Kreitman Robert J, Pastan Ira
The Laboratory of Molecular Biology, National Cancer Institute, National Institutes of Health, 37/5124b, 9000 Rockville Pike Bethesda, MD 20892-4255, USA.
The Laboratory of Molecular Biology, National Cancer Institute, National Institutes of Health, 37/5124b, 9000 Rockville Pike Bethesda, MD 20892-4255, USA.
Best Pract Res Clin Haematol. 2015 Dec;28(4):236-45. doi: 10.1016/j.beha.2015.09.003. Epub 2015 Oct 9.
Hairy cell leukemia (HCL) is an indolent B-cell malignancy effectively treated but not often cured by purine analog therapy; after multiple courses of purine analogs, patients can become purine analog resistant and in need of alternative therapies. Complete remission to single-agent purine analog is often accompanied by minimal residual disease (MRD), residual HCL cells detectable by immunologic methods, considered a risk factor for eventual relapse. Several different non-chemotherapy approaches are being used to target relapsed and refractory HCL, including inhibitors of BRAF, but so far only monoclonal antibody (MAb)-based approaches have been reported to eliminate MRD in a high percentage of patients. One of the MAb-based options for HCL currently under clinical investigation involves recombinant immunotoxins, containing a fragment of a MAb and a bacterial toxin. The bacterial toxin, a highly potent fragment from Pseudomonas exotoxin, catalytically ADP-ribosylates elongation factor 2 (EF2), resulting in protein synthesis inhibition and apoptotic cell death. Recombinant immunotoxins tested in HCL patients include LMB-2, targeting CD25, and BL22, targeting CD22. An affinity matured version of BL22, termed moxetumomab pasudotox (formerly HA22 or CAT-8015) achieved high CR rates in phase I, and is currently undergoing multicenter Phase 3 testing. Phase I testing was without dose-limiting toxicity, although 2 patients had grade 2 hemolytic uremic syndrome (HUS) with transient grade 1 abnormalities in platelets and creatinine. Preclinical work is underway to identify residues on moxetumomab pasudotox leading to immunogenicity. Moxetumomab pasudotox is undergoing pivotal testing for relapsed and refractory HCL.
毛细胞白血病(HCL)是一种惰性B细胞恶性肿瘤,嘌呤类似物疗法可有效治疗但通常无法治愈;经过多疗程嘌呤类似物治疗后,患者可能会对嘌呤类似物产生耐药性,需要替代疗法。单药嘌呤类似物治疗达到完全缓解时,通常伴有微小残留病(MRD),即通过免疫方法可检测到残留的HCL细胞,这被认为是最终复发的危险因素。目前正在使用几种不同的非化疗方法来治疗复发难治性HCL,包括BRAF抑制剂,但到目前为止,只有基于单克隆抗体(MAb)的方法被报道能在高比例患者中消除MRD。目前正在临床研究的HCL基于MAb的治疗选择之一涉及重组免疫毒素,其包含MAb片段和细菌毒素。该细菌毒素是来自铜绿假单胞菌外毒素的高效片段,催化ADP-核糖基化延伸因子2(EF2),导致蛋白质合成抑制和凋亡性细胞死亡。在HCL患者中测试的重组免疫毒素包括靶向CD25的LMB-2和靶向CD22的BL22。BL22的亲和力成熟版本,即莫西妥莫单抗帕苏妥昔(以前称为HA22或CAT-8015)在I期试验中达到了高缓解率,目前正在进行多中心3期试验。I期试验没有剂量限制性毒性,尽管有2例患者出现2级溶血尿毒综合征(HUS),血小板和肌酐有短暂的1级异常。目前正在进行临床前研究,以确定莫西妥莫单抗帕苏妥昔上导致免疫原性的残基。莫西妥莫单抗帕苏妥昔正在进行复发难治性HCL的关键试验。