Greene Teshell K, Lambert Michele P, Poncz Mortimer
Department of Pediatrics, The Children's Hospital of Philadelphia and the University of Pennsylvania School of Medicine, Philadelphia, PA 19104, USA.
J Genet Syndr Gene Ther. 2011 Nov 12;Suppl 1(1). doi: 10.4172/2157-7412.S1-001.
Hemophilia A is the most common inherited bleeding diathesis and is due to a deficiency of functional coagulation factor (F) VIII. Most patients have a severe deficiency and require a program of prophylactic plus acute infusions of recombinant FVIII to prevent significant joint and other target organ damage. One of the greatest challenges remaining in the care of these patients is that one fifth to third of the patients develop inhibitors to the infused proteins. While a significant portion of such inhibitors can be either overcome or the inhibitors eliminated, some patients with persistent and significant titers of inhibitors need to rely on second tier therapies that are not as effective at preventing significant bleeding morbidity or mortality. A number of groups have been developing therapeutic strategies for FVIII gene therapy for this disorder. Virtually all of these therapies have in common a rise in the plasma level of FVIII, and interpretation of their efficacy is straightforward related to levels achieved. However, several groups have also shown that FVIII can be ectopically expressed in developing megakaryocytes, where although plasma FVIII levels remain undetectable, this FVIII can be released and be effective at sites of platelet activation. Moreover, it is clear that this platelet (p) FVIII is protected to a degree from inhibitors, making pFVIII a particularly attractive strategy for gene therapy for hemophilia A. Yet at the same time, we have shown that pFVIII has a different availability and distribution in a growing thrombus than plasma FVIII. The clinical implications and challenges of these findings as murine and canine hemophilia A preclinical studies go forward with pFVIII are discussed.
甲型血友病是最常见的遗传性出血素质,是由于功能性凝血因子(F)VIII缺乏所致。大多数患者存在严重缺乏,需要进行预防性加急性输注重组FVIII的方案,以防止严重的关节和其他靶器官损伤。在这些患者的护理中,仍然存在的最大挑战之一是五分之一到三分之一的患者会产生针对输注蛋白的抑制剂。虽然这类抑制剂中的很大一部分可以被克服或消除,但一些抑制剂滴度持续且显著的患者需要依赖二线治疗,而这些治疗在预防严重出血发病率或死亡率方面效果不佳。许多研究小组一直在为这种疾病开发FVIII基因治疗的策略。几乎所有这些治疗方法的共同之处在于血浆FVIII水平升高,其疗效的解释与所达到的水平直接相关。然而,几个研究小组也表明,FVIII可以在发育中的巨核细胞中异位表达,尽管血浆FVIII水平仍检测不到,但这种FVIII可以释放并在血小板激活部位发挥作用。此外,很明显这种血小板(p)FVIII在一定程度上受到抑制剂的保护,这使得pFVIII成为甲型血友病基因治疗特别有吸引力的策略。然而,与此同时,我们已经表明,在正在形成的血栓中,pFVIII与血浆FVIII具有不同的可用性和分布。随着小鼠和犬类甲型血友病临床前研究对pFVIII继续推进,将讨论这些发现的临床意义和挑战。