复[ITD],19例D835/I836,4例ITD+D835/I836)。两种突变均与初诊时较高的白细胞(WBC)计数相关;白细胞计数≥10×10⁹/L的患者中75%存在FLT3突变。FLT3/ITD与M3v亚型(P<0.001)、bcr3 PML断点(P<0.001)以及相互的RARA-PML转录本表达(P=0.01)相关。微阵列分析显示FLT3/ITD、D835/I836和野生型FLT3患者之间的表达谱存在差异。FLT3突变患者诱导死亡的发生率较高(19%对9%;P=0.04),但5年时复发风险(28%对23%;P=0.5)或总生存率(59%对67%;P=0.2)无显著差异。在使用原代APL母细胞(n=6)进行的体外分化试验中,FLT3抑制剂CEP-701对FLT3/ITD+细胞的细胞存活/增殖有更大影响,但在全反式维甲酸(ATRA)存在的情况下这种抑制作用减弱。此外,在CEP-701存在的情况下,FLT3/ITD+细胞中ATRA诱导的分化减少。这些数据对将FLT3抑制剂用作APL的一线治疗具有启示意义。